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翻訳と辞書　辞書検索 [ 開発暫定版 ] スポンサード リンク Discovery and development of ACE inhibitors ： ウィキペディア英語版 Discovery and development of ACE inhibitors The discovery of an orally inactive peptide from snake venom established the important role of angiotensin converting enzyme (ACE) inhibitors in regulating blood pressure. This led to the development of Captopril, the first ACE inhibitor. When the adverse effects of Captopril became apparent new derivates were designed. Then after the discovery of two active sites of ACE: N-domain and C-domain, the development of domain-specific ACE inhibitors began. ==Development of first generation ACE inhibitors== The development of the nonapeptide teprotide (Glu-Trp-Pro-Arg-Pro-Gln-Ile-Pro-Pro), which was originally isolated from the venom of the Brazilian pit viper “Bothrops jararaca”, greatly clarified the importance of ACE in hypertension. However, its lack of oral activity limited its therapeutic utility. L-benzylsuccinic acid (2(R)-benzyl-3-carboxypropionic acid) was described to be the most potent inhibitor of carboxypeptidase A in the early 1980s. The authors referred to it as a by-product analog and it was proposed to bind to the active site of carboxypeptidase A via succinyl carboxyl group and a carbonyl group. Their findings established that L-benzylsuccinic acid is bound at a single locus at the active site of carboxypeptidase A. The authors discussed but dismissed the suggestion that the carboxylate function might bind to the catalytically functional zinc ion present at the active site. Later however this was found to be the case.〔 抄文引用元・出典: フリー百科事典『 ウィキペディア（Wikipedia）』 ■ウィキペディアで「Discovery and development of ACE inhibitors」の詳細全文を読む スポンサード リンク 翻訳と辞書 : 翻訳のためのインターネットリソース Copyright(C) kotoba.ne.jp 1997-2016. All Rights Reserved.