The DOI matches its Crossref record; 1 of the 1 references it cites were found in a registry or an index.
Conformational Adaptation in Drug–Target Interactions and Residence Time
Abstract
Although drug-target interactions are commonly illustrated in terms of structurally static binding and dissociation events, such descriptions are inadequate to explain the impact of conformational dynamics on these processes. For high-affinity interactions, both the association and dissociation of drug molecules to and from their targets are often controlled by conformational changes of the target. Conformational adaptation can greatly influence the residence time of a drug on its target (i.e., the lifetime of the binary drug-target complex); long residence time can lead to sustained pharmacology and may also mitigate off-target toxicity. In this perspective, the kinetics of drug-target association and dissociation reactions are explored, with particular emphasis on the impact of conformational adaptation on drug-target residence time.
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Citations
Cites
Drug-target residence time and its implications for lead optimization
Copeland, R. A., Pompliano, D. L., & Meek, T. D. (2006) · Nature Reviews Drug Discovery · doi:10.1038/nrd2082 · Cited by 1,464
Self-citation
Cited by
Roskoski, R. (2016) · Pharmacological Research · doi:10.1016/j.phrs.2015.10.021 · Cited by 886
The drug–target residence time model: a 10-year retrospective
Copeland, R. A. (2016) · Nature Reviews Drug Discovery · doi:10.1038/nrd.2015.18 · Cited by 722
Self-citationProtein Binding Pocket Dynamics
Stank, A., Kokh, D. B., Fuller, J. C., & Wade, R. C. (2016) · Accounts of Chemical Research · doi:10.1021/acs.accounts.5b00516 · Cited by 445
Fan, J., & de Lannoy, I. A. M. (2014) · Biochemical Pharmacology · doi:10.1016/j.bcp.2013.09.007 · Cited by 309
Drug–Target Kinetics in Drug Discovery
Tonge, P. J. (2018) · ACS Chemical Neuroscience · doi:10.1021/acschemneuro.7b00185 · Cited by 287
Metadata
- Authors
- Copeland, R. A.
- Venue
- Future Medicinal Chemistry
- Publisher
- Informa UK Limited
- Published
- 2011-09
- Volume
- 3
- Issue
- 12
- Pages
- 1491-1501
- ISSN
- 1756-8919 (ISSN-L)
- 1756-8927
- OpenAlex
- W2006932016
- Cited by
- 196
- References
- 1
- FWCI
- 5.76
- Type
- journal article
- Language
- en
- Open access
- closed
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