A practical strategy to develop isoform-selective near-infrared fluorescent probes for human cytochrome P450 enzymes.

ABSTRACT: Currently, the development of selective fluorescent probes toward targeted enzymes is still a great challenge, due to the existence of numerous isoenzymes that share similar catalytic capacity. Herein, a double-filtering strategy was established to effectively develop isoenzyme-specific fluorescent probe(s) for cytochrome P450 (CYP) which are key enzymes involving in metabolism of endogenous substances and drugs. In the first-stage of our filtering approach, near-infrared (NIR) fluorophores with alkoxyl group were prepared for the screening of CYP-activated fluorescent substrates using a CYPs-dependent incubation system. In the second stage of our filtering approach, these candidates were further screened using reverse protein-ligand docking to effectively determine CYP isoenzyme-specific

SUBMITTER: Feng L 

PROVIDER: S-EPMC9279627 | biostudies-literature | 2022 Apr

REPOSITORIES: biostudies-literature