Volume 10 Issue 9, September 2011

Bayer halts nearly two-thirds of its target-validation projects because in-house experimental findings fail to match up with published literature claims, finds a first-of-a-kind analysis on data irreproducibility.

Concerns about cancer risks prompted a negative vote by an FDA advisory committee on the SGLT2 inhibitor dapagliflozin, but experts remain hopeful for the novel class of antidiabetic drugs.

Joe Selby, the newly appointed Executive Director of the Patient-Centered Outcomes Research Institute (PCORI), discusses the agenda for the new federally-mandated comparative effectiveness research-focused organization.

Analysing data on bioactive compounds can provide insight for developing improved molecules, although much of this data currently resides in proprietary databases. However, even when such data is made available in research articles or public databases, key information is often missing, or the data is not in a format suited to data-mining. With the aim of addressing these issues, this article proposes reporting guidelines for bioactive entities, which have been developed by representatives from industry, academia and data resource providers.

Cancer cells have adapted metabolically to support their characteristic high rate of proliferation. Targeting the metabolic differences between cancer cells and normal cells is emerging as a promising therapeutic approach. Here, Vander Heiden discusses the associated challenges and limitations of this anticancer strategy and reviews evidence supporting specific metabolic enzymes as potential targets.

The identification of physiological and pharmacological functions of GABA_A (γ-aminobutyric acid, type A) receptor subtypes has renewed the interest in the GABA_Areceptor system as a target for the development of non-sedating anxiolytics, as well as of drugs for indications that are distinct from those of classical benzodiazepines, such as analgesia, schizophrenia and depression.

The amyloid cascade hypothesis — which posits that the deposition of the amyloid-β peptide in the brain is a central event in Alzheimer's disease (AD) pathology — has strongly influenced recent AD drug discovery efforts. However, so far all agents targeting amyloid-β have failed in Phase III trials. Here, Karran and colleagues re-evaluate the amyloid cascade hypothesis and explore the future potential of amyloid-β-targeting therapeutics.