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促黄体生成素释放激素(LH-RH)受体结构要求的最小空间差异研究

Minimal steric difference study of structural requirements for the luteinizing hormone-releasing hormone (LH-RH) receptor.

作者信息

Simon Z, Vlad A, Ciureanu M, Motoc I, Holban S

出版信息

Pol J Pharmacol Pharm. 1980 Mar-Apr;32(2):179-85.

PMID:6256722
Abstract

Quantitative structure-activity relation for amino acid substitution analogues of the LH-RH decapeptide were established by means of the receptor site mapping procedure based upon minimal steric differences. For a series of 17 analogues of LH-RH, obtained by substitutions of the C-terminal Gly-NH2 residue, a corelation coefficient r = 0.93 was obtained, for a series of 7 analogues, obtained by substitutions of the Leu7 residue, r = 0.95 was obtained. The shape of the LH-RH receptor regions interacting with the C-terminal of the decapetide and with the Leu7-side chain is inferred from this study.

摘要

基于最小空间差异的受体位点映射程序,建立了促黄体生成激素释放激素(LH-RH)十肽氨基酸取代类似物的定量构效关系。对于通过C末端甘氨酰胺(Gly-NH2)残基取代获得的一系列17种LH-RH类似物,相关系数r = 0.93;对于通过亮氨酸7(Leu7)残基取代获得的一系列7种类似物,r = 0.95。从本研究中推断出与十肽C末端和Leu7侧链相互作用的LH-RH受体区域的形状。

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