G Protein-Coupled Estrogen Receptor (GPER) Agonist Dual Binding Mode Analyses toward Understanding of its Activation Mechanism: A Comparative Homology Modeling Approach.

ABSTRACT: G protein-coupled estrogen receptor (GPER) has been shown to be important in several disease states such as estrogen sensitive cancers. While several selective ligands have been identified for the receptor, little is known about how they interact with GPER and how their structures influence their activity. Specifically, within one series of ligands, whose structure varied only at one position, the replacement of a hydrogen atom with an acetyl group changed a potent antagonist into a potent agonist. In this study, two GPER homology models were constructed based on the x-ray crystal structures of both the active and inactive β₂-adrenergic receptors (β₂AR) in an effort to characterize the differences of binding modes between agonists and antagonists to the receptor, and

SUBMITTER: Arnatt CK 

PROVIDER: S-EPMC4517684 | biostudies-literature | 2013 Jul

REPOSITORIES: biostudies-literature