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A Mini Review of Promiscuous Inhibitors, Nonspecific Inhibition and Detergent Effect

He Kelvin Bai

Abstract


High-throughput screening is widely employed in early stage of drug discovery for identification of novel leads. While high-throughput screening is able to search a large library of chemical compounds in a relative short period of time, it is susceptible to false-positive hits. In this mini review, we summarized the known attributes of promiscuous inhibitors and the mechanism of their inhibition effect, as well as the factors affecting its potency. Next, we reviewed the recent studies of the detergent effects on the promiscuous inhibitors and discussed the potential application to reduce false-positive signals. 


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References


Feng, B.Y, A Shelat, T.N Doman, R.K Guy, and B.K Shoichet. "High-Throughput Assays for Promiscuous Inhibitors." Nat. Chem. Bio., 2005: 146-148.

Feng, B.Y, and B.K Shoichet. "A detergent-based assay for the detection of promiscuous inhibitors." Nat. Protoc., 2006: 550-553.

Feng, B.Y, et al. "A High-throughput Screen for Aggregation-based Inhibition in a Large compound Library." J. Med. Chem, 2007: 2385-2390.

Inglese, J, et al. "High-throughput screening assays for the identification of chemical probes." Nat Chem Bio, 2007: 466-479.

McGovern, S.L, B.T. Helfand, B.Y. Feng, and B.K. Shoichet. "A specific mechanism of nonspecific inhibition." J. Med Chem, 2003: 4265-4272.

McGovern, S.L, E Caselli, N Grigorieff, and B.K Schoichet. "A Common Mechanism Underlying Promiscuous Inhibitors from Virtual and High-throughput Screening." J. Med. Chem, 2002: 1712-1722.

Ryan, A.J, N.M. Gray, P.N Lowe, and C.W Chung. "Effect of Detergent on "Promiscuous" Inhibitors." J. Med. Chem, 2003: 3448-3451.




DOI: http://dx.doi.org/10.15272%2Fjmpi.v1i5.42

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