Tripeptide growth hormone secretagogues.
A series of C-terminus capped dipeptides and tripeptides was synthesized as growth hormone (GH) secretagogues. Among them, tripeptide Aib-D-Trp-D-homoPhe-OEt showed low nanomolar activity in the rat pituitary assay. Thus, we have demonstrated that the GH secretagogue activity of the hexa-hepta-GH releasing peptides can be mimicked at the tripeptide level.
Yang
L
L
Department of Medicinal Chemistry, and Biochemistry & Physiology, Merck Research Laboratories, Rahway, NJ 07065, USA.
Morriello
G
G
Pan
Y
Y
Nargund
R P
RP
Barakat
K
K
Prendergast
K
K
Cheng
K
K
Chan
W W
WW
Smith
R G
RG
Patchett
A A
AA
D000595:Amino Acid Sequence; D000818:Animals; D004151:Dipeptides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013006:Growth Hormone / Q000378:metabolism*; D066298:In Vitro Techniques; D008958:Models, Molecular; D015394:Molecular Structure; D009842:Oligopeptides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D010902:Pituitary Gland / Q000378:metabolism; D051381:Rats; D013329:Structure-Activity Relationship
D004151:Dipeptides; D009842:Oligopeptides; C079956:alanyl-histidyl-(2-naphthyl)alanyl-tryptophyl-phenylalanyl-lysinamide; C041048:growth hormone releasing hexapeptide; D013006:Growth Hormone; C091874:growth hormone-releasing peptide-2