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Promotion of Drug Discovery Research by Utilizing Omics Technology.
PMID: 26831783 [PubMed - in process] (Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan)
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 3, 2016 Category: Drugs & Pharmacology Authors: Nagano K, Higashisaka K Tags: Yakugaku Zasshi Source Type: research

Challenge to the Development of Molecular Targeted Therapy against a Novel Target Candidate Identified by Antibody Proteomics Technology.
Abstract   Disease proteomics that systemically analyzes and identifies differentially expressed proteins between healthy and diseased samples is a potentially useful approach for obtaining target proteins for drug development. To date, however, very few target proteins have been identified from this field. A key issue that remains to be resolved is how to correctly identify target proteins from a number of potential candidates. To circumvent this problem, we have developed "antibody proteomics technology" in which a single chain Fv phage antibody library is utilized for proteome analysis. Here, we describe the a...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 3, 2016 Category: Drugs & Pharmacology Authors: Nagano K Tags: Yakugaku Zasshi Source Type: research

Functional Analysis of GATA4 Complex, a Cardiac Hypertrophy-response Transcriptional Factor, Using a Proteomics Approach.
Abstract   Various stresses on the heart, such as myocardial infarction and hemodynamic overload, activate the sympathetic nervous system and the renin-angiotensin system, ultimately reach the nuclei of cardiomyocytes, and change the pattern of gene expression associated with cardiac hypertrophy. Although present pharmacological therapy for heart failure targets such extracellular molecules, mortality due to heart failure is still high. A zinc finger protein, GATA4, is one of the hypertrophy-responsive transcription factors, forms a functional protein complex with an intrinsic histone acetyltransferase, p300, and...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 3, 2016 Category: Drugs & Pharmacology Authors: Sunagawa Y, Katanasaka Y, Wada H, Hasegawa K, Morimoto T Tags: Yakugaku Zasshi Source Type: research

Screening for Potential Drug Targets by Comprehensive Identification of Disease-specific Antigens Incorporated into Immune Complexes in Patients with Immunological Diseases.
Abstract   Our immune system resembles an intelligent security system, which continually monitors for foreign invaders (infectious diseases); however, in some cases, this system recognizes healthy parts as something harmful or foreign and then attacks them (autoimmune diseases). The defining characteristics of an autoimmune disease are the existence of T- and B-cell autoreactivity against self proteins (autoantigens). In addition to autoimmune diseases, aberrant host proteins that occur during a certain state of diseases (e.g., cancer) can be recognized as an autoantigen. Immune complexes (ICs) are produced durin...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 3, 2016 Category: Drugs & Pharmacology Authors: Ohyama K Tags: Yakugaku Zasshi Source Type: research

Application of Imaging Mass Spectrometry for Drug Discovery.
Abstract   Imaging mass spectrometry (IMS) can reveal the distribution of biomolecules on tissue sections. In this process, the biomolecules are directly ionized within tissue sections using matrix-assisted laser desorption/ionization, and then their distribution is visualized by pseudo-color based on the relative signal intensity. The biomolecules, such as fatty acids, phospholipids, glycolipids, peptides, proteins, and neurotransmitters, have been analyzed at a spatial resolution of 5 μm. A special instrument for IMS analysis was developed by Shimadzu. The IMS analysis does not require the labeling of biomolec...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 3, 2016 Category: Drugs & Pharmacology Authors: Hayasaka T Tags: Yakugaku Zasshi Source Type: research

Structural Pharmacology for Receptors and Transporters.
PMID: 26831788 [PubMed - in process] (Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan)
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 3, 2016 Category: Drugs & Pharmacology Authors: Shimizu T, Kato H Tags: Yakugaku Zasshi Source Type: research

Structural Analyses of Toll-like Receptor Sensing Single-stranded Nucleic Acids and Its Application.
We describe the crystal structure of a newly developed agonist, C2-butyl furo[2,3-c]quinolone. PMID: 26831789 [PubMed - in process] (Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan)
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 3, 2016 Category: Drugs & Pharmacology Authors: Shimizu T Tags: Yakugaku Zasshi Source Type: research

Structural Life Science towards the Regulation of Selective GPCR Signaling.
Abstract   G protein-coupled receptors (GPCRs) are the largest family of receptors in the human genome. They are involved in many diseases and also the target of approximately 30% of all modern medicinal drugs. GPCRs respond to a broad spectrum of chemical entities, ranging from photons, protons, and calcium ions to small organic molecules (including odorants and neurotransmitters), peptides, and glycoproteins. Many GPCRs are members of closely related subfamilies that respond to the same hormone or neurotransmitter. However, they have different physiologic functions based on the cells in which they are expressed...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 3, 2016 Category: Drugs & Pharmacology Authors: Kobayashi T Tags: Yakugaku Zasshi Source Type: research

Structural and Functional Studies on Photoactive Retinal Proteins: Light Becomes Drugs with Proteins.
Abstract   Retinal proteins possess vitamin A aldehyde (retinal) as a chromophore within seven transmembrane α-helices. Visible light absorption of them triggers trans-cis photoisomerization of the retinal chromophore and induces structural changes in the protein moiety, resulting in a variety of biological functions such as vision, ion transportation, and photosensing. Environmental genomics revealed that retinal proteins are widely distributed through all three biological kingdoms, eukarya, bacteria, and archaea, indicating the biological significance of their light energy conversion. In addition to their biol...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 3, 2016 Category: Drugs & Pharmacology Authors: Sudo Y Tags: Yakugaku Zasshi Source Type: research

In Vitro Selected Macrocyclic Peptides: Tools for Regulating the Conformational Freedom of Transmembrane Proteins.
Abstract   Membrane proteins allow a cell to communicate with its environment by relaying a signal or transporting a molecule through the cell membrane. Elucidation of the three-dimensional structure of a membrane protein provides a greater understanding of its function and mechanisms. Ultimately, this knowledge will enlighten researchers on how these proteins can be regulated to elicit a desired cellular response, which could lead to novel therapeutic medicine. Unfortunately, the determination of the high-resolution crystal structures of transmembrane proteins remains a challenge due to their poor solubility and...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 3, 2016 Category: Drugs & Pharmacology Authors: Hipolito CJ, Nishio K, Suga H Tags: Yakugaku Zasshi Source Type: research

Structural and Pharmacological Studies of an ABC Multidrug Transporter.
Abstract   A drug's effectiveness against a disease depends not only on its interaction with receptors but also its pharmacokinetics (absorption, distribution, metabolism, and extrusion; ADME). ATP binding cassette (ABC) multidrug transporters are important proteins that influence the ADME properties of a drug, especially the ABC transporter subfamily B member 1 (ABCB1). Elucidation of the molecular mechanisms of ABCB1 will contribute to our understanding of the molecular basis of ADME. Human ABCB1 is expressed in many organelles, and exports various substrates from cells using energy generated by its ATP hydrola...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 3, 2016 Category: Drugs & Pharmacology Authors: Yamaguchi T Tags: Yakugaku Zasshi Source Type: research

The Challenge of Developing New Treatments for NTDs Originating from Japan.
PMID: 26831794 [PubMed - in process] (Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan)
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 3, 2016 Category: Drugs & Pharmacology Authors: Kita K, Yamada H Tags: Yakugaku Zasshi Source Type: research

Current Trend of Drug Development for Neglected Tropical Diseases (NTDs).
Abstract   EBOLA hemorrhagic fever, a typical emerging infectious disease, began in December 2013 in the southern part of Guinea, and killed more than 11000 people by the end of June, 2015. In addition to emerging/re-emerging diseases and the 3 major infectious diseases i.e. HIV/AIDS, tuberculosis and malaria, neglected tropical diseases (NTDs) have recently become important tropical diseases of the poor. It is remarkable that Japan succeeded in the eradication of malaria and other tropical diseases, which include lymphatic filariasis and schistosomiasis. However, despite these achievements, it is important to su...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 3, 2016 Category: Drugs & Pharmacology Authors: Kita K Tags: Yakugaku Zasshi Source Type: research

International Partnership for Therapeutic Drug Development of NTDs by DNDi.
Abstract   The Drugs for Neglected Diseases initiative (DNDi), with headquarters in Geneva, is a non-profit drug research and development (R&D) organization and Product Development Partnership (PDP) which was established in 2003 by 7 founding organizations such as Médecins Sans Frontières (MSF), the Pasteur Institute, The Specific Programme for Research and Training in Tropical Diseases (WHO-TDR), etc. DNDi has worked mainly on the development of new treatments for neglected tropical diseases (NTDs), which is difficult to achieve under market economy conditions. DNDi has promoted overall drug discovery rese...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 3, 2016 Category: Drugs & Pharmacology Authors: Yamada H, Hirabayashi F, Brünger C Tags: Yakugaku Zasshi Source Type: research

Development and Distribution of Drugs for NTDs: Efforts of One Pharmaceutical Company.
Abstract   The Pharmaceutical Industry is expected to play a proactive global role in combatting neglected tropical diseases (NTDs) and other tropical diseases affecting low-income countries. Such a role would include novel medicine R&D, manufacturing and distribution. In order to succeed in this role, several challenges need to be overcome: a) the economic challenge or cost benefit balance for the development of these medicines, and b) sparse in-house experience with these diseases within the Industry. During the last decade, the Product Development Partnership (PDP) model has become an effective strategy to...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 3, 2016 Category: Drugs & Pharmacology Authors: Asada M Tags: Yakugaku Zasshi Source Type: research

Activity of NTDs Drug-discovery Research Consortium.
Abstract   Neglected tropical diseases (NTDs) are an extremely important issue facing global health care. To improve "access to health" where people are unable to access adequate medical care due to poverty and weak healthcare systems, we have established two consortiums: the NTD drug discovery research consortium, and the pediatric praziquantel consortium. The NTD drug discovery research consortium, which involves six institutions from industry, government, and academia, as well as an international non-profit organization, is committed to developing anti-protozoan active compounds for three NTDs (Leishmaniasis, ...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 3, 2016 Category: Drugs & Pharmacology Authors: Namatame I Tags: Yakugaku Zasshi Source Type: research

Industry, Academia and Government Partnership through the Global Health Innovative Technology Fund (GHIT).
Abstract   In developing countries, many people are unable to access basic healthcare services, resulting in many avoidable deaths and/or disabilities. The United Nations adopted the Millennium Development Goals in order to resolve this problem, and Japan has been contributing greatly to the achievement of these goals. In this context, in 2013 the Government of Japan proposed its Strategy on Global Health Diplomacy, and since then has been promoting Universal Health Coverage. Since the beginning of the 21st century, the particular importance of addressing neglected tropical diseases (NTDs) has been stressed by th...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 3, 2016 Category: Drugs & Pharmacology Authors: Hinoshita E Tags: Yakugaku Zasshi Source Type: research

Establishment for the Supporting of Pharmacies as the Healthcare Information Hub in the Community.
PMID: 26831800 [PubMed - in process] (Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan)
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 3, 2016 Category: Drugs & Pharmacology Authors: Saito M, Yamamoto M Tags: Yakugaku Zasshi Source Type: research

Current Status of Community Pharmacies: Expectations as a Health Information Hub, the Enforcement of Revised Pharmaceutical and Medical Device Act, and a New Role as Stakeholders.
Abstract   According to the "Japan Revitalization Strategy" established in June 2013, "the government will promote better contributions of local pharmacies and pharmacists in encouraging self-medication of citizens by making pharmacies the community-based hub for providing information, giving advice on the proper use of non-prescription drugs, etc. and offering consultation and information service concerning health". In addition, the "Demanded Function and Ideal Form of Pharmacy," published in January 2014, requested a change, from pharmacies that specialized in dispensing medicines to pharmacies that serve as wh...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 3, 2016 Category: Drugs & Pharmacology Authors: Saito M Tags: Yakugaku Zasshi Source Type: research

Japanese Model of Asheville Project. Its Overview and Initiative.
Abstract   The Asheville Project(®) began in 1996 in Asheville, North Carolina, where community pharmacists, in collaboration with physicians, provide health coaching to patients with lifestyle diseases to accomplish their improved self-management of the disease. The project has now widely expanded across the United States. With periodical coaching by pharmacists, according to the reports of these programs, patients have been reported to show improvements in self-management and laboratory data, including the number of doctor visits, medication adherence and the number of foot examinations. Economically, the tota...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 3, 2016 Category: Drugs & Pharmacology Authors: Furukawa A, Asada Y, Mori T, Inoue G, Atsuda K Tags: Yakugaku Zasshi Source Type: research

Pilot Study of "Japanese Model of Asheville Project"~How Did It Work?
This study evaluated the two primary measurements, which are A) the actual execution rate versus planned programs, and B) the patient satisfaction rate. In addition, the achievement rate of behavioral objectives, satisfaction rate of diabetes treatment, degree of concerns (Diabetes Treatment Satisfaction Questionnaire; DTSQ, Problem Areas in Diabetes; PAID) and other physiological indicators have been evaluated. With the approval of the IRB at Kitasato University, sixteen out of 18 patients have continued to participate in the support program, and the study has shown high patient satisfaction with pharmacist coaching suppo...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 3, 2016 Category: Drugs & Pharmacology Authors: Fujii H, Mori T, Furukawa A, Inoue G, Atsuda K Tags: Yakugaku Zasshi Source Type: research

Estimation of the Health Status of People in the Vicinity of Pharmacies Using Pharmacy Big Data.
Abstract   The purpose of this study was to propose a method for visualizing the patterns of the geographical propagation of influenza infection, and to elaborate parameters for the characterization of these patterns. First, a motion picture was prepared for the quotidian propagation of influenza infection in the Greater Tokyo Metropolitan area, which is considered a typical epidemic area for the 2012/2013 flu season. Second, hebdomadal recordings of patients with influenza infection in the 47 prefectures of Japan were grouped into 3 categories (1-peak, 2-peak, or multi-peak). The prefectures were arranged accord...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 3, 2016 Category: Drugs & Pharmacology Authors: Hayashi Y, Saito M, Yajima T Tags: Yakugaku Zasshi Source Type: research

Development of an Informative System for Consumers and Pharmacists Aimed at the Proper Use of Kampo OTCs.
Abstract   Kampo medicines must be used according to an individual's physical characteristics and symptoms to avoid lack of efficacy, adverse reactions or interactions with other drugs. As category-2 over-the-counter drugs (OTCs), Kampo OTCs are not targets of active explanations by pharmacists, and consumers usually decide to use OTCs by themselves on the basis of drug label information. However, information on the label is occasionally brief. To promote the proper use of Kampo OTCs, we herein propose an informative tool based on the Australian Shelf-Talker (information on the proper use of OTCs with a self-chec...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 3, 2016 Category: Drugs & Pharmacology Authors: Takano-Ohmuro H, Nakajima Y, Saito M, Yuda Y Tags: Yakugaku Zasshi Source Type: research

For the Establishment of an Informative Support Framework in Pharmacies: Informative Support System for Diabetes.
Abstract   According to the Japanese revitalization strategy endorsed by the government in June, 2013, pharmacies are expected to play an active role as the hub of health information. But this is not sufficiently organized: an infrastructure for providing neutral information which becomes the basis of such health information is not yet established for healthcare professionals, patients and consumers. As for drug information available subsequent to the marketing of pharmaceutical products, information from the pharmaceutical companies including Package Inserts and Interview-forms are often found. However, though s...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 3, 2016 Category: Drugs & Pharmacology Authors: Yamamoto M, Doi H, Watanabe K Tags: Yakugaku Zasshi Source Type: research

Role of Transient Receptor Potential Channels in Paclitaxel- and Oxaliplatin-induced Peripheral Neuropathy.
Abstract   Peripheral neuropathy is a common adverse effect of paclitaxel and oxaliplatin treatment. The major dose-limiting side effect of these drugs is peripheral sensory neuropathy. The symptoms of paclitaxel-induced neuropathy are mostly sensory and peripheral in nature, consisting of mechanical allodynia/hyperalgesia, tingling, and numbness. Oxaliplatin-induced neurotoxicity manifests as rapid-onset neuropathic symptoms that are exacerbated by cold exposure and as chronic neuropathy that develops after several treatment cycles. Although many basic and clinical researchers have studied anticancer drug-induce...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 3, 2016 Category: Drugs & Pharmacology Authors: Taguchi K Tags: Yakugaku Zasshi Source Type: research

Structure and Function of the Nuclear Receptor Constitutive Androstane Receptor.
Abstract   Animal defense mechanisms against both endogenous and exogenous toxic compounds function mainly through receptor-type transcription factors, including the constitutive androstane receptor (CAR). Following xenobiotic stimulation, CAR translocates into the nucleus and transactivates its target genes including oxygenic and conjugative enzymes and transporters in hepatocytes. We identified subcellular localization signals in the rat CAR: two nuclear localization signals (NLS1 and 2); two nuclear export signals (NES1 and 2); and a cytoplasmic retention region. The nuclear import of CAR is regulated by the i...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 3, 2016 Category: Drugs & Pharmacology Authors: Inouye Y Tags: Yakugaku Zasshi Source Type: research

Diversity of Plants Belonging to the Genus Ligularia (Asteraceae) Based on Terpenoids and Synthetic Studies on Some Terpenoids.
Abstract   The terpenoid constituents of Ligularia virgaurea (30 samples), Ligularia pleurocaulis (8 samples), Ligularia dictyoneura (8 samples), Ligularia brassicoides (5 samples), Ligularia lingiana (1 sample), and Ligularia liatroides (1 sample)(all belonging to section Senecillis of Ligularia, Asteraceae and collected in Yunnan, Sichuan, Qinghai, and Gansu provinces, China), from which 220 compounds were isolated, including 113 novel ones, are reviewed. Five chemotypes were identified in L. virgaurea based on their chemical constituents, while three clades were detected from the base sequences. Although intra...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 3, 2016 Category: Drugs & Pharmacology Authors: Tori M Tags: Yakugaku Zasshi Source Type: research

Study of Supplementary Analgesics Capable of Reducing the Dosage of Morphine.
This article reviews the potential mechanism of spinally mediated nociceptive behaviors evoked by i.t. M3G in mice. We discuss the possible presynaptic release of nociceptive neurotransmitters/neuromodulators such as substance P, glutamate, dynorphin, and Leu-enkephalin in the primary afferent fibers following i.t. M3G administration. It is possible to speculate that i.t. M3G could indirectly activate NK1, NMDA, and δ2-opioid receptors that lead to the release of nitric oxide (NO) in the dorsal spinal cord. The major function of NO is the production of cGMP and the activation of protein kinase G (PKG). The NO-cGMP-PKG pat...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 3, 2016 Category: Drugs & Pharmacology Authors: Komatsu T Tags: Yakugaku Zasshi Source Type: research

Implementation and Evaluation of Genetic Testing Seminars on Lifestyle-related Disease Prevention for Pharmacy Students.
Abstract   The field of pharmacotherapy has advanced to use molecular targeted agents, and pharmacists are now encouraged to focus on pharmacogenomics. A seminar titled "Implementation and evaluation of genetic testing of lifestyle-related disease genes" was presented to students at the Faculty of Pharmaceutical Sciences, Hiroshima University, describing the pharmacogenomic role of single nucleotide polymorphisms in obesity-related genes and alcohol metabolism-related genes. The seminar topic was selected first because pharmaceutical students were already familiar with some of the content, and secondly because we...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 3, 2016 Category: Drugs & Pharmacology Authors: Ikeda K, Hosoi T, Yoshii M, Sugiyama M, Ozawa K Tags: Yakugaku Zasshi Source Type: research

Pharmacists' Behavior in Clinical Practice: Results from a Questionnaire Survey of Pharmacy Students.
Abstract   A questionnaire survey was performed to obtain pharmacy students' impressions of pharmacists' behavior, to classify these based on professionalism, and to analyze the relationship between these experiences and students' satisfaction with their clinical practice in Japan. The questionnaire was answered by 327 5th-year pharmacy school students upon completing clinical practice at community pharmacies from 2011 to 2012. They rated their satisfaction with their clinical practice using a 6-point Likert scale, and provided descriptions of their experience such as, "This health provider is professional", or "...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 3, 2016 Category: Drugs & Pharmacology Authors: Nakada A, Akagawa K, Yamamoto H, Kato Y, Yamamoto T Tags: Yakugaku Zasshi Source Type: research

Chamical Biology for Pharmaceutical Sciences—Novel Approaches for Exploring Cellular Functions with Non-drug Chemicals.
Chamical Biology for Pharmaceutical Sciences—Novel Approaches for Exploring Cellular Functions with Non-drug Chemicals. Yakugaku Zasshi. 2016;136(1):1 Authors: Ojida A, Nakagawa H PMID: 26725659 [PubMed - in process] (Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan)
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - January 13, 2016 Category: Drugs & Pharmacology Authors: Ojida A, Nakagawa H Tags: Yakugaku Zasshi Source Type: research

Development of Fluorescence Sensing Mechanism for Cell Functional Analysis.
Abstract   Fluorescence probes are now widely used as indispensable tools in many cell functional analyses. At present, the design of fluorescent probes largely depends on the limited numbers of established sensing mechanisms such as photo-induced electron transfer (PET), photo-induced charge transfer (PCT), and fluorescence resonance energy transfer (FRET). Although these mechanisms are versatile in metal ion sensing, introduction of a new sensing mechanism is highly desirable not only to design a more sophisticated probe with high selectivity and sensitivity but also to expand the diversity of t...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - January 13, 2016 Category: Drugs & Pharmacology Authors: Ojida A, Takashima I Tags: Yakugaku Zasshi Source Type: research

Small-molecule Ligands That Manipulate the Intracellular Location of Proteins.
Abstract   Synthetic small-molecule ligands that control the intracellular location of proteins would be powerful tools for regulating cellular systems. However, the creation of such molecules has long remained unexplored because of the lack of a design methodology. Here, we introduce a new type of synthetic ligands, self-localizing ligands (SLLs), which spontaneously localize to specific subcellular regions in mammalian cells. We show that SLLs bind their target (exogenously expressed and endogenous) proteins and relocate them rapidly from the cytoplasm to their targeting sites. SLL-induced prote...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - January 13, 2016 Category: Drugs & Pharmacology Authors: Tsukiji S Tags: Yakugaku Zasshi Source Type: research

The Development of Luminescent Nano-probes on Hard X-ray Irradiation.
Abstract   X-rays are widely used in imaging applications such as diffraction imaging of crystals and medical imaging. In particular, X-ray computed tomography (CT) is a critical tool for clinical and disease diagnostics. The principle of conventional CT is based on X-ray attenuation caused by photoelectric absorption and scattering. In addition to conventional CT, a number of novel methodologies are presently under development, including state-of-the-art instrument technologies and chemical probes to fulfill diagnosis criteria. Among these novel methodologies, we have utilized hard X-ray-excited ...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - January 13, 2016 Category: Drugs & Pharmacology Authors: Osakada Y Tags: Yakugaku Zasshi Source Type: research

Visualization and Functional Regulation of Live Cell Proteins Based on Labeling Probe Design.
Abstract   There are several approaches to understanding the physiological roles of biomolecules: (1) by observing the localization or activities of biomolecules (based on microscopic imaging experiments with fluorescent proteins or fluorescent probes) and (2) by investigating the cellular response via activation or suppression of functions of the target molecule (by using inhibitors, antagonists, siRNAs, etc.). In this context, protein-labeling technology serves as a powerful tool that can be used in various experiments, such as for fluorescence imaging of target proteins. Recently, we developed ...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - January 13, 2016 Category: Drugs & Pharmacology Authors: Mizukami S, Kikuchi K Tags: Yakugaku Zasshi Source Type: research

Caged Gaseous Mediators and Their Control of Cellular Functions.
Abstract   Nitric oxide (NO) is historically well known as a toxic gas but now recognized as a physiological cellular mediator acting at very low concentrations. It is biosynthesized within the body, and modulates many signal transduction processes. For investigation of the functions of this gaseous mediator, it is necessary to use chemical donors that release NO specifically, and it is highly advantageous if the release can be made with precise spatiotemporal control. For this purpose, we have developed caged NO (photocontrollable NO-releasing compounds) with unique releasing mechanisms. One empl...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - January 13, 2016 Category: Drugs & Pharmacology Authors: Nakagawa H Tags: Yakugaku Zasshi Source Type: research

Frontier Pharmaceutics to Be Explored by Young Scientists: DDS Research for Innovative Drug Development.
PMID: 26725665 [PubMed - in process] (Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan)
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - January 13, 2016 Category: Drugs & Pharmacology Authors: Asai T, Tachikawa M Tags: Yakugaku Zasshi Source Type: research

Human Serum Albumin as Carrier in Drug Delivery Systems.
Abstract   Recently, human serum albumin (HSA) has emerged as a versatile carrier for therapeutic agents against diabetes, cancer, and infectious diseases. Market-approved products include fatty acid derivatives of human insulin for diabetes and the paclitaxel-HSA nanoparticle for various cancers such as metastatic breast cancer and advanced pancreatic cancer. In this review, we focus on the next-generation approach including HSA-binding bioactive gas such as nitric oxide (NO) for treating ischemic/reperfusion injury, cancer, and bacterial infection. To date, pharmacologically active compounds tha...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - January 13, 2016 Category: Drugs & Pharmacology Authors: Ishima Y, Maruyama T Tags: Yakugaku Zasshi Source Type: research

Analysis and Control of in Vivo Kinetics of Exosomes for the Development of Exosome-based DDS.
Analysis and Control of <i>in Vivo</i> Kinetics of Exosomes for the Development of Exosome-based DDS. Yakugaku Zasshi. 2016;136(1):49-53 Authors: Takahashi Y, Nishikawa M, Takakura Y Abstract &nbsp;&nbsp;Exosomes are secretory membrane vesicles containing lipids, proteins, and nucleic acids. They act as intercellular transporters by delivering their components to exosome recipient cells. Based on their endogenous delivery system properties, exosomes are expected to become drug delivery systems (DDS) for various molecules such as nucleic acid-based drugs. Important factors such as dr...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - January 13, 2016 Category: Drugs & Pharmacology Authors: Takahashi Y, Nishikawa M, Takakura Y Tags: Yakugaku Zasshi Source Type: research

Mitochondrial DDS Opens Innovative Pharmaceutics.
Abstract &nbsp;&nbsp;A variety of human diseases, including neurodegenerative disorders, ischemic heart disease, diabetes, and cancer have been reported to be associated with mitochondrial dysfunction. Because of this, mitochondrial therapy is expected to be useful and productive in the treatment of such diseases. We previously reported on the development of a MITO-Porter, a liposome-based nanocarrier that permits macromolecular cargos to be delivered into mitochondria via membrane fusion. Intracellular observations using the green fluorescence protein as a model macromolecule provided confirmation that a m...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - January 13, 2016 Category: Drugs & Pharmacology Authors: Yamada Y Tags: Yakugaku Zasshi Source Type: research

Understanding and Responding to the New Wave of Substance Abuse: Law-evading Drugs and Prescription Drug Abuse.
PMID: 26725669 [PubMed - in process] (Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan)
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - January 13, 2016 Category: Drugs & Pharmacology Authors: Shimane T, Funada M Tags: Yakugaku Zasshi Source Type: research

Drug Dependence and Cytotoxicity of Law-evading Drugs: Their Identities Explored from Basic Research.
Abstract &nbsp;&nbsp;Cases of people experiencing disturbed consciousness or dyspnea, causing traffic accidents, or requiring ambulance transport to hospital due to abuse of law-evading chemical substances have become a serious social problem in Japan. Most law-evading herbal products are marketed as incense or herbs and consist of finely chopped, dry vegetative matter mixed with chemical substances (drugs). Analysis of the chemical substances in these herbal products has demonstrated that they contain synthetic cannabinoids. Because there are many cannabinoid compounds, even if a particular drug is regulat...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - January 13, 2016 Category: Drugs & Pharmacology Authors: Funada M Tags: Yakugaku Zasshi Source Type: research

Knowledge regarding Proper Use Guidelines for Benzodiazepines.
Abstract &nbsp;&nbsp;Benzodiazepines (BZs) work by agonising gamma-aminobutyric acid (GABA)-BZ-receptor complex and thereby produce sedation and anti-anxiety effects. BZs are commonly used in several clinical areas as hypnotics or anti-anxiety drugs. However, these drugs once supplied by medical institutions often lead to abuse and dependence. Thus it is important for institutions to supply and manage BZs properly. At Tokyo Women's Medical University Hospital educational activities about proper use of BZs are performed by not only medical doctors but also pharmacists. We coordinate distribution of leaflets ...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - January 13, 2016 Category: Drugs & Pharmacology Authors: Inada K Tags: Yakugaku Zasshi Source Type: research

The Pharmacist as Gatekeeper of Prescription Drug Abuse: Return to “Community Scientists&rdquo.
This article begins by reviewing the current situation of prescription drug abuse and dependence in Japan. The role of pharmacists as gatekeepers in preventing prescription drug abuse is then examined. Finally, this article discusses the effect of intervention in the form of gatekeeper training for community pharmacists. PMID: 26725672 [PubMed - in process] (Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan)
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - January 13, 2016 Category: Drugs & Pharmacology Authors: Shimane T Tags: Yakugaku Zasshi Source Type: research

The Characteristics of Law-evading Drug Users and Effective Approaches.
Abstract &nbsp;&nbsp;The increasing number of law-evading drug users in Japan is becoming a serious social problem. Previous studies have shown that law-evading drug users are younger, more educated, and less antisocial than methamphetamine users. They also tend to have some type of psychiatric disorder before starting drug use; therefore one of the reasons that they start using drugs may be to alleviate certain psychiatric symptoms. Furthermore, if drug users are successful in avoiding arrest, they often lack the motivation to stop, which makes treatment difficult. Therapists are required to be non-confron...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - January 13, 2016 Category: Drugs & Pharmacology Authors: Kondo A Tags: Yakugaku Zasshi Source Type: research

Practical Use of Compound-target Interactions in Chemistry and Drug Discovery~A Chemoinformatics Approach~.
Practical Use of Compound-target Interactions in Chemistry and Drug Discovery<br/>&#xFF5E;A Chemoinformatics Approach&#xFF5E. Yakugaku Zasshi. 2016;136(1):95-6 Authors: Kaneko H, Nakamura S, Kawahsita N PMID: 26725674 [PubMed - in process] (Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan)
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - January 13, 2016 Category: Drugs & Pharmacology Authors: Kaneko H, Nakamura S, Kawahsita N Tags: Yakugaku Zasshi Source Type: research

Classification and Contribution Analysis of Aromatic Clusters in Protein-Ligand Complexes.
Abstract &nbsp;&nbsp;Intermolecular interactions are key features in the stabilization or destabilization of complexes. In particular, interactions involving aromatic rings have been extensively studied both theoretically and experimentally. Studies have shown that aromatic-aromatic interactions can be categorized by ring-ring orientation into a variety of different types, such as stacking interactions and T-shaped interactions. Because these different orientations affect stabilization, analyses of such interactions, for example ab initio molecular orbital calculations, are applied to pairs of aromatic ring...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - January 13, 2016 Category: Drugs & Pharmacology Authors: Yamasaki H, Koseki J, Nishibata Y, Hirono S Tags: Yakugaku Zasshi Source Type: research

Ring-system-based Chemical Structure Enumeration for de Novo Design.
Ring-system-based Chemical Structure Enumeration for <i>de Novo</i> Design. Yakugaku Zasshi. 2016;136(1):101-6 Authors: Miyao T, Kaneko H, Funatsu K Abstract &nbsp;&nbsp;De novo molecular design aims to propose molecules exhibiting desired properties and/or activities, as constructed from scratch. Although this approach opposes the widely used virtual screening (VS), the same criteria should be applied, such as ones based on substructure filters, and quantitative structure-property relationship (QSPR) and quantitative structure-activity relationship (QSAR) regression models. QSPR/QS...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - January 13, 2016 Category: Drugs & Pharmacology Authors: Miyao T, Kaneko H, Funatsu K Tags: Yakugaku Zasshi Source Type: research

In Silico Drug Design Using an Evolutionary Algorithm and Compound Database.
<i>In Silico</i> Drug Design Using an Evolutionary Algorithm and Compound Database. Yakugaku Zasshi. 2016;136(1):107-12 Authors: Kawai K, Takahashi Y Abstract &nbsp;&nbsp;Computational drug design plays an important role in the discovery of new drugs. Recently, we proposed an algorithm for designing new drug-like molecules utilizing the structure of a known active molecule. To design molecules, three types of fragments (ring, linker, and side-chain fragments) were defined as building blocks, and a fragment library was prepared from molecules listed in G protein-coupled receptor (GPC...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - January 13, 2016 Category: Drugs & Pharmacology Authors: Kawai K, Takahashi Y Tags: Yakugaku Zasshi Source Type: research

Molecular Simulations of Protein Systems toward Drug Discovery.
In this study, we propose a new conformational search method for proteins based on a genetic algorithm. We applied this method to an &alpha;-helical protein. We found that the conformations obtained from our simulations are in good agreement with the experimental results. PMID: 26725678 [PubMed - in process] (Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan)
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - January 13, 2016 Category: Drugs & Pharmacology Authors: Sakae Y, Nishikawa N, Tsukamoto S, Suzuki T, Okamoto Y Tags: Yakugaku Zasshi Source Type: research