Nature Reviews Drug Discovery contents January 2012 Volume 11 Number 1 pp 1-86

TABLE OF CONTENTS
January 2012 Volume 11 Number 1
Impact Factor 28.712 *	In this issue News and Analysis Research Highlights Reviews Also this month Collections: Ten years in drug discovery  Featured article: The pharmacological landscape and therapeutic potential of serine hydrolases Daniel A. Bachovchin & Benjamin F. Cravatt
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Nature Reviews Drug Discovery Turns Ten Timely Content, Leading Authors, Enhanced Experience Access selected free content from Nature Reviews Drug Discovery to celebrate the 10th anniversary of this leading publication. www.nature.com/nrd/collections/10/index.html
In this issue p1 | doi:10.1038/nrd3639 Full Text
Editorial: A decade in drug discovery p3 | doi:10.1038/nrd3648 Nature Reviews Drug Discovery marks its tenth anniversary this month, providing an opportunity to reflect on the evolution of the landscape of drug research and development (R&D). Full Text | PDF
NEWS AND ANALYSIS		Top
New neglected disease research scheme pools IP and expertise Simon Frantz p5 | doi:10.1038/nrd3642 WIPO Re:Search aims to encourage drug discovery for neglected diseases by broadening the scope of the assets members are willing to share. PDF
2011 in reflection Asher Mullard p6 | doi:10.1038/nrd3643 Last year saw an upturn in new drug approvals, the end of patent protection for the world's top-selling drug, continued regulatory negotiations and more. PDF
NEWS IN BRIEF
Falling R&D returns? | Amgen springs Enbrel patent surprise | Integrating whole-genome sequencing into drug trials p9 | doi:10.1038/nrd3644 PDF
BIOBUSINESS BRIEFS Deal watch: High hopes for oral SYK inhibitor in rheumatoid arthritis Monica Hoyos Flight p10 | doi:10.1038/nrd3631 PDF
Market watch: Upcoming market catalysts in Q1 2012 Edny Inui p10 | doi:10.1038/nrd3632 PDF
Trial watch: PCSK9 antibody reduces LDL cholesterol Sarah Crunkhorn p11 | doi:10.1038/nrd3633 PDF
PATENT WATCH Key patent-related events of the past 10 years | Japan | EU and the United Kingdom | United States | Patent applications 2002–2011 Charlotte Harrison p12 | doi:10.1038/nrd3641 PDF
AN AUDIENCE WITH Mark Fishman p14 | doi:10.1038/nrd3640 Mark Fishman, President of the Novartis Institutes for BioMedical Research, looks back on his past decade of heading up R&D. PDF
FROM THE ANALYST'S COUCH A decade of change John Arrowsmith p17 | doi:10.1038/nrd3630 Data on indicators such as the number and success rate of research and development projects illustrate trends in the pharmaceutical industry over the past decade. PDF
FRESH FROM THE PIPELINE Brentuximab vedotin Anas Younes, Uma Yasothan & Peter Kirkpatrick p19 | doi:10.1038/nrd3629 Antibody–drug conjugate specific for CD30 approved by the US Food and Drug Administration for the treatment of two types of lymphoma. PDF
RESEARCH HIGHLIGHTS Top Vaccines: Enhancing glycan presentation increases vaccine efficacy p21 | doi:10.1038/nrd3637 PDF Neurodegenerative disease: Novel ALS therapy shows promise in Phase II p22 | doi:10.1038/nrd3634 PDF G protein-coupled receptors: Case builds for TGR5 as metabolic syndrome target p22 | doi:10.1038/nrd3638 PDF Cancer: Opening the door to a new class of proteasome inhibitors p23 | doi:10.1038/nrd3636 PDF Antiparasitic drugs: Two-pronged tactics for malaria control p24 | doi:10.1038/nrd3635 PDF IN BRIEF Neurodegenerative disease: Inhibiting β-secretase in humans | Computational chemistry: Crowd-based enhancement of chemical diversity | Kinase inhibitors: Analysing kinase inhibitor selectivity PDF Drug Discovery JOBS of the week Senior Scientist - Drug Delivery Development Genentech Post-Doctoral (WW) - Target Identification and Drug Discovery - Immunobiology and Cancer Research Program (W Wang) Oklahoma Medical Research Foundation (OMRF) Sr. Research Biologist Merck Drug Discovery and Development Services Sales Manager 1975 Millipore Corp. Principle Scientist in Molecular / cellular Biology for drug discovery Shanghai Hengrui Pharmaceutical Co. Ltd More Science jobs from Drug Discovery EVENT Advances and Progress in Drug Design 21.-22.02.11 London, UK More science events from
REVIEWS		Top
Interfacial inhibitors: targeting macromolecular complexes Yves Pommier & Christophe Marchand p25 | doi:10.1038/nrd3404 Interfacial inhibitors bind to the interfaces of macromolecular machines (for example, polymerases or ribosomes) and stall their progress. A number of natural product and synthetic interfacial inhibitors are in the clinic for the treatment of cancer and bacterial infections. Here, Pommier and Marchand review the concept of interfacial inhibition, and discuss the rationale and methods for the discovery of novel interfacial inhibitors. Abstract | Full Text | PDF
Designing antimicrobial peptides: form follows function Christopher D. Fjell, Jan A. Hiss, Robert E. W. Hancock & Gisbert Schneider p37 | doi:10.1038/nrd3591 Natural antimicrobial peptides defend host organisms against microbes, but most have modest direct antibiotic activity. This article reviews the latest computer-assisted design strategies to develop enhanced peptide variants, and examines emerging data from clinical trials. These broad-spectrum peptides could lead to the development of next-generation antibiotics. Abstract | Full Text | PDF
The pharmacological landscape and therapeutic potential of serine hydrolases Daniel A. Bachovchin & Benjamin F. Cravatt p52 | doi:10.1038/nrd3620 Serine hydrolases are one of the largest and most diverse enzyme classes in nature and have many crucial roles in human physiology and disease. Several serine hydrolases are targets of clinically approved drugs, but many enzymes in this family remain poorly characterized and lack selective inhibitors. Here, Bachovchin and Cravatt discuss the therapeutic potential of serine hydrolases and present novel inhibitor discovery strategies. Abstract | Full Text | PDF | Supplementary information
Targeting proteinase-activated receptors: therapeutic potential and challenges Rithwik Ramachandran, Farshid Noorbakhsh, Kathryn DeFea & Morley D. Hollenberg p69 | doi:10.1038/nrd3615 Here, the authors highlight the role of proteinase-activated receptors in physiology and in conditions such as cancer and cardiovascular disorders. They also review possible strategies for developing proteinase-activated receptor antagonists and the challenges associated with this goal. Abstract | Full Text | PDF
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