Parathyroid Hormone Senses Extracellular Calcium To Modulate Endocrine Signaling upon Binding to the Family B GPCR Parathyroid Hormone 1 Receptor

ACS Chem Biol. 2018 Aug 17;13(8):2347-2358. doi: 10.1021/acschembio.8b00568. Epub 2018 Jul 11.

Abstract

Parathyroid hormone (PTH) binds to a family B G protein coupled receptor, parathyroid hormone 1 receptor (PTH1R). One of its functions is to regulate Ca2+ homeostasis in bone remodeling, during which Ca2+ can reach up to 40 mM. A truncated version of PTH, PTH(1-34), can fully activate PTH1R and has been used for osteoporosis treatments. Here, we used fluorescence anisotropy to examine the binding of PTH(1-34) to PTH1R purified in nanodiscs (PTH1R-ND) and found that the affinity increases 5-fold in the presence of 15 mM Ca2+. However, PTHrP(1-36), another truncated endogenous agonist for PTH1R, does not show this Ca2+ effect. Mutations of Glu19 and Glu22 in PTH(1-34) that are not conserved in PTHrP(1-36) largely abolished the Ca2+ effect. The results support that PTH(1-34) not only activates PTH1R but also uniquely senses Ca2+. This dual function of a peptide hormone is a novel observation that couples changes in extracellular environment with endocrine signaling. Understanding this can potentially reveal the complex role of PTH signaling in bone remodeling and improve the PTH(1-34) treatment for osteoporosis.

Publication types

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

MeSH terms

  • Amino Acid Sequence
  • Calcium / metabolism*
  • Cyclic AMP
  • HEK293 Cells
  • Humans
  • Models, Molecular
  • Parathyroid Hormone / chemistry
  • Parathyroid Hormone / metabolism*
  • Protein Binding
  • Receptor, Parathyroid Hormone, Type 1 / metabolism*
  • Signal Transduction*

Substances

  • PTH1R protein, human
  • Parathyroid Hormone
  • Receptor, Parathyroid Hormone, Type 1
  • Cyclic AMP
  • Calcium