A NONPEPTIDYL GROWTH-HORMONE SECRETAGOGUE

A NONPEPTIDYL GROWTH-HORMONE SECRETAGOGUE
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DOI:
10.1126/science.8503009
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发表时间:
1993-06-11
期刊:
影响因子:
56.9
通讯作者:
FISHER, MH
FISHER, MH
中科院分区:
综合性期刊1区
文献类型:
--
作者:
SMITH, RG;CHENG, K;FISHER, MH

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已鉴定出一种生长激素的非肽基促分泌素,其结构为3-氨基-3-甲基-N-(2,3,4,5-四氢-2-氧代-1-{[2 ′-(1H-四唑-5-基)(1,1 ′-联苯基)-4-基]甲基}-1H-1-苯并氮杂卓-3(R)-基)-丁酰胺(L-692,429)。L-692,429与天然生长激素促分泌素生长激素释放激素协同作用,并通过替代信号转导途径发挥作用。L-692,429的作用机制以及肽基和非肽基拮抗剂的研究表明,该分子是生长激素释放六肽His-D-Trp-Ala-Trp-D-Phe-Lys-NH 2(GHRP-6)的模拟物。L-692,429是生长激素的非肽基特异性促分泌素的实例。
A nonpeptidyl secretagogue for growth hormone of the structure 3-amino-3-methyl-N-(2,3,4,5-tetrahydro-2-oxo-1-{[2'-(1H-tetrazol-5-yl)(1,1'-biphenyl)-4-yl]methy1}-1H-1-benzazepin-3(R)-yl)-butanamide (L-692,429) has been identified. L-692,429 synergizes with the natural growth hormone secretagogue growth hormone-releasing hormone and acts through an alternative signal transduction pathway. The mechanism of action of L-692,429 and studies with peptidyl and nonpeptidyl antagonists suggest that this molecule is a mimic of the growth hormone-releasing hexapeptide His-D-Trp-Ala-Trp-D-Phe-Lys-NH2 (GHRP-6). L-692,429 is an example of a nonpeptidyl specific secretagogue for growth hormone.