Characterization of 12 GnRH peptide agonists - a kinetic perspective.

ABSTRACT:

Background and purpose

Drug-target residence time is an important, yet often overlooked, parameter in drug discovery. Multiple studies have proposed an increased residence time to be beneficial for improved drug efficacy and/or longer duration of action. Currently, there are many drugs on the market targeting the gonadotropin-releasing hormone (GnRH) receptor for the treatment of hormone-dependent diseases. Surprisingly, the kinetic receptor-binding parameters of these analogues have not yet been reported. Therefore, this project focused on determining the receptor-binding kinetics of 12 GnRH peptide agonists, including many marketed drugs.

Experimental approach

A novel radioligand-binding competition association assay was developed and optimized for the human GnRH receptor

SUBMITTER: Nederpelt I 

PROVIDER: S-EPMC4813373 | biostudies-literature | 2016 Jan

REPOSITORIES: biostudies-literature