Friday, November 25, 2011

Drug Discovery@nature.com 25 November 2011

Drug Discovery
TABLE OF CONTENTS

25 November 2011

News
Analysis
Research Highlights
Research & Reviews
Careers


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News

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Stem-cell pioneer bows out
doi:10.1038/479459a
Geron halts first-of-its-kind clinical trial for spinal therapy.
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Preemptive genotyping trialed to prevent adverse drug reactions
doi:10.1038/nm1111-1323
Schemes to couple a patient’s genetic information to effective intervention strategies could avoid serious adverse drug reactions.
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First drugs found to inhibit elusive cancer target
doi:10.1038/nm1111-1325
Buoyed by the promising therapeutic effects in mice with several types of cancer of JQ1, a small molecule that inhibits bromodomain protein 4 and thereby indirectly prevents MYC expression, companies are racing to test the molecules in clinical trials.
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Hepatitis C: move over interferon
doi:10.1038/nbt.2031
Following approval of hepatitis C virus protease inhibitors Incivek and Victrelis, companies are partnering to devise all-oral combination antiviral regimens without interferon alpha. But the virus is a long way from vanquished.
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Analysis

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Dampening neuroinflammation
doi:10.1038/scibx.2011.1254
Researchers have shown that a small molecule inhibitor of monoacylglycerol lipase reduces neuroinflammation in a mouse model of Parkinson's disease, and are studying the compound in other neurodegenerative and neurological diseases. Newco Abide Therapeutics is exercising an option to license these inhibitors.
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Vemurafenib
doi:10.1038/nrd3579
In August 2011, vemurafenib, an inhibitor of BRAF kinase, was approved by the US Food and Drug Administration for the treatment of patients with unresectable or metastatic melanoma with the BRAFV600E mutation.
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The depression market
doi:10.1038/nrd3585
This article outlines the existing therapies and key drugs that have recently been launched or are in clinical development for the treatment of major depressive disorder, a disorder for which fewer than half of patients currently receive drug treatment.
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Research Highlights

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Inflammatory diseases: Stopping monocytes in their tracks
doi:10.1038/nrd3590
A recently described method for specifically targeting inflammatory monocyte migration attenuates disease severity in mouse models of a number of inflammatory conditions.
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Lead identification: Keeping tetramers together
doi:10.1038/nrd3586
A new study has identified several drug candidates that inhibit the first step in amyloid formation by preventing the dissociation of transthyretin tetramers.
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Neurodevelopmental disorders: Mice that mirror autism
doi:10.1038/nrn3129
Mice lacking Cntnap2 show abnormal neuronal migration, asynchronous firing patterns and have an autism-like phenotype that can be partially normalized by treatment with risperidone.
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Research & Reviews

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Quantifying factors for the success of stratified medicine
doi:10.1038/nrd3557
Co-developing a drug with a diagnostic presents challenges for product developers, regulators, payers and physicians. This article uses data from case studies, coupled with modelling of clinical outcomes and economic value, to quantify the effects of decisions on key issues such as clinical trial design.
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Targeting protein prenylation for cancer therapy
doi:10.1038/nrc3151
This article outlines the mechanisms by which inhibitors of farnesyltransferase and geranylgeranyltransferase 1 are expected to confer anticancer effects, and strategies to overcome the overall lack of success of these agents in clinical trials compared with their preclinical efficacy.
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Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity
doi:10.1038/nbt.2017
Anastassiadis et al. used functional assays to profile the activities of 178 commercially available kinase inhibitors against 300 recombinant human protein kinases, revealing complex and often unexpected interactions between protein kinases and kinase inhibitors.
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Comprehensive analysis of kinase inhibitor selectivity doi:10.1038/nbt.1990
By profiling the binding of 72 kinase inhibitors to 442 human kinase catalytic domains, Davis et al. have uncovered group-specific differences in selectivity and suggest the feasibility of developing reasonably specific inhibitors for most kinases.
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Drug Discovery
JOBS of the week
Research Assistant
Cambridge Institute for Medical Research (CIMR)
Professor of Supramolecular Separations
University of Amsterdam, the Netherlands
Postdoctoral Fellowhip University of California / CNSI
University of California / California NanoSystems Institute
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Drug Discovery
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International Conference on Drug Therapy in TB Infection
06.-07.01.12
Edinburgh, UK
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Careers

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Career snapshots archive
Career snapshots feature people associated with drug discovery and drug development, with the aim of providing expert insights and advice on a wide range of positions and career paths in this field.
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