The Activation Mechanism of Glycoprotein Hormone Receptors with Implications in the Cause and Therapy of Endocrine Diseases*♦

A Brüser, A Schulz, S Rothemund, A Ricken… - Journal of Biological …, 2016 - ASBMB
Glycoprotein hormones (GPHs) are the main regulators of the pituitary-thyroid and pituitary-
gonadal axes. Selective interaction between GPHs and their cognate G protein-coupled
receptors ensure specificity in GPH signaling. The mechanisms of how these hormones
activate glycoprotein hormone receptors (GPHRs) or how mutations and autoantibodies can
alter receptor function were unclear. Based on the hypothesis that GPHRs contain an
internal agonist, we systematically screened peptide libraries derived from the ectodomain …