Login / Register for free to get access to My MedWorm

Chemists BlogsChemists Blogs RSS feedThis is an RSS file. You can use it to subscribe to this data in your favourite RSS reader, such as GoogleReader, or to display this data on your own website or blog. subscribe with MyMedWormSubscribe to this data using MyMedWorm.subscribe with GoogleReaderSubscribe to this data using GoogleReader.subscribe with BloglinesSubscribe to this data using Bloglines.subscribe with MyYahooSubscribe to this data using MyYahoo.

This page shows you the most recent publications within this specialty of the MedWorm directory.

Good Suppliers - And The Other Guysemail this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
Is it just me, or is the fine chemicals supply business getting even more out of hand than usual? I was just talking with a colleague who'd sourced an interesting intermediate, at the (steep!) price of about $900 for a gram. She placed the order and. . .you guessed it, the supplier immediately back-ordered it, saying the price had changed. It took someone from Purchasing to drag the new quote out of them (they apparently wouldn't give it over the phone). Now (to no one's surprise, I'm sure) the material is over $3000/gram, and will have a lead time of weeks. This sort of thing has gone one for a long time, of course. But ...
Source: In the Pipeline - March 18, 2010 Category: Chemists Tags: Life in the Drug Labs Source Type: blogs

More Blogrollemail this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
Here's another addition: A New Merck, Reviewed, which is someone's attempt to dig through everything about the new Merck/Schering-Plough hybrid. I'm not sure that all the info is reliable, of course, and whoever writes this has a strange way with italics, but it's worth a look. Update: this turns out to be the Wordpress backup site for Shearlings Got Plowed, which I've mentioned here before. With the merger, the blog's author is covering his bases. (Source: In the Pipeline)
Source: In the Pipeline - March 17, 2010 Category: Chemists Tags: Blog Housekeeping Source Type: blogs

Dietary Supplements, Chartedemail this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
I'm a complete sucker for dense but well-presented information, and this one isn't bad at all: here's a chart of nutritional supplements by the strength of the evidence for them in human trials. I haven't cross-checked the data, but the authors appear to have done some homework in PubMed, at least, and haven't included any non-human or in vitro data. The interactive version at the link is particularly fun to mess around with. (Thanks to a reader and commenter here who put me on to this). (Source: In the Pipeline)
Source: In the Pipeline - March 17, 2010 Category: Chemists Tags: Snake Oil Source Type: blogs

Theft at Eli Lillyemail this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
$75 million dollars worth of antipsychotics - that's a lot of pills, and I'm not surprised to see that the thieves used a tractor-trailer to haul everything off. You'd have to assume that there's a well-worked-out pathway to unload all of these things, and that no one's going to go to all this trouble on "spec". Glad to see that my industry's products are so much in demand. . . (Source: In the Pipeline)
Source: In the Pipeline - March 17, 2010 Category: Chemists Tags: Current Events Source Type: blogs

BioTime's Cellular Aging Resultsemail this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
A small company called BioTime has gotten a lot of attention in the last couple of days after a press release about cellular aging. To give you an idea of the company's language, here's a quote: "Normal human cells were induced to reverse both the "clock" of differentiation (the process by which an embryonic stem cell becomes the many specialized differentiated cell types of the body), and the "clock" of cellular aging (telomere length)," BioTime reports. "As a result, aged differentiated cells became young stem cells capable of regeneration." Hey, that sounds good to me. But when I read their paper in the journal Regene...
Source: In the Pipeline - March 17, 2010 Category: Chemists Tags: Biological News Source Type: blogs

Science Buildings: Good, Bad, and Weirdemail this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
The entries I've done on the "open-plan" Biochemistry building at Oxford (see also Jim Hu) generated a lot of comments from people who've worked in poorly designed science facilities. I've heard from Linda Wang, a reporter at C&E News, who's writing article on this very subject. She's looking for chemists who are willing to talk about both good and bad experiences working in various building designs, so if you fit that description, feel free to email her at l_wang-at-acs.org (email address de-spammified, just substitute the usual symbol) or give her a call at 202-872-4579. (Source: In the Pipeline)
Source: In the Pipeline - March 17, 2010 Category: Chemists Tags: Life in the Drug Labs Source Type: blogs

Beta-Amyloid: An Antibiotic?email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
Now here's something that I don't think anyone expected. A recent paper in PLoS One makes the case that beta-amyloid, the protein that has been fingered for decades as a major player in Alzheimer's disease, is actually part of the body's antimicrobial defenses. Well, it's good to hear that it's doing something. Many people had hypothesized that it was a useless (indeed, harmful) byproduct, a waste stream from aberrant processing of the amyloid precursor protein (APP). Still, there have been reports over the years that beta-amyloid was substrate for active transport pumps, might be a ligand for various receptors, etc., bu...
Source: In the Pipeline - March 16, 2010 Category: Chemists Tags: Alzheimer ' s Disease Source Type: blogs

Terra Incognitaemail this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
I was thinking the other day about the sheer number of reasonable chemical structures that have never been made. Chemical space is famously roomy - that's how we make a living in the drug industry, since we prefer to make things that have never been made before. And it still surprises non-chemists when I tell them that I make new compounds all the time - the feeling, I think, is that anything that's reasonably easy to make surely must have been mined out long ago. Not so. (It's worth remembering, though, that just because something's never been reported doesn't always mean that you can't buy it). What brought this to mind...
Source: In the Pipeline - March 16, 2010 Category: Chemists Tags: The Scientific Literature Source Type: blogs

Stem Cell Politicsemail this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
There have been complaints that something is going wrong in the publication of stem cell research. This isn't my field, so I don't have a lot of inside knowledge to share, but there appear to have been a number of researchers charging that journals (and their reviewers) are favoring some research teams over others: The journal editor decides to publish the research paper usually when the majority of reviewers are satisfied. But professors Lovell-Badge and Smith believe that increasingly some reviewers are sending back negative comments or asking for unnecessary experiments to be carried out for spurious reasons. In some...
Source: In the Pipeline - March 15, 2010 Category: Chemists Tags: The Scientific Literature Source Type: blogs

Tricor's Troublesemail this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
It's easy to lose sight of what a drug is supposed to do. Many conditions come on so slowly that we have to use blood chemistry or other markers to see the progress of therapy in a realistic time. And over time, that blood marker can get confused with the disease itself. To pick one famous example, try cholesterol. Everyone you stop on the street will know that "high cholesterol is bad for you". But the first thing you have to do is distinguish between LDL and HDL cholesterol - if the latter is a large enough fraction of the total, the aggregate number doesn't matter as much. And fundamentally, there's not a disease calle...
Source: In the Pipeline - March 15, 2010 Category: Chemists Tags: Cardiovascular Disease Source Type: blogs

A job interviewemail this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
I just got first job interview invitation, end of this month. Its for a medicinal chemistry position – at a good place and with a group that I want to work in, and the project is also very interesting  - so please keep your fingers crossed for me. Also, there won’t be that many updates here in the next few weeks – obvious reasons. Maybe I can dig up some procedures from old notebooks but for now I decided put up here two totally ancient recordings (like 40 years old) of Czech blues that I am quite fond of. Sorry for the incomprehensible language and less-then-awesome sound quality. (Source: Org Prep Daily)
Source: Org Prep Daily - March 13, 2010 Category: Chemists Authors: milkshake Tags: Uncategorized Source Type: blogs

Blogroll Updateemail this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
Time to sweep out the inactive chemistry sites and bring in some new ones. Welcome to Chemistry Blog, Pharma Strategy Blog, Practical Fragments, Fragment -Based Drug Discovery Literature, Symyx Blog, and All Things Metathesis! And in the resources section, there's Chempedia Lab, a chemistry-question site that's looking for a broader user base. (Source: In the Pipeline)
Source: In the Pipeline - March 12, 2010 Category: Chemists Tags: Blog Housekeeping Source Type: blogs

The PSA Test for Prostate Cancer: Uselessemail this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
The discoverer of the prostate-specific antigen (Richard Ablin) has a most interesting Op-Ed in the New York Times. He's pointing out what people should already know: that using PSA as a screen for prostate cancer is not only useless, but actually harmful. The numbers just aren't there, and Ablin is right to call it a "hugely expensive public health disaster". Some readers will recall the discussion here of a potential Alzheimer's test, which illustrates some of the problems that diagnostic screens can have. But that was for a case where a test seemed as if it might be fairly accurate (just not accurate enough). In the ca...
Source: In the Pipeline - March 12, 2010 Category: Chemists Tags: Biological News Source Type: blogs

Lilly Layoffs Today?email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
I keep hearing from several sources that Eli Lilly is announcing cuts today (well, filling in the details on previously announced cuts, anyway). True, or just rumor? (Source: In the Pipeline)
Source: In the Pipeline - March 12, 2010 Category: Chemists Tags: Business and Markets Source Type: blogs

Garage Biotechemail this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
Freeman Dyson has written about his belief that molecular biology is becoming a field where even basement tinkerers can accomplish things. Whether we're ready for it or not, biohacking is on its way. The number of tools available (and the amount of surplus equipment that can be bought) have him imagining a "garage biotech" future, with all the potential, for good and for harm, that that entails. Well, have a look at this garage, which is said to be somewhere in Silicon Valley. I don't have any reason to believe the photos are faked; you could certainly put your hands on this kind of equipment very easily in the Bay area....
Source: In the Pipeline - March 12, 2010 Category: Chemists Tags: Biological News Source Type: blogs

Nonsense About LSDemail this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
The Daily Telegraph in the UK has a story today claiming that a 1951 outbreak of hallucinations and dementia in the French village of Pont-Saint-Esprit was not (as everyone thought) an example of ergot poisoning. No, according to some guy who's writing a book, it was. . .a secret LSD experiment. Now, there most certainly were secret LSD experiments during the 1950s and 1960s. (The book Storming Heaven has a good account of them, as well as of the history of LSD in general). But it's rather hard to see why the CIA should decide to dose some village in the Auvergne, especially when the symptoms (burning sensations in the e...
Source: In the Pipeline - March 11, 2010 Category: Chemists Tags: Chemical News Source Type: blogs

Intermune's Riseemail this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
If you want to know why people continue to speculate in biotech stocks, just take a look at the stairsteppy last few days of trading in Intermune (ITMN). Last Thursday it was at $15; now it's at $38. And all you have to do to cash in on these moves is read the FDA's mind! That's not a money-making proposition, in case anyone thinks I'm advocating it. There are just too many surprises. But Intermune's good fortune started last week, when the FDA briefing documents came out on the application on the company's pirfenidone for idiopathic pulmonary fibrosis and were characterized as "not as bad as they could have been". (The c...
Source: In the Pipeline - March 11, 2010 Category: Chemists Tags: Regulatory Affairs Source Type: blogs

Vaccines in the Courtemail this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
The Supreme Court has agreed to hear a vaccine-liability case, in an attempt to untangle conflicting lower court rulings. This all turns on the 1986 act that shields manufacturers from liability suits and a followup law that establishes a separate compensation system for injuries. A Georgia Supreme Court ruling has recently held that such suits can go on in state court, which seems to contradict other court decisions (and the intent of the 1986 law as well, you'd think). I agree with Jim Edwards of BNET that although this particular case involves the DPT vaccine, the vaccines-cause-autism crowd will be watching this one v...
Source: In the Pipeline - March 10, 2010 Category: Chemists Tags: Regulatory Affairs Source Type: blogs

How Not to Do It: Liquid Oxygen Cylindersemail this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
We haven't had a How Not to Do It around here in a while, so here's a companion piece to the famous Sealed-Up Liquid Nitrogen Tank. This incident happened (as far as I can tell) about ten years ago. It's been used in a number of safety presentations then, thanks to the Airgas Corp., whose safety officer assembled a number of photos (and this is the time to emphasize that they had nothing to do with the accident itself, because people who work for a pressurized-gas company actually know how to handle pressure vessels. As opposed to the two guys who scavenged a liquid oxygen Dewar from a scrap metal yard and decided to put ...
Source: In the Pipeline - March 10, 2010 Category: Chemists Tags: How Not to Do It Source Type: blogs

A GSK/Sirtris Wrap-Upemail this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
Nature Biotechnology weighs in on the GSK/Sirtris controversy. They have a lot of good information, and I'm not just saying that because someone there has clearly read over the comments that have showed up to my posts on the subject. The short form: The controversy over Sirtris drugs reached a tipping point in January with a publication by Pfizer researchers led by Kay Ahn showing that resveratrol activates SIRT1 only when linked to a fluorophore. Although Ahn declined to be interviewed by Nature Biotechnology, a statement issued by Pfizer says the group's findings “call into question the mechanism of action of resverat...
Source: In the Pipeline - March 9, 2010 Category: Chemists Tags: Biological News Source Type: blogs

Hope Darn Well Springs Eternalemail this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
Well, it takes all kinds to make a market. And the collapse in Medivation's shares after their disastrous Phase III results the other day seem to have brought out some hopeful buyers. Take this guy: . . .I'm telling you right now, I believe that sell-off has gone twice as deep as good sense can justify. At least, that's the way I see it. First off, we should understand that drug trials are Medivation's business. Clinical trials are what the company does. This failed phase 3 study isn't to be considered a crash into a brick wall. It's not a crippling lawsuit. It's not the loss of a major customer account. It's simply a su...
Source: In the Pipeline - March 9, 2010 Category: Chemists Tags: Business and Markets Source Type: blogs

Bad News at Exelixisemail this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
I'm hearing from more than one source that Exelixis has laid off about 40% of their work force, which is somewhere around 250 people (the numbers I get don't all agree). This seems to be across the board, all departments, and most everyone is being asked to leave today. The Bay area biotech scene doesn't seem to be at its healthiest these days (although it's still in better shape than San Diego, from the sound of it), but this isn't going to help it one bit. . . (Source: In the Pipeline)
Source: In the Pipeline - March 8, 2010 Category: Chemists Tags: Business and Markets Source Type: blogs

Not Gonna Make That Oneemail this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
A discussion at work the other day got me to thinking: what structures do you medicinal chemists out there just refuse to work on? Any? We all have our own prejudices - in fact, if you get enough chemists into one conference room, one or another of them will probably rule out just about any structure you propose. Try that sometime, and be sure to sneak a few marketed drugs in there to tick people off. Don't like organoazides? Michael acceptors? Nitroaromatics? Epoxides? Chloromethyl ketones? They're out there working in the real world and making real money. Now, I'm not saying that you should concentrate on these things. ...
Source: In the Pipeline - March 8, 2010 Category: Chemists Tags: Life in the Drug Labs Source Type: blogs

Merck/Schering-Plough People?email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
Kim Girard, a reporter from CBS Interactive is doing a story on how people are coping with the merger - if you'd like to speak with her, she's at (de-spammified): kim.berg30-at-gmail.com. I didn't have any direct knowledge to help her, so I offered to post this to see if she gets something useful. . . (Source: In the Pipeline)
Source: In the Pipeline - March 5, 2010 Category: Chemists Tags: Business and Markets Source Type: blogs

Friday Book Recommendationemail this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
Here's another outside the field - in fact, it's outside of a lot of people's fields. Where Is Everybody? presents fifty possible solutions to the Fermi Paradox: if there are a lot of planets in the galaxy, and if life is pretty easy to get going, and if it's possible to travel or just communicate between solar systems. . .why haven't we seen anything? Enrico Fermi, in his typically disconcerting way, ran the math on this question during a lunchtime conversation in 1950, and realized that at least one of the common assumptions behind it must be off, and by a great deal. I was thinking about this last night, because this w...
Source: In the Pipeline - March 5, 2010 Category: Chemists Tags: Book Recommendations Source Type: blogs

Twelve and One Half Per Centemail this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
I will note here, with no additional comment whatsoever, that Jeff Kindler, Pfizer's CEO, has just been granted a raise in his base salary of 12.5%. Details at Pharmalot. (Source: In the Pipeline)
Source: In the Pipeline - March 5, 2010 Category: Chemists Tags: Business and Markets Source Type: blogs

Your Own Personal Bacteriaemail this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
There's a report in Nature on the bacteria found in the human gut that's getting a lot of press today (especially for a paper about, well, bacteria in the human gut). A team at the Beijing Genomics Institute, with many collaborators, has done a large shotgun sequencing effort on gut flora and identified perhaps one thousand different species. I can well believe it. The book I recommended the other day on bacteria field marks has something to say about that, pointing out that if you're just counting cells, that the cells of our body are far outnumbered by the bacteria we're carrying with us. Of course, the bacteria have an...
Source: In the Pipeline - March 5, 2010 Category: Chemists Tags: Biological News Source Type: blogs

Dimebon, Grasping at Strawsemail this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
Robert Langreth, an editor at Forbes, points to a possible way that Dimebon could get approval for Alzheimer's: for its behavioral effects, not anything to do with amyloid or memory. I'm not buying it, I have to say. Even Langreth's source admits that behavioral numbers didn't reach statistical significance. I don't see how this will be enough to rescue this one, even if one of the ongoing trials does use a behavioral score as an endpoint. Update: Langreth has an earlier piece on how Dimebon appears to have been overhyped from the beginning, a viewpoint I concur with. The same thing happens with any drug for Alzheimer's...
Source: In the Pipeline - March 4, 2010 Category: Chemists Tags: Alzheimer ' s Disease Source Type: blogs

Mental Health Break: The Alkali Metals Show Their Personalitiesemail this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
Some blogs run pictures of cats to give the readers a break from the ordinary. Around here, I thought that this might be appropriate. Here are the alkali metals, from top to bottom, differentiated in the most basic way possible. No, not by tasting them, sheesh: by tossing them into a dish of water: (Courtesy of the Open University site in the UK). One thing they don't go into is the effect of density. Up to potassium, the metals are still light enough to float. But cesium drops like the rock it is, with depth-charge results. I will consider running a photo of a cat, as long as he's working up a reaction. (Source: In the Pipeline)
Source: In the Pipeline - March 4, 2010 Category: Chemists Tags: How Not to Do It Source Type: blogs

Flowing, Not So Gentlyemail this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
I've written both here and elsewhere about flow chemistry, the technique where you pump your reactions through a reaction tube of some sort rather than mixing them up in a flask. And I freely admit that I have a fondness for the idea, but it's definitely not the answer to every problem. For one thing, I tend to like the idea of sending reactants over a bed of catalyst or solid-supported reagent (what I call Type II or Type III flow reactions in that 2008 link above). Type I reactions, in my scheme, are the ones where you just use a plain tube or channel, and all the reactants are present in solution. A big advantage of th...
Source: In the Pipeline - March 4, 2010 Category: Chemists Tags: Chemical News Source Type: blogs

Dimebon Comes Crashing to Earthemail this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
Earlier this month I wrote about Medivation and their Russian-derived clinical candidate for Alzheimer's disease, Dimebon (latrepirdine). At the time, I wrote that "A lot of eye-catching numbers from small Phase II trials tend to flatten out in the wider world of Phase III, and if forced, that's the way I'd bet here." Unfortunately, that's just what appears to have happened. The results are out today, and Dimebon has not showed any efficacy at all versus placebo. From the data given in the press release, the comparison is just absolutely flat; you could have been giving the study patients breath mints and seen the same nu...
Source: In the Pipeline - March 3, 2010 Category: Chemists Tags: Alzheimer ' s Disease Source Type: blogs

Fat Rats Make Poor Test Subjects?email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
Well, here's a brow-furrowing paper, courtesy of PNAS. Th authors, from the National Institute on Aging, contend that most laboratory rodents are overfed, under-stimulated, and are (to use their phrase) "metabolically morbid". This affects their suitability as control and experimental animals for a wide variety of assays. There seem to be effects across the board - the immune system, glucose and lipid handling, cardiovascular numbers, susceptibility to tumors, cognitive performance. The list is a long one, and the route causes seem to be ad libitum feeding and lack of exercise. The beneficial effects of some drugs in rode...
Source: In the Pipeline - March 3, 2010 Category: Chemists Tags: Animal Testing Source Type: blogs

AstraZeneca Makes Its Moveemail this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
OK, I think the company has made an official announcement on this. They're getting out of schizophrenia, bipolar disease, depression, anxiety, acid reflux, thrombosis, ovarian and bladder cancers, systemic scleroderma and hepatitis C. (So much for some of the company's current and recent big-selling areas. . .) As for facilities, they're shutting down early R&D in Wilmington and in Lund (Sweden), and the Charnwood site in the UK is closing. I haven't heard if there are other cuts going on in the sites (or therapeutic areas) that are remaining, though. Details in the comments. . . (Source: In the Pipeline)
Source: In the Pipeline - March 2, 2010 Category: Chemists Tags: Business and Markets Source Type: blogs

Why You Don't Want to Make Death-Star-Sized Drugsemail this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
I was just talking about greasy compounds the other day, and reasons to avoid them. Right on cue, there's a review article in Expert Opinion in Drug Discovery on lipophilicity. It has some nice data in it, and I wanted to share a bit of it here. It's worth noting that you can make your compounds too polar, as well as too greasy. Check these out - the med-chem readers will find them interesting, and who knows, others might, too: So, what are these graphs? They show how well compound cross the membranes of Caco-2 cells, a standard assay for permeability. These cells (derived from human colon tissue) have various active-tra...
Source: In the Pipeline - March 2, 2010 Category: Chemists Tags: Pharma 101 Source Type: blogs

The Plasmid Committee Will See You Nowemail this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
From Nature comes word of a brainlessly restrictive new law that's about to pass in Turkey. The country started out trying to get in line with EU regulations on genetically-modified crops, and ended up with a bill that forbids anyone to modify the DNA of any organism at all - well, unless you submit the proper paperwork, that is: . . .Every individual procedure would have to be approved by an inter-ministerial committee headed by the agriculture ministry, which is allowed 90 days to consider each application with the help of experts. The committee would be responsible for approving applications to import tonnes of GM soy...
Source: In the Pipeline - March 2, 2010 Category: Chemists Tags: Biological News Source Type: blogs

Blog Traffic - Thanks!email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
Just a quick note to say that traffic here broke all the house records last month - over 440,000 page views (partly thanks to a late surge in interest in the wonderful properties of dioxygen difluoride). The number of people interested in this sort of thing continues to exceed my estimates. . .! (Source: In the Pipeline)
Source: In the Pipeline - March 1, 2010 Category: Chemists Tags: Blog Housekeeping Source Type: blogs

Calorimetry: What Say You?email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
I've been involved in a mailing list discussion that I wanted to open up to a wider audience in drug discovery, so here goes. We spend our time (well, a lot of it, when we're not filling out forms) trying to get compound to bind well to our targets. And that binding is, of course, all about energy: the lower the overall energy of the system when your compound binds, relative to the starting state, the tighter the binding. That energy change can be broken down (all can all chemical free energy changes) into an enthalpic part and an entropic part (that latter one depends on temperature, but we'll assume that everything's be...
Source: In the Pipeline - March 1, 2010 Category: Chemists Tags: Drug Assays Source Type: blogs

Layoffs Coming at Eli Lilly?email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
I hate to start the week out like this, but I have a report that Lilly is looking to cut quite a few chemistry positions (and maybe others), with word to come on Friday, March 12. Anyone else have anything on this? Update: to clarify, these appear to be the layoffs that were announced last fall, not a new series. It's just that we finally seem to be finding out who stays and who doesn't. . . (Source: In the Pipeline)
Source: In the Pipeline - March 1, 2010 Category: Chemists Tags: Business and Markets Source Type: blogs

A Friday Book Recommendationemail this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
This isn't exactly med-chem, but its focus probably overlaps with the interests of a number of readers around here. I recently came across a copy of A Field Guide to Bacteria and enjoyed it very much. I don't think there's another book quite like it available: it describes where you're likely to find different varieties of bacteria (from hot springs to your fridge), how they behave in a natural environment (as opposed to a culture dish) and how to identify them by field marks, if possible. It's not written for microbiologists, but it can provide a different perspective even if you work in the field (since many people that ...
Source: In the Pipeline - February 26, 2010 Category: Chemists Tags: Infectious Diseases Source Type: blogs

HER2 Confusionemail this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
For years now, drug companies and journalists have been touted the new era of personalized medicine. This is one of those things that always seems to be arriving, but is taking its time getting here. The industry has sunk a huge pile of money into biomarker research, and it's safe to say that it hasn't paid off yet - although, at the same time, one still has to think that it should, eventually. Nature Biotechnology has a good article that shows how tricky the whole business can be. HER2 is one of the more validated cancer biomarkers, and there's a drug (Herceptin) that's targeted specifically for breast cancer patients th...
Source: In the Pipeline - February 26, 2010 Category: Chemists Tags: Cancer Source Type: blogs

Layoff Newsemail this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
More job loss news to report, unfortunately. Pharmalot comes in with an item that fits with what I'm hearing, that Sanofi-Aventis appears to be making small cuts, over and over, at its various sites. There hasn't been a single big announcement that I've heard, but the company seems to be shrinking headcount nonetheless. And I've also heard recently that Astra-Zeneca is ready to announce more layoffs, although I don't have a handle on the size. This appears to be some of the follow-through from their earlier nonspecific announcements - it looks as if they're finally going to start getting down to some details. Anyone with ...
Source: In the Pipeline - February 26, 2010 Category: Chemists Tags: Business and Markets Source Type: blogs

Cranking Awayemail this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
Not as much time to blog this morning (and it's been hard getting into the site, since there are a lot of people who apparently want to know how to order some dioxygen difluoride). For one thing, I'm clearing a bunch of reactions out, and I've been devoting thought to how to do that in the laziest possible manner. Maybe I should clarify that. What I mean is, how do I work up all these reactions quickly, in such a way as to make clean compounds that are worth testing, but spend the least amount of effort doing so? There are, of course, all sorts of brute-force ways to bang these things through, some of which would involve ...
Source: In the Pipeline - February 25, 2010 Category: Chemists Tags: Life in the Drug Labs Source Type: blogs

Knocking on Doorsemail this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
A correspondent writes in with an interesting and useful question: he's with a small company that believes that it's discovered a useful lead compound in an area where they're hard to find. But no one there has any experience with knocking on the doors of Big Pharma to talk about a deal, and they're wondering about the best way to go about it. I (and people like me) can provide some general advice. But I know that there are consultants out there who've brokered things like this before and have both contacts and expertise that can help out. But that just kicks the problem along: how does a fledgling company find one of tho...
Source: In the Pipeline - February 24, 2010 Category: Chemists Tags: Business and Markets Source Type: blogs

Steve Nissen's Meeting with GSKemail this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
Well, this is interesting. Back when Steve Nissen was about to publish his meta-analysis on the safety of Avandia (rosigiltazone), he met with several GlaxoSmithKline executives before the paper came out. At the time, GSK was waiting on data from the RECORD study, which was trying to address the same problem (unconvincingly, for most observers, in the end). Nissen had not, of course, shown his manuscript to anyone at GSK, and for their part, the execs had not seen the RECORD data, since it hadn't been worked up yet. Well, not quite, perhaps on both counts. As it happens, a reviewer had (most inappropriately) faxed a copy ...
Source: In the Pipeline - February 24, 2010 Category: Chemists Tags: Diabetes and Obesity Source Type: blogs

Write A Book, Why Don't Youemail this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
Yesterday's "Things I Won't Work With" post has brought on calls to turn these (and some other parts of the blog) into a book. And you know, I'm game, actually - but I have no real contacts in the publishing world. If anyone out there in the readership knows a good agent, or knows someone who does, I'd be glad to have some contact information. Thanks! (Source: In the Pipeline)
Source: In the Pipeline - February 24, 2010 Category: Chemists Tags: Blog Housekeeping Source Type: blogs

Things I Won't Work With: Dioxygen Difluorideemail this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
The latest addition to the long list of chemicals that I never hope to encounter takes us back to the wonderful world of fluorine chemistry. I'm always struck by how much work has taken place in that field, how long ago some of it was first done, and how many violently hideous compounds have been carefully studied. Here's how the experimental prep of today's fragrant breath of spring starts: The heater was warmed to approximately 700C. The heater block glowed a dull red color, observable with room lights turned off. The ballast tank was filled to 300 torr with oxygen, and fluorine was added until the total pressure was 90...
Source: In the Pipeline - February 23, 2010 Category: Chemists Tags: Things I Won ' t Work With Source Type: blogs

Avandia: Off the Market or Not?email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
The Senate report that leaked on Avandia (rosiglitazone) over the weekend has made plenty of headlines. It quotes an internal FDA report that recommends flatly that the drug be removed from the market, since its beneficial effects can be achieved by use of the competing PPAR drug Actos (pioglitazone), which doesn't seem to have the same cardiovascular risks. The two drugs have been compared (retrospectively) head to head, and Avandia definitely seems to have come out as inferior due to safety concerns. There had been worries for several years about side effects, but the red flag went up for good in 2007, and the arguing h...
Source: In the Pipeline - February 22, 2010 Category: Chemists Tags: Diabetes and Obesity Source Type: blogs

The Front Lines of Cancer Treatmentemail this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
The New York Times is starting a series of articles on the clinical trials of a recent B-Raf inhibitor (from Plexxikon and Roche, PLX4032). The first installment is an excellent look at what early-stage clinical research is like in this field. For example: Typically, Phase 1 trials are limited to a few dozen patients and end when the dose reaches the point where side effects like rashes and diarrhea make patients too uncomfortable. Dr. Flaherty and Dr. Chapman started the first three patients on 200 milligrams per day. After two months with no side effects — and no response — they doubled it. Two more months passed...
Source: In the Pipeline - February 22, 2010 Category: Chemists Tags: Cancer Source Type: blogs

Two For One Saleemail this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
A double complaint this morning, and both from the same literature item - if I were charging anything for the blog, I'd say that it's delivering value for the money. At any rate, the first kvetch is something that I know that many chemists have noticed when reading more biology/medical-oriented journals. You'll see some paper that talks about a new compound that does X, Y, and Z. It'll be named with some sort of code, and they'll tell you all about its interesting effects. . .but they don't get around to actually telling you what the damned stuff is. As I say, this is a chemist's complaint. Many biologists are fine stipul...
Source: In the Pipeline - February 19, 2010 Category: Chemists Tags: The Scientific Literature Source Type: blogs

Biology By the Numbersemail this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
I've been meaning to write about this paper in PNAS for a while. The authors (from Cal Tech and the Weizmann Institute) have set up a new web site, are calling for a more quantitative take on biological questions. They say that modern techniques are starting to give up meaningful inputs, and that we're getting to the point where this perspective can be useful. A web site, Bionumbers, has been set up to provide ready access to data of this sort, and it's well worth some time just for sheer curiosity's sake. But there's more than that at work here. To pick an example from the paper, let's say that you take a single E. coli ...
Source: In the Pipeline - February 18, 2010 Category: Chemists Tags: Biological News Source Type: blogs