Synthesis, structure and biological activity of alpha-trifluoromethyl-substituted thyreotropin releasing hormone

被引：11
|
作者：
Koksch, B [1 ]
Ullmann, D [1 ]
Jakubke, HD [1 ]
Burger, K [1 ]
机构：
[1] UNIV LEIPZIG,DEPT ORGAN CHEM,D-04103 LEIPZIG,GERMANY
来源：
JOURNAL OF FLUORINE CHEMISTRY | 1996年 / 80卷 / 01期
关键词：
alpha-trifluoromethyl-substituted amino acids; TRH; proteolytic stability; NMR spectroscopy; IR spectroscopy;
D O I：
10.1016/S0022-1139(96)03461-6
中图分类号：
O61 [无机化学];
学科分类号：
070301 ; 081704 ;
摘要：
The incorporation of alpha-trifluoromethyl pyroglutamic acid into thyreotropin releasing hormone TRH, results in the complete stability of the pGlu-His bond against proteolytic degradation by pyroglutamyl aminopeptidase II. The influence of the trifluoromethyl group on structure and receptor affinity has been studied.
引用
收藏
页码：53 / 57
页数：5
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