Table of contents
In this issue
p273 | doi:10.1038/nrd2561
Editorial: A double-edged sword
p275 | doi:10.1038/nrd2562
News and Analysis
Vaccine partnerships to tackle neglected diseases | PDF (1,037 KB)
p277 | doi:10.1038/nrd2564
News Feature
All systems go | PDF (1,037 KB)
p278 | doi:10.1038/nrd2565
News in Brief
Diabetes drug development to get tougher | First FDA-approved biologic of 2008 | Pfizer acquires Encysive | More restrictions for anaemia medications | Avastin approval highlights questions about surrogate end points | MHRA urges EU to tighten drug-safety reporting rules | PDF (693 KB)
p280 | doi:10.1038/nrd2566
Patent watch
Stem-cell patents valid | Mircera remains off the US market ... for now | Cabilly rejected again | Mixed results for Celebrex | Melanocortin receptor modulators | PDF (305 KB)
p282 | doi:10.1038/nrd2567
An Audience With
John Powers | PDF (133 KB)
p284 | doi:10.1038/nrd2568
From the analyst's couch
Therapies for COPD | PDF (343 KB)
p285 | doi:10.1038/nrd2533
Fresh from the Pipeline
Etravirine | PDF (235 KB)
p287 | doi:10.1038/nrd2563
Research Highlights
Neurodegenerative disease: Capturing MS targets | PDF (267 KB)
p289 | doi:10.1038/nrd2557
Addiction: Damping down alcohol dependence | PDF (221 KB)
p290 | doi:10.1038/nrd2556
Cardiovascular disease: An emerging role for RAS? | PDF (317 KB)
p290 | doi:10.1038/nrd2558
Antimicrobials: Cholesterol-biosynthesis inhibitor stops infection | PDF (218 KB)
p291 | doi:10.1038/nrd2554
Psychiatric disorders: Double GPCR trouble | PDF (249 KB)
p292 | doi:10.1038/nrd2555
In brief
Analgesia | Chemical biology | Anti-Parasitic drugs | Anticancer drugs | PDF (93 KB)
p292 | doi:10.1038/nrd2559
Perspectives
Opinion
Defining drug disposition determinants: a pharmacogenetic–pharmacokinetic strategy
David A. Katz, Bernard Murray, Anahita Bhathena & Leonardo Sahelijo
p293 | doi:10.1038/nrd2486
Katz and colleagues summarize knowledge on associations between drug pharmacokinetics and variations in genes coding for proteins involved in drug disposition. They propose a novel strategy in which pharmacogenetic data from early clinical studies is used both to feed back to further in vitro studies of drug pharmacokinetics and to feed forward to optimize later-stage clinical trials, and discuss how this could improve drug development.
Reviews
Targeting melanocortin receptors: an approach to treat weight disorders and sexual dysfunction
Jarl E. S. Wikberg & Felikss Mutulis
p307 | doi:10.1038/nrd2331
The melanocortin system is a central element in the control of energy homeostasis, sexual behaviour and autonomic functions. Here, Wikberg and Mutulis discuss the potential of targeting melanocortin receptors across multiple therapeutic areas, and highlight opportunities and challenges for drug discovery in the melanocortin pathway.
Cell-division inhibitors: new insights for future antibiotics
Rowena L. Lock & Elizabeth J. Harry
p324 | doi:10.1038/nrd2510
In recent years, the prevalence of multidrug-resistant bacteria has grown considerably, exacerbated by the limited discovery of novel classes of antibacterial agents. Here, Lock and Harry discuss the therapeutic potential of inhibiting bacterial cell division, highlight specific cell-division proteins representing likely antimicrobial targets, and review the recent progress in this exciting new field.
Structural diversity of G protein-coupled receptors and significance for drug discovery
Malin C. Lagerström & Helgi B. Schiöth
p339 | doi:10.1038/nrd2518
Understanding of the functional significance of the wide structural diversity of G-protein-coupled receptors (GPCRs) — one of the most important families of drug targets — has advanced considerably in recent years. This article provides a comprehensive overview of the five main human GPCR families, discussing gene repertoire, general ligand preference, common and unique structural features, and the potential for future drug discovery.
Article series: A guide to drug discovery
High-throughput electrophysiology: an emerging paradigm for ion-channel screening and physiology
John Dunlop, Mark Bowlby, Ravikumar Peri, Dmytro Vasilyev & Robert Arias
p358 | doi:10.1038/nrd2552
Ion channels remain an under-exploited drug target class owing to the low-throughput nature of patch-clamp electrophysiology. In this Review, Dunlop and colleagues evaluate automated electrophysiology platforms and discuss their impact in terms of ion-channel screening, lead optimization and the assessment of cardiac ion-channel safety liability.
