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

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 insi...

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Bibliographic Details
Main Authors: Schuetz, Doris A. (Author) , Kokh, Daria B. (Author) , Sadiq, Kashif (Author) , Wade, Rebecca C. (Author)
Format: Article (Journal)
Language:English
Published: 2017, Apr 13
In: Drug discovery today
Year: 2017, Volume: 22, Issue: 6, Pages: 896-911
ISSN:1878-5832
DOI:10.1016/j.drudis.2017.02.002
Online Access:Verlag, Volltext: http://dx.doi.org/10.1016/j.drudis.2017.02.002
Verlag, Volltext: http://www.sciencedirect.com/science/article/pii/S1359644617300958
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Author Notes: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, Chris De Graaf, Rob Leurs, Matthias Frech, Rebecca C. Wade, Elizabeth Cunera Maria de Lange, Adriaan P. IJzerman, Anke Müller-Fahrnow and Gerhard F. Ecker
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Summary: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.
Item Description:Gesehen am 18.04.2018
Physical Description:Online Resource
ISSN:1878-5832
DOI:10.1016/j.drudis.2017.02.002

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