Rotanova T V, Ivanova A G, Antonov V K, Rakadjieva A, Blagoev B
Int J Pept Protein Res. 1976;8(3):225-31.
The inhibitory effect of alkylboronic acids H(CH2)nB(OH)2(n=2-8) and Ph(CH2)n-B(OH)2, (n=0-4), on the alkaline mesentericopeptidase-catalysed hydrolysis of synthetic substrates was studied. It was shown that alkylboronic acids act as bifunctional reversible inhibitors. The borate group interacts with an ionogenic group of the enzyme with a pKa of about 6.9-7.0. The latter is probably the catalytically active imidazole of the active centre. The hydrocarbon part of the molecule also takes part in the formation of the enzyme-inhibitor complex. The dependence of the degree of the enzyme-inhibitor complex formation upon the length of the side-chain of the inhibitor indicates the presence of two binding sites on the enzyme molecule.
研究了烷基硼酸H(CH2)nB(OH)2（n = 2 - 8）和Ph(CH2)n - B(OH)2（n = 0 - 4）对碱性肠系膜肽酶催化合成底物水解的抑制作用。结果表明，烷基硼酸作为双功能可逆抑制剂。硼酸基团与酶的一个离子ogenic基团相互作用，其pKa约为6.9 - 7.0。后者可能是活性中心具有催化活性的咪唑。分子的烃基部分也参与酶 - 抑制剂复合物的形成。酶 - 抑制剂复合物形成程度对抑制剂侧链长度的依赖性表明酶分子上存在两个结合位点。
