| Literature DB >> 28412474 |
Doris A Schuetz1, Wilhelmus Egbertus Arnout de Witte2, Yin Cheong Wong2, Bernhard Knasmueller1, Lars Richter1, Daria B Kokh3, S Kashif Sadiq3, Reggie Bosma4, Indira Nederpelt5, Laura H Heitman5, Elena Segala6, Marta Amaral7, Dong Guo5, Dorothee Andres8, Victoria Georgi8, Leigh A Stoddart9, Steve Hill9, Robert M Cooke6, Chris De Graaf4, Rob Leurs4, Matthias Frech10, Rebecca C Wade11, Elizabeth Cunera Maria de Lange2, Adriaan P IJzerman5, Anke Müller-Fahrnow8, Gerhard F Ecker12.
Abstract
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.Mesh：
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Year: 2017 PMID： 28412474 DOI： 10.1016/j.drudis.2017.02.002
Source DB: PubMed Journal: Drug Discov Today ISSN： 1359-6446 Impact factor: 7.851