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 Leurs; Matthias Frech; Rebecca C. Wade; Elizabeth Cunera Maria de Lange; Adriaan P. IJzerman; Anke Müller-Fahrnow; Gerhard F. Ecker

doi:10.1016/j.drudis.2017.02.002

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 Journal › Review article › Academic › peer-review

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 language	English
Pages (from-to)	896-911
Number of pages	16
Journal	Drug Discovery Today
Volume	22
Issue number	6
DOIs	https://doi.org/10.1016/j.drudis.2017.02.002
Publication status	Published - 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., Sadiq, S. K., Bosma, R., Nederpelt, I., Heitman, L. H., Segala, E., Amaral, M., Guo, D., Andres, D., Georgi, V., Stoddart, L. A., Hill, S., Cooke, R. M., de Graaf, C., ... 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

@article{01725d85dd5f482b98219107c56cbe82,

title = "Kinetics for Drug Discovery: an industry-driven effort to target drug residence time",

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.",

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

year = "2017",

month = jun,

day = "1",

doi = "10.1016/j.drudis.2017.02.002",

language = "English",

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Schuetz, DA, de Witte, WEA, Wong, YC, Knasmueller, B, Richter, L, Kokh, DB, Sadiq, SK, Bosma, R, Nederpelt, I, Heitman, LH, Segala, E, Amaral, M, Guo, D, Andres, D, Georgi, V, Stoddart, LA, Hill, S, Cooke, RM, de Graaf, C, Leurs, R, Frech, M, Wade, RC, de Lange, ECM, IJzerman, AP, Müller-Fahrnow, A & Ecker, GF 2017, 'Kinetics for Drug Discovery: an industry-driven effort to target drug residence time', Drug Discovery Today, vol. 22, no. 6, pp. 896-911. https://doi.org/10.1016/j.drudis.2017.02.002

TY - JOUR

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T2 - an industry-driven effort to target drug residence time

AU - Schuetz, Doris A.

AU - de Witte, Wilhelmus Egbertus Arnout

AU - Wong, Yin Cheong

AU - Knasmueller, Bernhard

AU - Richter, Lars

AU - Kokh, Daria B.

AU - Sadiq, S. Kashif

AU - Bosma, Reggie

AU - Nederpelt, Indira

AU - Heitman, Laura H

AU - Segala, Elena

AU - Amaral, Marta

AU - Guo, Dong

AU - Andres, Dorothee

AU - Georgi, Victoria

AU - Stoddart, Leigh A.

AU - Hill, Steve

AU - Cooke, Robert M.

AU - de Graaf, C.

AU - Leurs, Rob

AU - Frech, Matthias

AU - Wade, Rebecca C.

AU - de Lange, Elizabeth Cunera Maria

AU - IJzerman, Adriaan P.

AU - Müller-Fahrnow, Anke

AU - Ecker, Gerhard F.

PY - 2017/6/1

Y1 - 2017/6/1

N2 - 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.

AB - 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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DO - 10.1016/j.drudis.2017.02.002

M3 - Review article

AN - SCOPUS:85019391969

SN - 1359-6446

VL - 22

SP - 896

EP - 911

JO - Drug Discovery Today

JF - Drug Discovery Today

IS - 6

ER -

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

Abstract

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