A comprehensive map of molecular drug targets

A comprehensive map of molecular drug targets

2017 January ; 16(1): 19–34. doi:10.1038/nrd.2016.230. | Rita Santos, Oleg Ursu, Anna Gaulton, A. Patricia Bento, Ramesh S. Donadi, Cristian G. Bologa, Anneli Karlsson, Bissan Al-Lazikani, Anne Hersey, Tudor I. Oprea, and John P. Overington
This article presents an updated comprehensive map of molecular targets for 1,578 US FDA-approved drugs, curated from three independent teams. The map includes 893 human and pathogen-derived biomolecules, with a focus on the distribution of targets across disease areas and the success of privileged target families. The authors highlight the challenges in defining efficacy targets, particularly for broad-spectrum drugs and those with complex mechanisms of action. They also explore the relationship between drug targets, therapeutic areas, and the conservation of targets in animal models. The analysis reveals that privileged families such as GPCRs, ion channels, protein kinases, and nuclear receptors continue to dominate the drug target space, while the proportion of protein kinase and protease targets has increased. The study emphasizes the importance of maintaining and updating this data set to guide future drug development and innovation.This article presents an updated comprehensive map of molecular targets for 1,578 US FDA-approved drugs, curated from three independent teams. The map includes 893 human and pathogen-derived biomolecules, with a focus on the distribution of targets across disease areas and the success of privileged target families. The authors highlight the challenges in defining efficacy targets, particularly for broad-spectrum drugs and those with complex mechanisms of action. They also explore the relationship between drug targets, therapeutic areas, and the conservation of targets in animal models. The analysis reveals that privileged families such as GPCRs, ion channels, protein kinases, and nuclear receptors continue to dominate the drug target space, while the proportion of protein kinase and protease targets has increased. The study emphasizes the importance of maintaining and updating this data set to guide future drug development and innovation.
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