Kubota Eiji, Dean Rachel G, Balding Leanne C, Burrell Louise M
Department of Medicine, University of Melbourne, Austin, Australia.
Essays Biochem. 2002;38:129-39. doi: 10.1042/bse0380129.
The natriuretic peptide and renin-angiotensin systems are physiological counterparts with opposite roles in the regulation of electrolyte balance and blood pressure. In both systems, membrane-bound, zinc-dependent peptidases play an important role in the inactivation or activation of the system. Angiotensin-converting enzyme (ACE) converts angiotensin I into angiotensin II, and neutral endopeptidase (NEP) degrades the natriuretic peptides. Simultaneous inhibition NEP and ACE by a single molecule (a vasopeptidase inhibitor) is a new therapeutic approach in hypertension. Wider applications for vasopeptidase inhibitors being studied include their role as cardioprotective agents in heart failure, as renoprotective agents in chronic renal failure and diabetic nephropathy, and as vasculoprotective agents in endothelial dysfunction and athersclerosis.
利钠肽系统和肾素-血管紧张素系统是生理上的对应物，在调节电解质平衡和血压方面起着相反的作用。在这两个系统中，膜结合的、锌依赖性肽酶在系统的失活或激活中起重要作用。血管紧张素转换酶（ACE）将血管紧张素I转化为血管紧张素II，而中性内肽酶（NEP）降解利钠肽。通过单一分子同时抑制NEP和ACE（一种血管肽酶抑制剂）是治疗高血压的一种新方法。正在研究的血管肽酶抑制剂的更广泛应用包括其作为心力衰竭中的心脏保护剂、慢性肾衰竭和糖尿病肾病中的肾脏保护剂以及内皮功能障碍和动脉粥样硬化中的血管保护剂的作用。
