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Rational development of novel activity probes for the analysis of human cytochromes P450
Sellars, J.D. Skipsey, M. Sadr-ul-Shaheed Gravell, Sebastian Abumansour, Hamza M.A. Kashtl, Ghasaq J. Irfan, Jawaria Khot, Mohamed Pors, Klaus Patterson, Laurence H.
Sellars, J.D.
Skipsey, M.
Sadr-ul-Shaheed
Gravell, Sebastian
Abumansour, Hamza M.A.
Kashtl, Ghasaq J.
Irfan, Jawaria
Khot, Mohamed
Pors, Klaus
Patterson, Laurence H.
Publication Date
08/06/2016
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(c) Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim. This is the peer-reviewed version of the following article: Sellars JD, Skipsey M, Sadr-ul-Shaheed S et al (2016) Rational development of novel activity probes for the analysis of human cytochromes P450. ChemMedChem. 11(11): 1122-1128, which has been published in final form at http://dx.doi.org/10.1002/cmdc.201600134. This article may be used for non-commercial purposes in accordance with Wiley Terms and Conditions for Self-Archiving.
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Abstract
The identification and quantification of functional cytochromes P450 (CYPs) in biological samples is proving important for robust analyses of drug efficacy and metabolic disposition. In this study, a novel CYP activity-based probe was rationally designed and synthesised, demonstrating selective binding of CYP isoforms. The dependence of probe binding upon the presence of NADPH permits the selective detection of functionally active CYP. This allows the detection and analysis of these enzymes using biochemical and proteomic methodologies and approaches.
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Accepted manuscript
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Sellars JD, Skipsey M, Sadr-ul-Shaheed et al (2016) Rational development of novel activity probes for the analysis of human cytochromes P450. ChemMedChem. 11(11): 1122-1128.
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