Inhibition of angiotensin converting enzyme with Nα-phosphoryl-L-alanyl-L-proline and Nα-phosphoryl-L-valyl-L-tryptophan

Add time:08/02/2019    Source:sciencedirect.com

SummaryThe inhibition constants (Ki) and modes of inhibition have been determined for Nα-phosphoryl-L-alanyl-L-proline and Nα-phosphoryl-L-valyl-L-tryptophan against rabbit pulmonary angiotensin converting enzyme (dipeptidyl carboxpeptidase, E.C. 3.4.15.1). Phosphorylalanylproline and phosphorylvalyltryptophan are noncompeptitive inhibitors of the hydrolysis of hippuryl-L-histidyl-L-leucine in 100 mM phosphate buffer at pH 8.3 with Ki's of 9 nM and 51 nM respectively. In 50 mM Tris-hydrochloride buffer at pH 7.5, however, phosphorylalanylproline is a competitive inhibitor of the hydrolysis of hippuryl-L-histidyl-L-leucine with a Ki of 1.4 nM, and thus is one of the most potent inhibitors known for this enzyme.

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