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[血管紧张素转换酶肽抑制剂的构象受限类似物的合成与分析]

[Synthesis and analysis of conformationally restricted analogs of peptide inhibitors of the angiotensin-converting enzyme].

作者信息

Filatova M P, Krit N A, Komarova O M, Orekhovich V N, Reissmann S

出版信息

Bioorg Khim. 1986 Jan;12(1):59-70.

PMID:3004512
Abstract

To investigate conformations of peptide inhibitors of the angiotensin-converting enzyme in the enzyme-inhibitor complex, the synthesis, studies of inhibitory activity, and conformational calculations of analogues of bradykinin-potentiating peptides with N-methylalanine or D-alanine in place of L-proline or L-alanine residues have been carried out. All the analogues showed a sharp decrease of inhibitory activity in comparison with the natural peptides, that might be considered as an indirect confirmation of the earlier proposed "conformation of inhibition" of the above-mentioned peptides.

摘要

为了研究血管紧张素转换酶 - 抑制剂复合物中肽类抑制剂的构象,已开展了缓激肽增强肽类似物的合成、抑制活性研究以及构象计算,这些类似物用N - 甲基丙氨酸或D - 丙氨酸取代了L - 脯氨酸或L - 丙氨酸残基。与天然肽相比,所有类似物的抑制活性均急剧下降,这可被视为对上述肽类“抑制构象”的早期提议的间接证实。

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