Accueil > Publications > Recherche par années > Années 1990 > 1996

Coric, P ; Turcaud, S ; Meudal, H ; Roques, BP ; Fournie Zaluski, MC

Optimal recognition of neutral endopeptidase and angiotensin-converting enzyme active sites by mercaptoacyldipeptides as a means to design potent dual inhibitors

Journal of Medicinal Chemistry 39 (6) 1210-1219

par Administrateur - publié le , mis à jour le

Abstract :

An interesting approach for the treatment of congestive heart failure and chronic hypertension could be to avoid the formation of angiotensin II by inhibiting angiotensin converting enzyme (ACE) and to protect atrial natriuretic factor by blocking neutral endopeptidase 24.11 (NEP). This is support-ed by recent results obtained with potent dual inhibitors of the two zinc metallopeptidases, such as RE 105, HSCH2CH(CH3)PhCONHCH(CH3)COOH (Fournie-Zaluski et rrl. Proc, Natl. Acad. Sci. U.S.A, 1994, 91, 4072-4076), which reduces blood pressure in experimental models of hypertension, independently of the stilt and renin angiotensin system status.