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

Doris A. Schuetz, Wilhelmus Egbertus Arnout de Witte, Yin Cheong Wong, Bernhard Knasmueller, Lars Richter, Daria B. Kokh, S. Kashif Sadiq, Reggie Bosma, Indira Nederpelt, Laura H Heitman, Elena Segala, Marta Amaral, Dong Guo, Dorothee Andres, Victoria Georgi, Leigh A. Stoddart, Steve Hill, Robert M. Cooke, C. de Graaf, Rob LeursMatthias Frech, Rebecca C. Wade, Elizabeth Cunera Maria de Lange, Adriaan P. IJzerman, Anke Müller-Fahrnow, Gerhard F. Ecker*

*Corresponding author for this work

Research output: Contribution to JournalReview article

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.

Original languageEnglish
Pages (from-to)896-911
Number of pages16
JournalDrug Discovery Today
Volume22
Issue number6
DOIs
Publication statusPublished - 1 Jun 2017

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Schuetz, D. A., de Witte, W. E. A., Wong, Y. C., Knasmueller, B., Richter, L., Kokh, D. B., ... Ecker, G. F. (2017). Kinetics for Drug Discovery: an industry-driven effort to target drug residence time. Drug Discovery Today, 22(6), 896-911. https://doi.org/10.1016/j.drudis.2017.02.002