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Rational Development of Novel Activity Probes for the Analysis of Human Cytochromes P450

Lookup NU author(s): Dr Jon Sellars

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Abstract

© 2016 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim 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.

Publication metadata

Author(s): Sellars JD, Skipsey M, Sadr-ul-Shaheed, Gravell S, Abumansour H, Kashtl G, Irfan J, Khot M, Pors K, Patterson LH, Sutton CW

Publication type: Article

Publication status: Published

Journal: ChemMedChem

Year: 2016

Volume: 11

Issue: 11

Pages: 1122-1128

Print publication date: 08/06/2016

Online publication date: 06/05/2016

Acceptance date: 04/03/2016

ISSN (print): 1860-7179

ISSN (electronic): 1860-7187

Publisher: John Wiley and Sons Ltd

URL: https://doi.org/10.1002/cmdc.201600134

DOI: 10.1002/cmdc.201600134

PubMed id: 27154431

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