Irvine G B, Elmore D T
Biochem J. 1979 Nov 1;183(2):389-94. doi: 10.1042/bj1830389.
N-Diazoacetyl-L-phenylalanine 3-phenyl[2,3-3H]propylamide was synthesized and shown to inhibit pepsin A (EC3,4,23.1) and cathepsin D (EC 3.4.23.5) irreversibly and stoicheiometrically in the presence of Cu2+. Quantitative separation of the inhibited enzyme from excess reagent by gel filtration followed by measurement of the radioactivity of the protein peak provided a method for determining the operational molarity of these enzymes. Several other putative active-site-directed irreversible inhibitors were synthesized, but were inactive. Data on the synthesis of these compounds have been deposited as Supplementary Publication SUP50096 (4 pages) at the British Library Lending Division, Boston Spa, Wetherby, West Yorkshire LS23 7BQ, U.K., from whom copies can be obtained on the terms indicated in Biochem. J. (1978) 169, 5.
合成了N-重氮乙酰基-L-苯丙氨酸3-苯基[2,3-³H]丙酰胺,结果表明,在Cu²⁺存在的情况下,该化合物能不可逆地、化学计量地抑制胃蛋白酶A(EC3,4,23.1)和组织蛋白酶D(EC 3.4.23.5)。通过凝胶过滤将被抑制的酶与过量试剂定量分离,然后测量蛋白质峰的放射性,提供了一种测定这些酶活性摩尔浓度的方法。还合成了其他几种假定的活性位点导向不可逆抑制剂,但均无活性。这些化合物的合成数据已作为补充出版物SUP50096(共4页)存放在英国西约克郡韦瑟比市波士顿温泉村的英国国家图书馆出借部,其地址为LS23 7BQ,可按《生物化学杂志》(1978年)第169卷第5页所示条件从该处获取复印件。