非蛋白氨基酸和多肽对细菌胶原酶的影响

A. Sargsyan, Ani J. Karapetyan, L. Hayriyan, A. Hovhannisyan, M. Melkumyan, G. Oganezova, N. Avetisyan, N. Hovhannisyan
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引用次数: 0

摘要

细菌溶胶原蛋白酶由于其在全球氮循环中的重要作用和在某些疾病中的毒性作用而引起越来越多的关注。抑制这些酶是有吸引力的,因为它不直接攻击病原体,而是阻止梭菌对宿主的定植和浸润。光活性非蛋白α-氨基酸对溶组织梭菌胶原酶有抑制作用。基于结构的药物设计方法(建模)和确定氨基酸存在下酶活性的方法已被用于鉴定胶原酶的低分子量抑制剂。发现了抑制胶原酶活性的化合物,并估计了IC50值。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
THE INFLUENCE OF NON-PROTEIN AMINO ACIDS AND PEPTIDES ON BACTERIAL COLLAGENASE
Bacterial collagenolytic proteases have drawn increasing attention due to their essential role in the global nitrogen cycling and their virulent role in some diseases. The inhibition of these enzymes is attractive, as it does not attack the pathogen directly but rather blocks the colonization and infiltration of the host by the clostridia. Optically active non-protein α-amino acids have been screened for their ability to inhibit collagenase of Clostridium histolyticum. Both structure-based drug design approach (modeling) and that of determining enzyme activity in the presence of amino acids have been used to identify low molecular weight inhibitors of collagenase. The compounds able to inhibit collagenase activity have been revealed and IC50 values have been estimated.
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