Highly potent and specific inhibitors of human renin
摘要：
We have designed and synthesized a series of small peptides containing a perfluoroalkyl ketone group at the C-terminal position of the angiotensin I sequence as inhibitors of human renin. From this series of compounds, 8 and 10 showed strong inhibition of human renin (IC 50 = 3 × 10 9, 7 × 10 9 M, respectively). Compound 10 did not inhibit pepsin and cathepsin D at 10 4 M. Comparison of the IC 50 of compound 8 and compound 11 (8.7 × 10 7 M) demonstrated the marked effect of the perfluoropropyl group on the potency of inhibition on renin, presumably due to the strong electron-withdrawing effect causing the ketone in 8 to exist predominantly as the hydrate — thus mimicking the tetrahedral transition state during hydrolysis of the scissile Leu 10—Val 11 amide bond.
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DOI：
10.1016/0014-5793(87)80834-7
被引量：
年份：
1987
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