三肽生长激素促分泌素

Tripeptide growth hormone secretagogues.

作者信息

Yang L, Morriello G, Pan Y, Nargund R P, Barakat K, Prendergast K, Cheng K, Chan W W, Smith R G, Patchett A A

机构信息

Department of Medicinal Chemistry, and Biochemistry & Physiology, Merck Research Laboratories, Rahway, NJ 07065, USA.

出版信息

Bioorg Med Chem Lett. 1998 Apr 7;8(7):759-64. doi: 10.1016/s0960-894x(98)00103-6.

DOI:10.1016/s0960-894x(98)00103-6

PMID:9871537

Abstract

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.

摘要

合成了一系列C端封端的二肽和三肽作为生长激素（GH）促分泌素。其中，三肽Aib-D-色氨酸-D-高苯丙氨酸乙酯在大鼠垂体试验中显示出低纳摩尔活性。因此，我们已经证明，六肽至七肽生长激素释放肽的GH促分泌素活性可以在三肽水平上模拟。