Development of amide-based fluorescent probes for selective measurement of carboxylesterase 1 activity in tissue extracts.

ABSTRACT: Carboxylesterases are well known for their role in the metabolism of xenobiotics. However, recent studies have also implicated carboxylesterases in regulating a number of physiological processes including metabolic homeostasis and macrophage development, underlying the need to quantify them individually. Unfortunately, current methods for selectively measuring the catalytic activity of individual carboxylesterases are not sufficiently sensitive to support many biological studies. In order to develop a more sensitive and selective method to measure the activity of human carboxylesterase 1 (hCE1), we generated and tested novel substrates with a fluorescent aminopyridine leaving group. hCE1 showed at least a 10-fold higher preference for the optimized substrate 4-MOMMP than the 13 other ester

SUBMITTER: Kodani SD 

PROVIDER: S-EPMC5696082 | biostudies-literature | 2017 Dec

REPOSITORIES: biostudies-literature