Epitope mapping of the receptor-bound agonistic form of human chorionic gonadotropin (hCG) in comparison to the antagonistic form (deglycosylated hCG)

Biochem Biophys Res Commun. 1991 Jul 31;178(2):699-706. doi: 10.1016/0006-291x(91)90164-3.

Abstract

On the surface of free human chorionic gonadotropin (hCG), we can distinguish with our panel of monoclonal antibodies (MCA) 14 topographically distinct epitopes (designated alpha 1 - alpha 5, beta 1 - beta 5, alpha beta 1 - alpha beta 4, depending on the subunit they are attached to). Only 2, i.e. the adjacent beta 3 and beta 5 epitopes, of these 14 are accessible to 125I-labeled MCA binding, when hCG is first allowed to bind to the rat testis hCG receptor. This result indicates that the agonist hCG assumes a defined orientation in its receptor-bound state and that, except for that small area comprising the beta 3 and beta 5 epitopes, most of its surface is masked by the hCG receptor. We therefore asked whether the competitive antagonist deglycosylated hCG (degly-hCG), which, when free, is antigenically (as to number and topography of epitopes) indistinguishable from native hCG, would interact with the receptor differently, that is, in a way that can be discerned by this epitope accessibility paradigm. Here we describe that on receptor-bound degly-hCG the beta 3 and beta 5 epitopes were concealed as were all other epitopes. This observation, together with finding the receptor affinity of degly-hCG to be 4 times higher than that of native hCG, suggests that degly-hCG assumes a signal transduction-incompetent ligand orientation and at the same time interacts with the receptor more intensively, i.e. establishes additional ("antagonist accessory") protein-protein contacts besides those involved in agonist binding. It thus appears that the carbohydrate moieties function to prevent formation of such accessory contacts.

MeSH terms

  • Animals
  • Antibodies, Monoclonal*
  • Cell Membrane / metabolism
  • Chorionic Gonadotropin / immunology
  • Chorionic Gonadotropin / metabolism*
  • Epitopes / analysis*
  • Kinetics
  • Male
  • Models, Structural
  • Protein Conformation
  • Radioligand Assay
  • Rats
  • Receptors, Gonadotropin / metabolism*
  • Testis / metabolism

Substances

  • Antibodies, Monoclonal
  • Chorionic Gonadotropin
  • Epitopes
  • Receptors, Gonadotropin