Synthetic analogs of growth hormone-releasing factor with antagonistic activity in vitro

Biochem Biophys Res Commun. 1990 Feb 28;167(1):360-6. doi: 10.1016/0006-291x(90)91773-l.

Abstract

Analogs of human and rat growth hormone-releasing factor (hGRF and rGRF), related to [D-Arg2]hGRF(1-29)NH2, were synthesized by solid phase methodology. Their capacity to inhibit growth hormone secretion stimulated by hGRF(1-44)NH2 was tested on rat anterior pituitary cells in monolayer culture. Among the analogs of hGRF, [D-Arg2,29,Arg30]hGRF(1-30)NH2 showed the highest antagonistic potency of 3.64 relative to [D-Arg2]hGRF(1-29)NH2 = 1. However, the most potent analog synthesized thus far was [N-Ac-His1,D-Arg2,Ala15]rGRF(1-29)NH2, which showed a relative potency of 27.7.

Publication types

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

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Cells, Cultured
  • Growth Hormone / antagonists & inhibitors
  • Growth Hormone / metabolism
  • Growth Hormone-Releasing Hormone / analogs & derivatives
  • Growth Hormone-Releasing Hormone / pharmacology*
  • Humans
  • Molecular Sequence Data
  • Pituitary Gland, Anterior / cytology
  • Pituitary Gland, Anterior / drug effects*
  • Rats

Substances

  • Growth Hormone
  • Growth Hormone-Releasing Hormone