Carboetomidate: an analog of etomidate that interacts weakly with 11β-hydroxylase.

ABSTRACT:

Background

Carboetomidate is a pyrrole etomidate analog that is 3 orders of magnitude less potent an inhibitor of in vitro cortisol synthesis than etomidate (an imidazole) and does not inhibit in vivo steroid production. Although carboetomidate's reduced functional effect on steroid synthesis is thought to reflect lower binding affinity to 11β-hydroxylase, differential binding to this enzyme has never been experimentally demonstrated. In the current study, we tested the hypothesis that carboetomidate and etomidate bind with differential affinity to 11β-hydroxylase by comparing their abilities to inhibit photoaffinity labeling of purified enzyme by a photoactivatable etomidate analog and to modify the enzyme's absorption spectrum in a way that is indicative of ligand binding. In add

SUBMITTER: Shanmugasundararaj S 

PROVIDER: S-EPMC3836822 | biostudies-literature | 2013 Jun

REPOSITORIES: biostudies-literature