A follicle-stimulating hormone receptor ecto-domain epitope that is a target for receptor immunoneutralization yet does not affect ligand contact and activation

Endocrine. 2000 Dec;13(3):361-7. doi: 10.1385/endo:13:3:361.

Abstract

The follicle-stimulating hormone receptor (FSHR) large extracellular domain suggests that interaction of ligand with receptor is likely to be complex. Residues 265-296 of the FSHR are part of a sequence primarily nonhomologous with other glycoprotein hormone receptors. A reasonable hypothesis is that this sequence of the FSHR plays a role in binding FSH. Flow cytometry studies of this region revealed that antibody X179 against peptide R265-S296 binds to human FSHR expressed by CHO cells and can be competed against by preincubating the cells with hFSH. These results suggested that the region corresponding to residues 265-296 in the extracellular domain of the FSHR is involved in binding to hormone. To test this hypothesis 10 scanning alanine mutants of rFSHR at the 265-296 epitope were generated, and the binding characteristics of these mutants were studied. Their affinity constants for 125I-hFSH did not deviate greatly from that of wild-type FSHR, in which some mutants exhibited an approximately two- to threefold reduction in Ka compared to wild-type receptor, and no mutation abolished signal transduction. These results lead to rejection of the hypothesis that this region contains residues critical for conveying hormone specificity and receptor-dependent hormone action.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Alanine
  • Amino Acid Sequence
  • Animals
  • Binding Sites
  • CHO Cells
  • Cricetinae
  • Epitopes / chemistry
  • Epitopes / immunology*
  • Flow Cytometry
  • Follicle Stimulating Hormone / metabolism*
  • Gene Expression
  • Humans
  • Immune Sera / metabolism
  • Immune Sera / pharmacology
  • Molecular Sequence Data
  • Mutagenesis
  • Radioligand Assay
  • Receptors, FSH / genetics
  • Receptors, FSH / immunology*
  • Receptors, FSH / metabolism*
  • Recombinant Proteins / metabolism
  • Signal Transduction
  • Spodoptera / metabolism
  • Structure-Activity Relationship
  • Transfection

Substances

  • Epitopes
  • Immune Sera
  • Receptors, FSH
  • Recombinant Proteins
  • Follicle Stimulating Hormone
  • Alanine