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Kinetics for Drug Discovery: an industry-driven effort to target drug residence time

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DRUG DISCOVERY TODAY
卷 22, 期 6, 页码 896-911

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ELSEVIER SCI LTD
DOI: 10.1016/j.drudis.2017.02.002

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  1. Innovative Medicines Initiative Joint Undertaking (IMI JU) [115366]
  2. EU's Seventh Framework Programme (FP7)
  3. European Federation of Pharmaceutical Industries and Associations (EFPIA)
  4. Klaus Tschira Foundation

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A considerable number of approved drugs show non-equilibrium binding characteristics, emphasizing the potential role of drug residence times for in vivo efficacy. Therefore, a detailed understanding of the kinetics of association and dissociation of a target-ligand complex might provide crucial insight into the molecular mechanism-of-action of a compound.This deeper understanding will help to improve decision making in drug discovery, thus leading to a better selection of interesting compounds to be profiled further. In this review, we highlight the contributions of the Kinetics for Drug Discovery (K4DD) Consortium, which targets major open questions related to binding kinetics in an industry-driven public-private partnership.

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