Effect of detergent on "promiscuous" inhibitors

Ali J. Ryan; Norman M. Gray; Peter N. Lowe; Chun Wa Chung

doi:10.1021/jm0340896

Effect of detergent on "promiscuous" inhibitors

Ali J. Ryan, Norman M. Gray, Peter N. Lowe, Chun Wa Chung^*

^*Corresponding author for this work

Research output: Contribution to journal › Article › peer-review

223 Citations (Scopus)

Abstract

The term "promiscuous" inhibitors has been coined for compounds whose inhibition mechanism involves the interaction of aggregates of many compound molecules with the target protein, rather than the binding of individual molecules. This paper demonstrates that promiscuous inhibitors can be differentiated from classical 1:1 inhibitors by the judicious use of detergents, making it possible to configure assays that significantly reduce this undesirable mechanism of inhibition without compromising assay performance.

Original language	English
Pages (from-to)	3448-3451
Number of pages	4
Journal	Journal of Medicinal Chemistry
Volume	46
Issue number	16
DOIs	https://doi.org/10.1021/jm0340896
Publication status	Published - 31 Jul 2003
Externally published	Yes

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AB - The term "promiscuous" inhibitors has been coined for compounds whose inhibition mechanism involves the interaction of aggregates of many compound molecules with the target protein, rather than the binding of individual molecules. This paper demonstrates that promiscuous inhibitors can be differentiated from classical 1:1 inhibitors by the judicious use of detergents, making it possible to configure assays that significantly reduce this undesirable mechanism of inhibition without compromising assay performance.

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Effect of detergent on "promiscuous" inhibitors

Abstract

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