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The focus for the use of bioinformatics resources in the pharmaceutical industry is increasingly moving from the vigorous pursuit of intellectual property towards exploration of pre-competitive collaborations and engagement with the public domain. In this article, we discuss the rationale for these changes and the associated challenges, and also propose new areas of public–private collaboration in computational biology and chemistry that could enhance drug discovery in academia and industry.
The dysregulated activity of protein kinases is commonly implicated in human cancers, and many anti-cancer agents aiming to inhibit specific kinases are now approved or under investigation. Here, Settleman and colleagues discuss factors responsible for the variability in clinical sensitivity to small-molecule kinase inhibitors that should be considered in the development and use of new agents.
The protein methyltransferases (PMTs) are emerging as a group of enzymes that play key parts in human diseases. This Review highlights data that support the validation of PMTs as therapeutic targets, including the structural and mechanistic data that support the concept of the PMTs as a druggable target class.
The nicotinic acetylcholine receptors (nAChRs) are ligand-gated ion channels, the activity of which modulates many neurotransmitter systems. They are therefore therapeutic targets for the treatment of several central nervous system disorders. In this article, Taly and colleagues present recent advances in our understanding of the atomic structure, functional organization and conformational transitions of the nAChR that may be applied to drug discovery, and discuss agents currently in development.
