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After more than a decade of clinical development for cancer and numerous failures, Phase III trials of cyclin-dependent kinase inhibitors are beginning.
Chris Lipinski, originator of the 'rule of five' guidelines for predicting the oral bioavailability of drug candidates, discusses their impact as well as efforts to expand drug-like chemical space and drug repositioning initiatives.
An analysis of recent approved and failed marketing applications for new drugs evaluated by the European Medicines Agency highlights the factors that are most likely to be associated with non-approval.
In vitropharmacological profiling is playing an increasing part in identifying undesirable off-target effects of candidate drugs earlier in the drug discovery process. In this article, authors from four large pharmaceutical companies share their views on the rationale, strategies and methodologies forin vitropharmacological profiling, and recommend a minimal panel of targets for screening.
Tankyrases — members of the poly(ADP-ribose) polymerase (PARP) protein superfamily — are involved in diverse cellular processes, including WNT signalling and telomere maintenance. Here, the authors describe the biology of tankyrases and the discovery of tankyrase-specific inhibitors, which could have broad clinical utility. The challenges that lie ahead for the clinical development of PARP family inhibitors in general are also examined.
The protein kinase C (PKC) family of highly related protein kinases are implicated in several diseases and have been a major focus of drug discovery efforts. However, no single drug specifically targeting a PKC isozyme has yet received approval. Here, Mochly-Rosen and colleagues review the efforts, challenges and opportunities in developing PKC modulators.
Here, the authors discuss how cytokines could be used as therapeutic targets for individuals with asthma that is inadequately controlled using current therapies. They also highlight the need for phenotyping asthma subtypes in order to achieve the best possible patient-focused treatment.
