Synthetic analogs of growth hormone-releasing factor with antagonistic activity in vitro.
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.
Sato
K
K
Department of Molecular Endocrinology, Whittier Institute for Diabetes and Endocrinology, La Jolla, CA 92037.
Hotta
M
M
Kageyama
J
J
Hu
H Y
HY
Dong
M H
MH
Ling
N
N
D000595:Amino Acid Sequence; D000818:Animals; D002478:Cells, Cultured; D013006:Growth Hormone / Q000037:antagonists & inhibitors / Q000378:metabolism; D013007:Growth Hormone-Releasing Hormone / Q000031:analogs & derivatives / Q000494:pharmacology*; D006801:Humans; D008969:Molecular Sequence Data; D010903:Pituitary Gland, Anterior / Q000166:cytology / Q000187:drug effects*; D051381:Rats
D013006:Growth Hormone; D013007:Growth Hormone-Releasing Hormone