MedWorm: Chemists

More Industrial Espionage

In the Pipeline — Tue, 07 Feb 2012 16:41:01 +0100

Well, we last got into arguments about industrial espionage here in December, so it's what? February already? Then here we go: from C&E News, we have this: Federal prosecutors charged last week that Chinese government officials played a role in the theft from Dupont of technology to manufacture the paint pigment titanium dioxide. According to a document filed on Jan. 31 in U.S. District Court for the Northern District of California, Federal Bureau of Investigation officials obtained letters in a search of the home of Walter Liew. The letters show that Liew “was tasked by representatives of the People’s Republic of China government to obtain technology used to build chloride-route titanium dioxide factories,” prosecutors say. Here are more details from Reuters. More on this as it d...

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Tau Spreads On Its Own?

In the Pipeline — Tue, 07 Feb 2012 13:33:09 +0100

I've been meaning to mention the very interesting work that's shown up on tau protein in Alzheimer's. That's generally taken a back seat to amyloid in the protein-pathologies-of-Alzheimer's derby, but no one has been able to rule it out as a causative event, either. And the progress of tau pathology through the brain is quite suggestive - it tends to start in one region (the entorhinal cortex) and spread from there. The question is, what's driving that process? Is it tau itself spreading, or perhaps something inside the cell that causes tau problems is spreading, or is it some set of external conditions (that lead to tau pathologies) which is spreading? This latest work goes a good way towards settling that question. (Here's one group's paper in PLoS One; the other paper in Neuron doesn't...

Direct Enantioselective Arylation of Amides

Organometallic Current — Tue, 07 Feb 2012 05:00:00 +0100

Angewchem Synthesis of 3-Fluoro-3-aryl Oxindoles: Direct Enantioselective Arylation of Amides Linglin Wu, Laura Falivene, Dr. Emma Drinkel, Sharday Grant, Priv.-Doz. Dr. Anthony Linden, Prof. Dr. Luigi Cavallo and Prof. Dr. Reto Dorta (Source: Organometallic Current)

Cooperative Effects in Palladium-Catalyzed Enantioselective C(sp3)–H Functionalization

Organometallic Current — Tue, 07 Feb 2012 05:00:00 +0100

Angewchem Chiral Monodentate Phosphines and Bulky Carboxylic Acids: Cooperative Effects in Palladium-Catalyzed Enantioselective C(sp3)–H Functionalization Tanguy Saget, Sébastien J. Lemouzy and Prof. Dr. Nicolai Cramer (Source: Organometallic Current)

spirocyclic oxindoles via a direct C–H, Ar–H functionalisation

Organometallic Current — Tue, 07 Feb 2012 05:00:00 +0100

TL Copper-catalysed approach to spirocyclic oxindoles via a direct C–H, Ar–H functionalisationCatherine L. Moody, Vilius Franckevičius, Pauline Drouhin, Johannes E.M.N. Klein, Richard J.K. Taylor (Source: Organometallic Current)

Academia and Industry, Suing Each Other

In the Pipeline — Mon, 06 Feb 2012 16:51:13 +0100

This is not the sort of academic-industry interaction I had in mind. There's a gigantic lawsuit underway between Agios and the Abramson Institute at the University of Pennsylvania, alleging intellectual property theft. There are plenty more details at PatentBaristas: According to the complaint filed in the US District Court Southern District Of New York, the Institute was created by an agreement between The Abramson Family Foundation and the Trustees of the University of Pennsylvania. The Foundation donated over $110 Million Dollars to the Institute with the condition that the money was to be used to explore new and different approaches to cancer treatment. Dr. Thompson later created a for-profit corporation that he concealed from the Institute. After a name change, that entity became th...

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Let's Start Off the Meeting With An Ad, OK?

In the Pipeline — Mon, 06 Feb 2012 16:42:43 +0100

I'm sitting in the main conference hall at the SLAS meeting as things get going. And I have to say, it's a big crowd, and there are some very interesting things on the agenda. But I've just seen something I've never seen before: an ad being played on the screens for the entire attending audience, just before the keynote address. Thermo Scientific has clearly put a lot of money into this meeting (as well they should), but sitting through a NFL-voice-over style ad during the kickoff to a scientific meeting ("The power to win!" is a real first. (Source: In the Pipeline)

The Academic-Industrial Collaboration in Drug Discovery Panel: Today

In the Pipeline — Mon, 06 Feb 2012 13:36:30 +0100

As mentioned before, I'm going to be moderating a panel today on industry-academic collaborations in drug discovery at the SLAS meeting in San Diego. It starts at 10:30 AM Pacific Time, and you can access a live stream of the event here (scroll down). And if anyone has more questions on the subject they'd like to see raised (or things that they'd rather not see raised again!), please add them to the comments for this post. I'll be checking it during the day. (Source: In the Pipeline)

Glass Structure, Atom by Atom

In the Pipeline — Mon, 06 Feb 2012 05:07:54 +0100

For a really stunning electron micrograph of the thinnest possible layer of glass, see here. (If you don't have journal access, here's a release with some details). What's even more striking is that the semi-random arrangement of atoms is basically an exact match of a hypothesis from 1932 by W. H. Zachariasen at Chicago. And maybe it's just me, but high-resolution images of molecular structure like this still give me the shivers. I mean, I've seen all sorts of electron density maps from X-ray crystallography, but somehow this sort of thing gives one a more direct feeling of looking at the individual atoms. And for some reason, that seems like something Man Was Not Meant to Do - perhaps it's all those old elementary school textbooks that told me that atoms could never be seen. (Then again,...

How the Andrulis Paper Got Published

In the Pipeline — Fri, 03 Feb 2012 19:43:32 +0100

The editor of the journal Life has published an attempt at detailing how the notorious Andrulis paper managed to make its way into print. See how convincing you find it. In the course of explaining that it can be hard to find reviewers for interdisciplinary topics, and how the journal tries to find reputable people in each field (and carefully checks author suggestions for reviewers), we have this: Life is a new journal that deals with new and sometime difficult interdisciplinary matters. Consequently, the journal will occasionally be presented with submitted articles that are controversial and/or outside conventional scientific views. Some papers recently accepted for publication in Life have attracted significant attention. Moreover, members of the Editorial Board have objected to these...

AstraZeneca in Waltham

In the Pipeline — Fri, 03 Feb 2012 12:26:50 +0100

From several reports, here's what I have on AstraZeneca's plans in Waltham: they've told people there that cuts are coming. But they haven't gotten very specific on when, or who, or how many. All those questions (that is, all the questions there could be) are under review. Pfizer has done this to their people before, as have other companies in the throes of layoffs, and it's the only way I know to actually push morale and productivity down even further in such a situation. You come to work for weeks, for months, not knowing if your, your lab, or your whole department is heading for the chopping block. All you're sure of is that someone is. And will your own stellar performance persuade upper management to keep you, when the time comes? Not likely, under these conditions - it'll more likel...

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Fluorine NMR: Why Not?

In the Pipeline — Thu, 02 Feb 2012 16:50:37 +0100

Fluorine NMR is underused in chemistry. Well, then again, maybe it's not, but it's one of those thing that just seems like it should have more uses than it does. (Here's a recent bookon the subject). Fluorine is a great NMR nucleus - all the F in the world is the same isotope, unless you're right next to a PET scanning facility - and the different compound show up over a very wide range of chemical shifts. You've got that going for you, coupling information, NOE, basically all your friends from proton NMR. There's a pretty recent paper showing a good use of all these qualities (blogged about here at Practical Fragments as well). A group at Amgen reports on their work using fluorine NMR as a fragment-screening tool. They can take mixtures of 10 or 12 compounds at a time (because of all tho...

AstraZeneca Layoffs and Closings

In the Pipeline — Thu, 02 Feb 2012 02:50:20 +0100

Update: it's all true. 7,300 job cuts in total. Montreal and Soedertaelje (Sweden) to close. And AZ seems to be all but getting out of pain/CNS, cutting down to a few dozen people who will do external collaborations. Oh, and they're buying back 4.5 billion dollars worth of stock, instead of spending that money on what the company tries to make a profit on. So there is that. If you'd like to hear AZ tell you how all this is making them more productive, here's the press release. I've been hearing reports, which I hope are incorrect but as yet have no reason to doubt, that the AstraZeneca site in Montreal is set to close as a result of this latest round of layoffs. The official announcement is coming in a few hours - I wanted to put up this post so that more details can be added in the comme...

Potassium Hydride Is Not Your Friend

In the Pipeline — Wed, 01 Feb 2012 13:26:02 +0100

Noted chem-blogger Milkshake seems to have had a close call with a fire started by a tiny potassium hydride residue. It looks like he made it through without serious injury, but that sort of thing will definitely shake a person up. I hate potassium hydride. Its relative sodium hydride is a common reagent, but it's much tamer (and even so, can cause interesting fires - I knew someone who ignited a heap of it on the pan of a balance while he was weighing it out, which slowed things down a bit). Sodium hydride is usually sold as a 60% dispersion, a dark grey powder soaked with mineral oil to keep it from deteriorating too quickly (and to keep it from setting everything on fire). You can buy 95% sodium hydride, the dry stuff, and there are people who swear by it, but I tend to sweat at it. Yo...

Smugness as a Warning Sign

In the Pipeline — Wed, 01 Feb 2012 12:18:23 +0100

At Xconomy, Luke Timmerman has words of wisdom for people in the small biotech world: "Never back smug". That's a quote from venture capitalist Bob More, and it rings true to me as well. Says TImmerman: ". . .it strikes me that life sciences has more than its share of spinmeisters, hypesters, smoke-and-mirrors actors, and worse." Then there’s smugness, that arrogance or sense of superiority. Developing innovative new drugs or devices requires a strong ego, high IQ, stamina, an inspiring personality that attracts other people, and other things. Often, that combination spills over into smugness or arrogance. More says he watches for a lot of the same cues that his sister, a teacher, watches for. . . I suspect that many readers will have encountered this trait (very occasionally) in their...

Oxidation of the Methylene Group of Aryl(di)azinylmethanes

Organometallic Current — Wed, 01 Feb 2012 05:00:00 +0100

Angewchem Synthesis of Aryl(di)azinyl Ketones through Copper- and Iron-catalyzed Oxidation of the Methylene Group of Aryl(di)azinylmethanes Johan De Houwer, Prof. Dr. Kourosch Abbaspour Tehrani and Prof. Dr. Bert U. W. Maes (Source: Organometallic Current)

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Atom- and Step-Economical Pathway to Chiral Benzobicyclo[2.2.2]octenones

Organometallic Current — Wed, 01 Feb 2012 05:00:00 +0100

Angewchem Atom- and Step-Economical Pathway to Chiral Benzobicyclo[2.2.2]octenones through Carbon–Carbon Bond Cleavage Dr. Lantao Liu, Dr. Naoki Ishida and Prof. Dr. Masahiro Murakami (Source: Organometallic Current)

A General Solution for the 2-Pyridyl Problem

Organometallic Current — Wed, 01 Feb 2012 05:00:00 +0100

Angewchem A General Solution for the 2-Pyridyl Problem Graham R. Dick, Eric M. Woerly and Prof. Martin D. Burke (Source: Organometallic Current)

Oxidative Trifluoromethylthiolation of Aryl Boronic Acids

Organometallic Current — Wed, 01 Feb 2012 05:00:00 +0100

Angewchem Copper-Catalyzed Oxidative Trifluoromethylthiolation of Aryl Boronic Acids with TMSCF3 and Elemental Sulfur Chao Chen, Yan Xie, Lingling Chu, Dr. Ruo-Wen Wang, Prof. Dr. Xingang Zhang and Prof. Dr. Feng-Ling Qing (Source: Organometallic Current)

The Andrulis Paper's Fallout

In the Pipeline — Tue, 31 Jan 2012 17:30:11 +0100

The fallout from the bizarre Andrulis paper continues. Carl Zimmer reports that editorial board members are resigning from the journal, having had no idea that their names would wind up over something like this. Naturally, that brings up the question of just who did let this thing through the review process, but my bet is that we'll never know. Whoever signed off on it is no doubt running for cover. Another useful feature this affair has had is the chance to see who just posts press releases for fun and profit, and who has some tiny residual bit of editorial discretion. In the former category, apparently, are PhysOrg.com and ScienceDaily.com (the latter has taken down their post. But then again, the Times of India bit for it as well. . . (Source: In the Pipeline)

AstraZeneca Cutting Even More?

In the Pipeline — Tue, 31 Jan 2012 15:56:01 +0100

OK, this is one of those less-than-cheerful mornings on the blog, apparently. Word is in the British press that AstraZeneca is preparing to announce thousands more job cuts later this week. No more concrete details yet - all the company has said is that "clear focus on cash and value creation will continue", and isn't that just about the most encouraging thing you've ever heard? More as this develops. (Source: In the Pipeline)

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The Future of Pharma? Yikes.

In the Pipeline — Tue, 31 Jan 2012 15:11:00 +0100

Someone has been soaking up the atmosphere at a large pharma company, for sure. "Look, I'm a chemist. I thought you hired me to do chemistry. But so far, all I've heard is gibberish. . .don't you do chemistry here?". Some of you may enjoy that, but for others, it might just be a bit too realistic to be amusing. . . The same user has several other videos on YouTube, such as this one, which (in addition to a few four-letter words), features the phrase "Get off the Kool-Aid!" Clearly someone needs to go through some more training. (Thanks to Pharmalot for the original link). (Source: In the Pipeline)

Catalytic Enantioselective Saucy–Marbet Claisen Rearrangement

Organometallic Current — Tue, 31 Jan 2012 05:00:00 +0100

Angewchem Asymmetric Synthesis of Allenyl Oxindoles and Spirooxindoles by a Catalytic Enantioselective Saucy–Marbet Claisen Rearrangement Trung Cao, Joshua Deitch, Dr. Elizabeth C. Linton and Prof. Marisa C. Kozlowski (Source: Organometallic Current)

Dehydrogenative Aryl-Aryl Bond Formation

Organometallic Current — Tue, 31 Jan 2012 05:00:00 +0100

Angewchem [RhIIICp*]-Catalyzed Dehydrogenative Aryl-Aryl Bond Formation Dr. Joanna Wencel-Delord, Corinna Nimphius, Prof. Dr. Frederic W. Patureau and Prof. Dr. Frank Glorius (Source: Organometallic Current)

Stereoselective Metal-Free Oxyaminations

Organometallic Current — Tue, 31 Jan 2012 05:00:00 +0100

Angewchem Highly Stereoselective Metal-Free Oxyaminations Using Chiral Hypervalent Iodine Reagents Umar Farid and Prof. Dr. Thomas Wirth (Source: Organometallic Current)

Intramolecular Redox-Triggered C-H Functionalization

Organometallic Current — Tue, 31 Jan 2012 05:00:00 +0100

Angewchem Intramolecular Redox-Triggered C-H Functionalization Dr. Igor D. Jurberg, Dr. Bo Peng, Eckhard Wöstefeld, Maximilian Wasserloos and Dr. Nuno Maulide (Source: Organometallic Current)

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Intermolecular Coupling of 2-Silylaryl Bromides with Alkynes

Organometallic Current — Tue, 31 Jan 2012 05:00:00 +0100

Angewchem Palladium-Catalyzed Intermolecular Coupling of 2-Silylaryl Bromides with Alkynes: Synthesis of Benzosiloles and Heteroarene-Fused Siloles by Catalytic Cleavage of the C(sp3)-Si Bond Dr. Yun Liang, Weizhi Geng, Junnian Wei and Prof. Dr. Zhenfeng Xi (Source: Organometallic Current)

Carbomagnesiation of Alkynyl(aryl)thioethers

Organometallic Current — Tue, 31 Jan 2012 05:00:00 +0100

Angewchem Synthesis of Functionalized Benzo[b]thiophenes by the Intramolecular Copper-Catalyzed Carbomagnesiation of Alkynyl(aryl)thioethers M. Sc. Thomas Kunz and Prof. Dr. Paul Knochel (Source: Organometallic Current)

General and Convenient Reduction of Aromatic and Aliphatic Primary Amides

Organometallic Current — Tue, 31 Jan 2012 05:00:00 +0100

Angewchem Two Iron Catalysts are Better than One: A General and Convenient Reduction of Aromatic and Aliphatic Primary Amides Dr. Shoubhik Das, Bianca Wendt, Dr. Konstanze Möller, Dr. Kathrin Junge and Prof. Dr. Matthias Beller (Source: Organometallic Current)

Easy Access to Functionalized Pyrroles

Organometallic Current — Tue, 31 Jan 2012 05:00:00 +0100

Angewchem Highly Regioselective Migration of the Sulfonyl Group: Easy Access to Functionalized Pyrroles Xiaoyi Xin, Dr. Dongping Wang, Dr. Xincheng Li and Prof. Dr. Boshun Wan (Source: Organometallic Current)

Intramolecular Oxidative Oxyarylation of Hydroxyalkenes

Organometallic Current — Tue, 31 Jan 2012 05:00:00 +0100

Angewchem Combined Oxypalladation/C-H Functionalization: Palladium(II)-Catalyzed Intramolecular Oxidative Oxyarylation of Hydroxyalkenes Rong Zhu and Prof. Dr. Stephen L. Buchwald (Source: Organometallic Current)

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Highly Efficient Narasaka–Heck Cyclizations

Organometallic Current — Tue, 31 Jan 2012 05:00:00 +0100

Angewchem Highly Efficient Narasaka–Heck Cyclizations Mediated by P(3,5-(CF3)2C6H3)3: Facile Access to N-Heterobicyclic Scaffolds Adele Faulkner and Dr. John F. Bower (Source: Organometallic Current)

Enantioselective Synthesis of Spiro Cyclopentane-1,3′-indoles

Organometallic Current — Tue, 31 Jan 2012 05:00:00 +0100

Angewchem Enantioselective Synthesis of Spiro Cyclopentane-1,3′-indoles and 2,3,4,9-Tetrahydro-1H-carbazoles by Iridium-Catalyzed Allylic Dearomatization and Stereospecific Migration Qing-Feng Wu, Chao Zheng and Prof. Dr. Shu-Li You (Source: Organometallic Current)

Conversion of Ketones to Enamides with Ammonia and Acetic Anhydride

Organometallic Current — Tue, 31 Jan 2012 05:00:00 +0100

Angewchem Direct Titanium-Mediated Conversion of Ketones to Enamides with Ammonia and Acetic Anhydride Dr. Jonathan T. Reeves, Zhulin Tan, Dr. Zhengxu S. Han, Dr. Guisheng Li, Dr. Yongda Zhang, Yibo Xu, Dr. Diana C. Reeves, Dr. Nina C. Gonnella, Dr. Shengli Ma, Dr. Heewon Lee, Dr. Bruce Z. Lu and Dr. Chris H. Senanayake (Source: Organometallic Current)

Asymmetric Hydrogenation of Benzofurans

Organometallic Current — Tue, 31 Jan 2012 05:00:00 +0100

Angewchem Ruthenium NHC Catalyzed Highly Asymmetric Hydrogenation of Benzofurans Dr. Nuria Ortega, Slawomir Urban, Bernhard Beiring and Prof. Dr. Frank Glorius (Source: Organometallic Current)

Oxidative C–H/N–H Bond Functionalizations of Anilines

Organometallic Current — Tue, 31 Jan 2012 05:00:00 +0100

OL Cationic Ruthenium(II) Catalysts for Oxidative C–H/N–H Bond Functionalizations of Anilines with Removable Directing Group: Synthesis of Indoles in WaterLutz Ackermann and Alexander V. Lygin (Source: Organometallic Current)

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Pd-Catalyzed Regioselective C–H Olefination/Cyclization Sequence

Organometallic Current — Tue, 31 Jan 2012 05:00:00 +0100

OL Synthesis of Indolo [1,2-a]Quinoxalines via a Pd-Catalyzed Regioselective C–H Olefination/Cyclization SequenceLiang Wang, Wei Guo, Xiao-Xiao Zhang, Xu-Dong Xia, and Wen-Jing Xiao (Source: Organometallic Current)

Oxidative C–H Bond Olefination of N-Methoxybenzamides

Organometallic Current — Tue, 31 Jan 2012 05:00:00 +0100

OL Ruthenium-Catalyzed Oxidative C–H Bond Olefination of N-Methoxybenzamides Using an Oxidizing Directing GroupBin Li, Jianfeng Ma, Nuancheng Wang, Huiliang Feng, Shansheng Xu, and Baiquan Wang (Source: Organometallic Current)

Ruthenium-Catalyzed Oxidative C–H/O–H Bond Cleavages

Organometallic Current — Tue, 31 Jan 2012 05:00:00 +0100

OL Versatile Synthesis of Isocoumarins and α-Pyrones by Ruthenium-Catalyzed Oxidative C–H/O–H Bond CleavagesLutz Ackermann, Jola Pospech, Karolina Graczyk, and Karsten Rauch (Source: Organometallic Current)

One-Pot Synthesis of Dihydrobenzosiloles from Styrenes

Organometallic Current — Tue, 31 Jan 2012 05:00:00 +0100

OL General and Practical One-Pot Synthesis of Dihydrobenzosiloles from StyrenesAlexey Kuznetsov and Vladimir Gevorgyan (Source: Organometallic Current)

Xanthone Formation from 2-Aryloxybenzaldehydes

Organometallic Current — Tue, 31 Jan 2012 05:00:00 +0100

OL Rhodium-Catalyzed Xanthone Formation from 2-Aryloxybenzaldehydes via Cross-Dehydrogenative Coupling (CDC)Ping Wang, Honghua Rao, Ruimao Hua, and Chao-Jun Li (Source: Organometallic Current)

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Oxidative C(sp2)–H Cycloetherification of o-Arylphenols

Organometallic Current — Tue, 31 Jan 2012 05:00:00 +0100

OL Cu-Catalyzed Oxidative C(sp2)–H Cycloetherification of o-Arylphenols for the Preparation of DibenzofuransJiaji Zhao, Yong Wang, Yimiao He, Lanying Liu, and Qiang Zhu (Source: Organometallic Current)

Oxidative Lactonization and Diacetoxylation of Alkenes

Organometallic Current — Tue, 31 Jan 2012 05:00:00 +0100

JOC Triflic Acid Catalyzed Oxidative Lactonization and Diacetoxylation of Alkenes Using Peroxyacids as OxidantsYan-Biao Kang and Lutz H. Gade (Source: Organometallic Current)

(Un)stoppable Pixantrone

In the Pipeline — Mon, 30 Jan 2012 18:09:42 +0100

This one mixes two categories on the blog: "Regulatory Affairs" with "How Not to Do It". A small company called Cell Therapeutics (catchy name) has been developing pixantrone for last-ditch non-Hodgkin's lymphoma. You'll note from that Wikipedia article that this compound has been knocking around for a long time, and it's had a very hard road towards any sort of approval. In 2010, an FDA advisory committee voted it down 12-0, and from the sound of things, it wasn't even that close. But the company appealed and resubmitted, since hope springs eternal and all. They were heading towards an FDA decision next week, and the company's CEO was apparently been going around to investors telling them how confident he was of approval. You see, one of the drug's major critics at the FDA, he claimed, h...

Potassium hydride self-ignition

Org Prep Daily — Mon, 30 Jan 2012 17:40:46 +0100

I had a rather bad fire last Friday. I was washing a large jacketed glass reaction vessel used for polymer scale-ups, after pouring the reaction mixture out, and a tiny particle of potassium hydride (from this poorly quenched reaction) that was adhering to the bottom of the reaction flask ignited just as I was giving the flask a proper acetone rinse. So I had a flaming flask in my hands + burning hands + flaming sink in front + a whole bunch of wash bottles ablaze next to me (plastic wash bottles peeing their burning solvents around…) A colleague promptly put the fire out with a mid-sized CO2 fire extinguisher before the flames spread any further. There was no damage to the lab, my fingers or the reaction mixture but it was pretty scary situation – considering how fires in orga...

The Key to Everything? Not Quite.

In the Pipeline — Mon, 30 Jan 2012 12:57:49 +0100

Here's one of the strangest things I've ever seen in the scientific literature. A new journal, Life, apparently solicited papers for their inaugural issues, and one of them was from Erik Andrulis at Cast Western's School of Medicine. The manuscript came in at 105 printed pages, which should have rung at least a tiny alarm bell, you'd think. And if that wasn't a bit concerning, perhaps the title ("Theory of the Origin, Evolution, and Nature of Life") might have seemed a bit sweeping? Or the abstract, which promises that "The theoretical framework unifies the macrocosmic and microcosmic realms, validates predicted laws of nature, and solves the puzzle of the origin and evolution of cellular life in the universe." No? Nothing to worry about yet? But editors aren't supposed to just look at pa...

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George Whitesides: The Concept of the Scientific Paper is Eroding Before Our Very Eyes

Depth-First — Sun, 29 Jan 2012 00:00:34 +0100

George Whitesides is well known as an innovator and one of chemistry’s most visible representatives. He has the distinction of being credited with the highest Hirsch index for any living chemist. You could say he knows something about scientific publication. The above video excerpt was taken from an extended interview with Whitesides on the topic of publication. Although the full interview series is worth watching, most striking are Whitesides’ views on the changes happening in scientific publication and what the future is likely to hold: One of the troubles with universities is there’s a tendency to do terrific research, embed it in prose that is impenetrable even to experts, bury it in papers, and have to everyone’s surprise nothing come out of it. �...

Roche Goes Hostile for Illumina

In the Pipeline — Fri, 27 Jan 2012 14:39:23 +0100

Roche is not only a big drug company, it's a big diagnostics company. And that's what's driving their unsolicited bid for Illumina, a gene-sequencing company from San Diego. Illumina has been one of the big players in the "How quickly and cheaply can we sequence a person's entire genome" game, and apparently Roche believes that there's something in it for them. But as that Reuters link above shows, a lot of other people don't agree, and would rather partner than acquire (Chris Viehbacher, CEO of Sanofi, seems to have been waiting for the opportunity to unburden himself of thoughts to that effect). He may well be right. Sequencing has been a can-you-top-this field for some time, and I don't think that the process is finished yet. What if you buy a technology that's superseded before it has...

Arsenic Bacteria Ride Again. (Or Don't).

In the Pipeline — Fri, 27 Jan 2012 12:56:13 +0100

You may not have heard much about the arsenic-bacteria controversy recently, but you're about to hear quite a bit more. Rosie Redfield of UBC, one of the fastest and most vocal critics of the original paper, has been trying to reproduce it in her own group. There's a manuscript in preparation, but since she's been blogging on some of the progress, the import is clear: it hasn't been going well for the "bacteria can take up arsenic in their biomolecules" hypothesis. Scrolling back at that link will give you the story. Here's a summary at Nature News (with a clarification from Redfield on one point). I look forward to seeing how this plays out - but remember, the startling results always have to prove themselves by happening again. Einmal ist keinmal. Update: there's another story here, to...

Science, A Zero-Sum World, and the State of the Union

In the Pipeline — Thu, 26 Jan 2012 17:50:16 +0100

I always regret it when politics creeps into this blog. But I just finished reading this post over at The Economist's "Free Exchange" glog, and I can't resist linking to it. The author focuses on a few lines from the President's State of the Union speech, and gets rather agitated: Later, the president added: "Don’t let other countries win the race for the future." The context, innocuously enough, was in calling for greater support for American research and development efforts. But the language of this statement is either daft or ghastly, depending on how charitably one is willing to read it. Is Mr Obama so dense as to miss that when America invents things other countries benefit, and vice versa? If a German discovers a cure for cancer, shouldn't we be ecstatic about that, rather than a...

Putting a Number on Chemical Beauty

In the Pipeline — Thu, 26 Jan 2012 12:31:12 +0100

There's a new paper out in Nature Chemistry called "Quantifying the Chemical Beauty of Drugs". The authors are proposing a new "desirability score" for chemical structures in drug discovery, one that's an amalgam of physical and structural scores. To their credit, they didn't decide up front which of these things should be the miost important. Rather, they took eight properties over 770 well-known oral drugs, and set about figuring how much to weight each of them. (This was done, for the info-geeks among the crowd, by calculating the Shannon entropy for each possibility to maximize the information contained in the final model). Interestingly, this approach tended to give zero weight to the number of hydrogen-bond acceptors and to the polar surface area, which suggests that those two measur...

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Five Things to Do Instead of Protesting the Research Works Act (HR 3699)

Depth-First — Wed, 25 Jan 2012 21:29:56 +0100

Conclusions The resolution to the scientific publishing crisis will not come through a government bailout in the form of public access policies. It will come from starving entrenched old-guard publishers of the only value they’re currently adding to the scientific publication system - imprimatur. Regardless of whether you’re a leader in your field or just a concerned scientist, imprimatur comes from the combined perceptions of you and your peers. Fortunately, perceptions can change. The way to create a scientific publication system that advances the cause of science is to make it repugnant, ridiculous, and lonely to participate in one that doesn’t. (Source: Depth-First)

Panel on Academic-Industrial Collaboration in Drug Discovery

In the Pipeline — Wed, 25 Jan 2012 15:00:21 +0100

So, what questions should be asked? I've been asked to moderate a panel discussion ("Bridging the Valley of Death") at the upcoming Society for Laboratory Automation and Screening conference in San Diego. It's a session moderated by Bill Janzen from the University of North Carolina and Michelle Palmer from the Broad Institute, and the panelists are John Luk from the National University of Singapore, Rudy Juliano from UNC, Mao Mao from Pfizer (San Diego), Alan Palkowitz from Eli Lilly, and John Reed from Sanford-Burnham. The discussion will be live-streamed (I'll put up the link that day), so if you're interested in that sort of thing, tune in. And as it says here, questions will be gathered "through social media sites, expert opinions and audience participation". And since this is one of ...

Open Office Plans - A Question or Two

In the Pipeline — Wed, 25 Jan 2012 12:18:52 +0100

As a follow-up to that post on open offices (and the others referenced in it), I've had a letter from a reader who wonders the following: (1) How many recent research buildings have been built with open offices, as opposed to cubicles or actual office space? Is this the wave-of-the-future, or is it just a few high-profile examples getting attention? (2) Does anyone know of any examples where a research department has tried an open-office plan and moved back from it after the experience? Just to clarify, I don't mean large, relatively open lab spaces (those are pretty common, and often seem to work just fine). What's in question are the wide-open no-walls office and desk areas, with the extreme being the ones where no one has any actual assigned space at all. Thoughts? (Source: In the Pi...

Comments (And Everything Else) Are Back

In the Pipeline — Wed, 25 Jan 2012 12:12:10 +0100

Things are running around here again, after some problems with the comment system. Unfortunately, it looks like everything from about Monday mid-day disappeared into the Great Bit Bucket. That's unfortunate, since I know that there must have been some good stories in that "Weirdest Presentation" post - if anyone has the energy to add them again, there would be an audience for them! (Source: In the Pipeline)

Comment Trouble

In the Pipeline — Mon, 23 Jan 2012 23:46:46 +0100

I've noticed that comments to today's posts seem to have stopped appearing sometime around noon EST. Rooting around under the hood is ongoing; I'll let everyone know what the outcome is. With any luck, things can be rescued! (Source: In the Pipeline)

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This All Too Open Office

In the Pipeline — Mon, 23 Jan 2012 17:55:19 +0100

Since the topic of open offices in lab design has come up around here several times, I thought I'd point out this op-ed from the New York Times. It's from the author of a new book, Quiet: The Power of Introverts in a World That Can't Stop Talking, and you can guess her point from that title: SOLITUDE is out of fashion. Our companies, our schools and our culture are in thrall to an idea I call the New Groupthink, which holds that creativity and achievement come from an oddly gregarious place. Most of us now work in teams, in offices without walls, for managers who prize people skills above all. Lone geniuses are out. Collaboration is in. But there’s a problem with this view. Research strongly suggests that people are more creative when they enjoy privacy and freedom from interruption. ...

Strangest Presentation You've Seen?

In the Pipeline — Mon, 23 Jan 2012 13:55:15 +0100

Friday's mention of the Brindley lecture prompts me to throw this question out: what's the most weirdly memorable scientific presentation you've ever seen? I'll put one out there that still sticks in my mind. Back in 1998, I was attending the Gordon Conference on Heterocycles. One of the speakers was a young faculty member from Montana, who was supposed to be speaking on metal-catalyzed reactions of indoles. Instead, he came in with a completely different slide deck on origins-of-life chemistry, which made it clear, rather quickly, that he not only did not buy into the "RNA world" hypothesis, but considered it (and much other origins-of-life work) to be the next thing to a conspiracy. The audience took this in with some visible discomfort, as the talk itself became more passionate and ag...

Worst Lecture of All, Or Greatest?

In the Pipeline — Fri, 20 Jan 2012 16:40:54 +0100

Depends on your perspective! Since it's Friday, I present this memoir of the infamous Brindley lecture from 1983. G.S. Brindley appears to have been a pioneer in urology, and in fact discovered the first useful therapies for erectile dysfunction. But the way he chose to announce these discoveries to the world was. . .well, read the article. Let's just say that he was intent on leaving no doubts, and that no doubts were left. (Source: In the Pipeline)

Alnylam Cuts Back Hard

In the Pipeline — Fri, 20 Jan 2012 13:52:06 +0100

The news is that Alnylam, the RNAi company just down the street from where I'm writing, is cutting about a third of its workforce to try to get its best prospects through the clinic. This is a familiar story in the small-pharma world; there's often money to try to get things through the clinic, or to pay everyone in the earlier-stage R&D - but nowhere near enough money to do both. There are companies that have gone through this stage several times, sometimes rehiring the same people when the money began flowing again. You could see this coming, what with the news in that research space over the last couple of years. It's going to be a race to see if Alnylam can get something that will bring the income before time and resources get too tight. I wish them luck - I think there's really somet...

Zelboraf: Treat One Cancer, Speed Up Another?

In the Pipeline — Fri, 20 Jan 2012 12:27:50 +0100

You may well recall the excitement around the late-stage clinical data for Zelboraf (vermurafenib, PLX4032) in metastatic melanoma. The drug was approved late last summer, but (like all the other therapeutic options in oncology), it has its issues. One of those appears to be speeding up the course of squamous cell carcinoma. (Here's the NEJM article and the accompanying editorial). A significant number of patients on Zelboraf have turned up with this other form of skin cancer. To be sure, they surely had these cancerous cells beforehand (which tend to feature RAS mutations), but the effects of the drug on the MAP-kinase pathway seem to kick up their activity. (The same effect is seen on melanoma cells that don't have the V600E mutation - if you give Zelboraf without genotyping the patient...

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Digital Destruction in Scientific Publishing: Why This Scientist Supports the Research Works Act (HR 3699)

Depth-First — Thu, 19 Jan 2012 19:29:32 +0100

Conclusions We as scientist have nobody to blame but ourselves for the mess that scientific publication has become. If we lack the courage to risk career setbacks by publishing in ‘third-tier’ open access journals, experimenting with open science using the many free tools the Web offers, or boycotting old-guard publishers, then we must wait patiently for digital destruction to break this ridiculous cycle for us. (Source: Depth-First)

Dapagliflozin Goes Down (For the Last Time?)

In the Pipeline — Thu, 19 Jan 2012 17:47:04 +0100

To no one's surprise, the FDA has rejected dapagliflozin, an SGLT2 inhibitor for diabetes. The advisory panel voted it down back during the summer, and the agency has asked AstraZeneca and Bristol-Myers Squibb to provide more safety data. As it stands, the increased risk of bladder and breast cancer (small but significant) that was seen in the clinic just outweighs the drug's benefits. That's the sodium-glucose cotransporter 2, and what it does normally is reabsorb glucose in the kidney to keep it from going on into the urine and being lost. It's been the subject of quite a bit of drug development over the last few years, with the thought being that spilling glucose out of the bloodstream, as an adjunct to other diabetes therapy, might be more of a feature than a bug. Not with that safet...

Takeda Announces Cuts

In the Pipeline — Thu, 19 Jan 2012 14:09:07 +0100

2,800 over the next four years. More of them are in Europe than in the US (via the Nycomed acquisition), but there are hundreds of positions to be lost in this country, too. For now, the company seems to be just saying that they'll be in all parts of the organization, without much in the way of details. Those will, in time, become all too apparent. Add that to last week's Novartis announcement (about 2,000 jobs, mostly in sales and marketing), and we're not off to a great 2012 on this front, are we? (Source: In the Pipeline)

The Research Works Act: One (Two!) Against and One For

In the Pipeline — Thu, 19 Jan 2012 12:22:56 +0100

I noted that the Nature Publishing Group has come out against the proposed Research Works Act, which would roll back the requirement that research funded by the US government be made freely available after (at most) one year. They are, I believe, the largest and most prominent journal publisher to take such a stand (although I'll be glad to be wrong about that): NPG and Digital Science do not support the Research Works Act. NPG and Digital Science exist to support the creation and dissemination of human knowledge on a sustainable commercial basis. We seek to enable the open exchange of ideas, especially in scientific communities, in line with the requirements and objectives of relevant stakeholders. Update: from the comments, the AAAS (publishers of Science) have also come out against t...

Replacement process solvents

Org Prep Daily — Wed, 18 Jan 2012 17:45:04 +0100

A recent Organic Process R&D editorial (thanks Chemjobber for pointing it out) publicizes Pfizer Process Group green solvent replacement chart that discourages chemists from using solvents that are either known to be toxic, dangerous to use on large scale or are expensive to dispose as waste. OPR&D makes it now a submission policy that if you used a problematic solvent in your work you have to demonstrate in your paper that you tried (and failed) to find more process-friendly alternatives. I think it is a sensible policy for a chemistry process journal (and it probably makes the editors job of rejecting marginal manuscripts easier). Also, Innocentive challenge was recently promising an award (up to 8k) to a winning proposal for replacing dipolar aprotic solvents like DMF, DMAc, NM...

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Selling Sanofi's Compounds on the Side

In the Pipeline — Wed, 18 Jan 2012 16:20:40 +0100

Now here is an amazingly stupid move: a medicinal chemist at Sanofi (Yuan Li) downloaded a large set of proprietary compounds from the company's files, and founded another company on the side to sell them. Strangely enough, someone at Sanofi noticed that their in-house compounds were appearing for sale at Abby Pharmtech, of Newark, Delaware. (Better take a look at that web site while you can). It is supposedly the US subsidiary of Xiamon KAK, of Xiamen, China. According to this criminal complaint (thanks to Pharmalot for the link), Sanofi found (in May and June of last year) 6,000 of their internal compounds showing up on SciFinder as available from Abby. A search of Li's computer at Sanofi showed all sorts of useful stuff - a listing of 144,000 compounds in a file called "Abby Pharmtech"...

Fun With Epigenetics

In the Pipeline — Wed, 18 Jan 2012 14:06:46 +0100

If you've been looking around the literature over the last couple of years, you'll have seen an awful lot of excitement about epigenetic mechanisms. (Here's a whole book on that very subject, for the hard core). Just do a Google search with "epigenetic" and "drug discovery" in it, any combination you like, and then stand back. Articles, reviews, conferences, vendors, journals, startups - it's all there. Epigenetics refers to the various paths - and there are a bunch of them - to modify gene expression downstream of just the plain ol' DNA sequence. A lot of these are, as you'd imagine, involved in the way that the DNA itself is wound (and unwound) for expression. So you see enzymes that add and remove various switches to the outside of various histone proteins. You have histone acyltransfe...

Warp Drive Bio: Best Name or Worst?

In the Pipeline — Tue, 17 Jan 2012 16:28:49 +0100

There are small drug firms and there are small drug firms - if you know what I mean. Which category is Warp Drive Bio going to fall into? If you've never heard of them - and that name is rather memorable - then don't worry, they're new. Its founders are big names on the industry/academic drug discovery border: Greg Verdine, Jim Wells, and George Church. Here's the rundown: Warp Drive Bio is driving the reemergence of natural products in the era of genomics to create breakthrough treatments that make an important difference in the lives of patients. Built upon the belief that nature is the world's most powerful medicinal chemist, Warp Drive Bio is deploying a battery of state-of-the-art technologies to access powerful drugs that are now hidden within microbes. Key to the Warp Drive Bio ap...

Newhouse Research

In the Pipeline — Tue, 17 Jan 2012 16:22:02 +0100

Looks like the former Merck site in Newhouse is beginning to get some tenants as part of "Biocity Scotland". I wish everyone involved good luck - we need more smaller firms, because that's the only way to get larger firms. Isn't it? (Source: In the Pipeline)

Down With the Research Works Act

In the Pipeline — Tue, 17 Jan 2012 12:32:52 +0100

Back in December, a short bill was introduced in the House called the "Research Works Act". Its backers, Darrell Issa (R-CA) and Carolyn Maloney (D-NY), describe it as something that will maintain the US's standing in scientific publishing. After looking over its language and reading a number of commentaries on it, I have to disagree: this looks to me like shameless rent-seeking by the commercial scientific publishers. And it pains me to say that, because I know several people in that business. But it's a business whose long-term model has problems. (See the Addendum below if you're not in the field and want a brief summary of how scientific publishing works). The problem is, the work of the editorial staff has changed a good deal over the years. Back when everyone sent in hard copies of ...

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On the (F)utility of Extending the Molfile Format

Depth-First — Tue, 17 Jan 2012 03:59:07 +0100

Conclusions No amount of retrofitting will solve the fundamental flaws of V2000 as a chemical representation and information exchange format. They are: Optional specification of implicit hydrogen counts. Encoding the side effect properties of charge and bond order, rather than the fundamental property of electron count. Elevation of bonding and stereochemistry templates to the status of fundamental properties. Deeply-ingrained and restrictive notions of bonding that precludes multi-center bonds or bonds with odd electron counts. Decades of inertia on the part of software providers and the cheminformatics community. V3000 offers some true innovations in the areas of partial stereochemistry definition and biopolymer encoding that are worth underst...

Defending Das' Resvertrol Research. Oh, Come On.

In the Pipeline — Mon, 16 Jan 2012 13:34:46 +0100

I'm getting all the press releases from Bill Sardi, of Resveratrol Partners, as he does damage control from the Das scandal at UConn. And I have to say, he's putting in the hours getting these together. Problem is, on some key points, he doesn't know what his biggest problems are. The latest one is titled "World Without Resveratrol: Researcher Falsely Accused", and claims that this may all be a plan to "send a message" to any academic who collaborates with the makers of resveratrol pills. The release goes on about how these are old accusations, which Das has refuted since then, and asks why these ancient concerns are coming up now, eh? The phrase "orchestrated hit job" is used. But that glosses over the times of the whole investigation, which has been a very detailed and involved one, and...

Biogen: A "Decimated" Pipeline?

In the Pipeline — Mon, 16 Jan 2012 13:07:40 +0100

You don't want coverage like this: "Biogen CEO Tries to Refill Early-Stage Pipeline He Decimated". That would be George Scanos: . . .Scangos and his research chief eliminated about 17 early-stage drug projects in 2010 and last year to hone the company's focus, leaving it with only about four early-stage compounds. Biogen exited oncology and cardiovascular research and is now targeting drugs to treat neurological and autoimmune conditions. . . "We didn't want to fund projects that were unlikely to generate value," Scangos said in an interview on the sidelines of the J.P. Morgan health-care conference in San Francisco this week. . .But even if Biogen's late-stage pipeline delivers successful new drugs soon, the company needs more compounds in early-stage testing to sustain long-term growth...

Dealing With Dishonesty

In the Pipeline — Fri, 13 Jan 2012 16:22:15 +0100

So, we've been talking here since yesterday about what looks like large-scale fraud, but there's small-scale stuff that goes on inside various labs (often in academia, which is where people like this are supposed to wash out). Many readers will have encountered, in their grad school days, the person whose reactions won't quite reproduce, who comes in while you're not around and "borrows" your reagents, and who can't quite locate that key procedure when it's time to look at it closely. (And yes, I've had dealings with members of this tribe before, and they're no fun at all). Here's a reminiscence from a professor at Nebraska of how he dealt with someone like this, and his technique may be something that others have tried (or been tempted to). It worked, though. This is the flip side of the...

A Resveratrol Research Scandal. Oh, Joy.

In the Pipeline — Thu, 12 Jan 2012 17:05:12 +0100

My inbox has exploded with the story that many reports on the effects of resveratrol appear to be fraudulent. Prof. Dipak Das of Connecticut is at the center of what looks like a huge research stink bomb, which is being well covered by Retraction Watch (here and here), among others. The Chronicle of Higher Education has a lot of good info as well. Here's what's known so far: UConn has a press release saying that Das has been under investigation for the last three years, and that the university (along with the Office of Research Integrity) has uncovered substantial evidence of fraud and misconduct. An extensive research misconduct investigation has led the University of Connecticut Health Center to send letters of notification to 11 scientific journals that had published studies conducted...

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Sanofi's Bridgewater Site - Closing This Week?

In the Pipeline — Thu, 12 Jan 2012 13:44:28 +0100

Someone in a position to know has told me that Sanofi's Bridgewater, NJ site, which has long been a focus of layoffs, is now closing even faster than people thought. Originally, it was supposed to be "by the end of 2012". According to my source, though, they told everyone there yesterday that the last day would be Friday (!). No buyer for the site is known - rumor have had it that Allergan is interested, but that would seem to be far off, if indeed it's happening at all. Any more details out there? (Source: In the Pipeline)

Welcome To the Jungle! Here's Your Panther.

In the Pipeline — Thu, 12 Jan 2012 12:45:58 +0100

English has no word of its own for schadenfreude, so we've had to appropriate the German one, and we're in the process of making it our own - just as we did with "kindergarten", not to mention "ketchup" and "pyjamas", among fifty zillion more. That's because the emotion is not peculiar to German culture, oh no. We can feel shameful joy at others' discomfort with the best of them - like, for example, when people start to discover from experience just how hard drug discovery really is. John LaMattina has an example over at Drug Truths. Noting the end of a research partnership between Eli Lilly and the Indian company Zydus Cadila, he picked up on this language: “Developing a new drug from scratch is getting more expensive due to increased regulatory scrutiny and high costs of clinical tri...

Ten Years of Science Blogging. Already?

In the Pipeline — Wed, 11 Jan 2012 13:21:07 +0100

Today marks my ten-year blogging anniversary. That doesn't seem possible, but there it is: ten years since I sat down and chose a Blogger template and starting typing away into the void. So what have I learned in all that time (and after all that blather?) Where It Fits and How It's Done I may well have been the first science blogger, because it didn't take me long to start talking about drug discovery, as opposed to current events and the like. (Even in 2002, I thought that blogging the news was an overcrowded field, and little did I know how much more crowded it would become). But blogging drug discovery still isn't a very crowded field at all, for various reasons. One of those surely is that most of it is done in an industrial setting, and very few people have felt comfortable blogging...

The JP Morgan Myths

In the Pipeline — Mon, 09 Jan 2012 16:24:26 +0100

The JP Morgan Healthcare Conference is underway this week out in San Francisco, so there are a lot of biotech/pharma headlines to come out of that. Luke Timmerman over at Xconomy has "Five Myths" to come out of the conference. Unfortunately, two of them are that biotech IPOs are picking up, and that the general mood is upbeat. . . (Source: In the Pipeline)

A Look Into the Future?

In the Pipeline — Mon, 09 Jan 2012 13:40:55 +0100

For a look into a possible drug-discovery future (from the computational optimist viewpoint), you might want to check out a brief bit of science fiction, "Alpha Shock", in the Journal of Computer-Aided Molecular Design. Some excerpts to give you the general idea: ". . .Of course, the compounds were of little value if they couldn’t be formulated. Sanjay was pressed for time, and nanobot development still took several weeks, so he had to go “old school.” Sanjay accessed World Crystallography Repository’s (WCR) formulation suite and entered the 2D structures of his compounds. The system linked to the Amazon Hyper-Cloud and initiated a series of quantum chemical calculations to develop a custom force field for the solid phase simulations. Unfortunately the preliminary results were dis...

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SciFinder Access For the Unemployed

In the Pipeline — Fri, 06 Jan 2012 21:05:25 +0100

If you had SciFinder access, but are now unemployed and would like to use it during your job hunt, CAS now has a program to make that possible for free. I'm glad to see them taking this step; a lot of people have asked for something like this for some time now. (Source: In the Pipeline)

Do We Believe These Things, Or Not?

In the Pipeline — Fri, 06 Jan 2012 14:15:16 +0100

Some of the discussions that come up here around clinical attrition rates and compound properties prompts me to see how much we can agree on. So, are these propositions controversial, or not? 1. Too many drugs fail in clinical trials. We are having a great deal of trouble going on with these failure rates, given the expense involved. 2. A significant number of these failures are due to lack of efficacy - either none at all, or not enough. 2a. Fixing efficacy failures is hard, since it seems to require deeper knowledge, case-by-case, of disease mechanisms. As it stands, we get a significant amount of this knowledge from our drug failures themselves. 2b. Better target selection without such detailed knowledge is hard to come by. Good phenotypic assays are perhaps the only shortcut, but a...

Reaction to Andy Grove's Clinical Trial Proposals

In the Pipeline — Thu, 05 Jan 2012 16:18:28 +0100

I should mention that Science is publishing some letters that it received in response to Andy Grove's proposal to rework the clinical trial system for drug development. Sidney Wolfe and Michael Carome of Public Citizen aren't too happy with the idea, as you might expect. Their take, as I would reword it, could be summarized as "Hey, the existing system allows the drug industry to spew unsafe crap all over the market, and this would make it even worse". Actually, the language in their letter isn't far off: A. Grove proposes returning to the era before the enactment of the 1938 Federal Food, Drug, and Cosmetic Act, when new drugs were marketed in the United States without evidence that they were safe or effective. His irrational and dangerous proposal, which would limit the Food and Drug ...

Lead-Oriented Synthesis - What Might That Be?

In the Pipeline — Thu, 05 Jan 2012 12:20:41 +0100

A new paper in Angewandte Chemie tries to open another front in relations between academic and drug industry chemists. It's from several authors at GSK-Stevenage, and it proposes something they're calling "Lead-Oriented Synthesis". So what's that? Well, the paper itself starts out as a quick tutorial on the state and practice of medicinal chemistry. That's a good plan, since Angewandte Chemie is not primarily a med-chem journal (he said with a straight face). Actually, it has the opposite reputation, a forum where high-end academic chemistry gets showplaced. So the authors start off by reminded the readership what drug discovery entails. And although we've had plenty of discussions around here about these topics, I think that most people can agree on the main points laid out: 1. Physical...

The Changing Literature

In the Pipeline — Wed, 04 Jan 2012 17:43:06 +0100

The folks behind Retraction Watch (Adam Marcus and Ivan Oransky) have a piece in Nature on what it's been like since they started the blog. They note a new trend - for new data to appear when a retraction is called for (or made), but without any clarity about whether these new corroborative results have been peer-reviewed themselves. And they're absolutely right that a retraction should state exactly why the paper is being retracted; those "This paper has been withdrawn by the authors" notices are less than useless.Their experiences have them calling for a different way of looking at scientific papers in general: ". . . It is important to point out that an increase in retractions isn't necessarily a bad thing, because they correct the scientific record. But the greater visibility of pape...

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Osiris And Their Stem Cells

In the Pipeline — Wed, 04 Jan 2012 13:21:06 +0100

The topic of whether stem-cell therapies are overhyped - OK, let me show my cards, the topic of just how overhyped they are - last came up around here in November, when Geron announced that they were getting out of the business. And yesterday had a good example of why people tend to hold their noses and fan away the fumes whenever a company press-releases something in this area. I'm talking about Osiris Therapeutics, who have been working for some time on a possible stem cell therapy (called Prochymal) for Type I diabetes. That's certainly not a crazy idea, although it is an ambitious one - after all, you get Type I when your insulin-producing cells die off, so why not replace them? Mind you, we're not quite sure why your insulin-producing cells die off in the first place, so there's room...

2012 In Startups

In the Pipeline — Tue, 03 Jan 2012 18:01:10 +0100

Looking over the startup funding landscape, Bruce Booth finds some reasons for optimism. I hope he's right. There's a notch cut out of the small pharma/biotech ecosystem, a gap representing all the companies that didn't get formed in the last few years. Filling that has to be a good thing. (Source: In the Pipeline)

That's Sir Andrew to You

In the Pipeline — Tue, 03 Jan 2012 15:15:20 +0100

A reader in the UK sends along the news that GlaxoSmithKline's CEO, Andrew Witty, made the New Year's Honours list. His knighthood really put the "Sir" in "Sirtris acquisition", doesn't it? (Source: In the Pipeline)

The Research World Staggers Back to Work

In the Pipeline — Tue, 03 Jan 2012 13:34:17 +0100

Let's see here. . .145 messages in the work e-mail queue, but most of them are automated reminders that reminded me of the same thing every day of the break. Now to the lab bench. . .now, that was a good idea, making sure that everything was labeled before leaving. As I've said here before, too many times you come back to a bunch of stuff that you were just sure that you're remember every detail of, and feel like a moron as you look at the label on the vial or flask: "Second batch". "Mostly clean". "Large run". Fascinating! Large run of what, exactly? I have, in years past, been reduced to running NMR and LC/MS on my own reactions just to try to figure out what they were, and that's not right. Reagents that I'd ordered back before the break have come in, and I do recall why I ordered them...

Nowhere to Go But Up?

In the Pipeline — Wed, 28 Dec 2011 17:27:14 +0100

I wanted to let people know that I've got a "Perspective" piece in ACS Medicinal Chemistry Letters, entitled "Nowhere to Go But Up?". The journal is starting to run these opinion/overview articles, and contacted me for one - I hope it's the sort of thing that they were looking for! (Source: In the Pipeline)

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The UCLA Lab Fatality: Criminal Charges Filed

In the Pipeline — Wed, 28 Dec 2011 17:02:17 +0100

Most readers here will remember the fatal lab accident at UCLA in 2009 involving t-butyllithium, which took the life of graduate student Sheri Sangji. Well, there's a new sequel to that: the professor involved, Patrick Harran, has been charged along with UCLA with a felony: "willfully violating occupational health and safety standards". A warrant has been issued for his arrest; he plans to turn himself in when he returns from out of town this season. The University could face fines of up to $1.5 million per charge; Harran faces possible jail time. This is the first time I've heard of such a case going to criminal prosecution, and I'm still not sure what I think about it. It's true that the lab was found to have several safety violations in an inspection before the accident - but, on the o...

Media Note

In the Pipeline — Fri, 23 Dec 2011 15:46:40 +0100

I'm going to be on a short segment of Marketplace on public radio tonight, talking about cancer therapy. So if your holidays aren't complete without hearing me vent my opinions - and my wife, among others, tells me that hers aren't! - then tune in. (Source: In the Pipeline)

Holiday Break

In the Pipeline — Fri, 23 Dec 2011 15:20:46 +0100

Posting will be irregular next week for the holidays. I may put up a recipe or two, the way I did last year, and I'll certainly jump in for any big stories that might pop up. Otherwise, I'll be lounging around, gathering my strength for the new year. And hoping that we don't get what we got last year - relentless snowstorms, pounding in one after the other, which started about one day after Christmas. The less time I spend slogging through 40 inches of the stuff to go out and rake it off the roof, the better. Makes it rather difficult for a guy to set up a telescope, too, even in the unlikely event of a clear sky. So I'd like to take this opportunity to wish everyone who's celebrating it a Merry Christmas, and I'll certainly throw in a Happy Hanukah as well. The Iranians have already cele...

More From Hua - A Change of Business Plans?

In the Pipeline — Thu, 22 Dec 2011 15:24:00 +0100

You may remember the mention of Hua Pharmaceuticals here back in August, and the follow-up with details from the company. They're trying to in-license drugs from other companies and get them approved as quickly as possible in China. The original C&E News article made them sound wildly ambitious, while the company's own information just made them sound very ambitious. Now we have some more information: Roche has licensed their glucokinase activator program (for diabetes) to Hua (that's a development effort I wrote about here). And that's an interesting development, because the Hua folks told me that: "Hua Medicine intends to in-license patented drugs from the US and EU, and get them on the market and commercialized in the 4 year timeframe in China. This is about the average time it takes ...

Merry Christmas, Fred

In the Pipeline — Thu, 22 Dec 2011 14:27:01 +0100

I believe that this story has been mentioned in the comments here, but since I've heard from the actual person involved, I thought I'd pass on the canonical version. Someone I used to work with at Schering-Plough found himself (like many others in his position) out of a job in late October. He had a previously scheduled trip to Florida the next day, and as he boarded the plane, who should he see sitting in first class but Fred Hassan, the CEO of Schering-Plough who'd helped engineer the deal with Merck? As the chemist involved put it, "After quickly scanning to make sure there wasn’t a body guard looking guy near him", he said "Hi, Fred!" Hassan looked up and asked "Do I know you?" "Well," said the chemist, "no, probably not, but I'm a medicinal chemist with Schering-Plough, and now Mer...

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Merry Christmas & Happy New Year