Synthetic human parathyroid hormone-like protein stimulates bone resorption and causes hypercalcemia in rats

J Clin Invest. 1988 Feb;81(2):596-600. doi: 10.1172/JCI113358.

Abstract

Parathyroid hormone-like adenylate cyclase-stimulating proteins (hACSPs) have been implicated as one of the calcemic, bone-resorbing agents in patients with humoral hypercalcemia of malignancy. We report the synthesis of an amino-terminal hACSP fragment, Tyr36 hACSP (1-36) amide. The synthetic hACSP is a potent agonist of renal membrane adenylate cyclase (Km, 1.7 X 10(-10)) and of bone cell adenylate cyclase (Km 1 X 10(-9)M). It is a potent bone-resorbing agent in vitro, stimulating 45Ca release from fetal rat long bones at a concentration of 10(-9) M. When infused via osmotic minipumps into rats, it is also a potent calcemic factor in vivo, inducing a rise in serum calcium from (mean +/- SD) 10.6 +/- 0.6 to 19.7 +/- 3.2 mg/dl when infused at 1.4 micrograms/h and from 9.9 +/- 0.7 to 11.4 +/- 1.2 mg/dl when infused at 0.14 micrograms/h. These findings indicate that biologically active hACSP fragments can be synthesized. One such synthetic peptide possesses the in vitro and in vivo bioactivities demonstrated in native, tumor-derived hACSPs. It is also a potent calcemic, bone-resorbing agent.

Publication types

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

MeSH terms

  • Adenylyl Cyclases / metabolism
  • Amino Acid Sequence
  • Base Sequence
  • Bone Resorption / drug effects*
  • Cloning, Molecular
  • Enzyme Activation / drug effects
  • Humans
  • Hypercalcemia / chemically induced*
  • Molecular Sequence Data
  • Neoplasm Proteins / genetics
  • Neoplasm Proteins / pharmacology*
  • Parathyroid Hormone / pharmacology
  • Recombinant Proteins / pharmacology

Substances

  • Neoplasm Proteins
  • Parathyroid Hormone
  • Recombinant Proteins
  • parathyroid hormone-like adenylate cyclase-stimulating protein, human
  • Adenylyl Cyclases