Mapping of a carboxyl-terminal active site of parathyroid hormone by calcium-imaging

Cell Calcium. 1998 Jun;23(6):413-21. doi: 10.1016/s0143-4160(98)90098-7.

Abstract

We recently showed that the C-terminal fragment PTH (52-84) effectively increases intracellular free calcium ([Ca2+]i) in a subset of growth plate chondrocytes not activated by the N-terminal PTH fragment (1-34). Here we characterize the active site on C-terminal PTH (52-84) with respect to calcium (Ca2+)-signaling and the mechanism involved by using synthetic PTH-subfragments in digital CCD ratio-imaging experiments. Our results show amino acids 73-76 to be the core region for increasing [Ca2+]i. Ryanodine (1 microM), caffeine (10 mM), lithium (2 mM), or cyclopiazonic acid (2-5 microM), agents that interfere with intracellular Ca2+ release, all failed to block PTH (52-84) induced [Ca2+]i increases. Depletion of extracellular calcium ([Ca2+]o) blocked PTH (52-84) induced [Ca2+]i increases, indicating a transmembrane Ca2+ influx. In contrast to voltage-gated and Ca2+ release activated Ca2+ influx, PTH (52-84) evoked Ca2+ influx was not blocked by nickel (1 mM). We conclude that PTH amino acids 73-76 are essential for activation of a nickel-insensitive Ca2+ influx pathway in growth plate chondrocytes that is likely to be of relevance for matrix calcification, a key step in endochondral bone formation.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Binding Sites
  • Bradykinin / pharmacology
  • Caffeine / pharmacology
  • Cartilage / embryology
  • Cartilage / metabolism
  • Chondrocytes / metabolism*
  • Egtazic Acid / pharmacology
  • Humans
  • Image Processing, Computer-Assisted
  • Lithium / pharmacology
  • Models, Biological
  • Parathyroid Hormone / metabolism*
  • Protein Sorting Signals / metabolism
  • Ryanodine / pharmacology
  • Thapsigargin / pharmacology
  • Time Factors

Substances

  • Parathyroid Hormone
  • Protein Sorting Signals
  • Ryanodine
  • Caffeine
  • Egtazic Acid
  • Thapsigargin
  • Lithium
  • Bradykinin