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Rational Development of Novel Activity Probes for the Analysis of Human Cytochromes P450
Author(s) -
Sellars Jonathan D.,
Skipsey Mark,
Gravell Sebastian,
Abumansour Hamza,
Kashtl Ghasaq,
Irfan Jawaria,
Khot Mohamed,
Pors Klaus,
Patterson Laurence H.,
Sutton Chris W.
Publication year - 2016
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201600134
Subject(s) - cytochrome p450 , chemistry , gene isoform , biochemistry , enzyme , computational biology , drug development , identification (biology) , biology , drug , pharmacology , gene , botany
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.