Mazumder B, Sikdar R, Sen P C
Department of Chemistry, Bose Institute, Calcutta.
Indian J Biochem Biophys. 1991 Apr;28(2):136-9.
The microsomal membranes isolated from rat testes have been found to contain a Mg(2+)-dependent and a Mg(2+)-independent Ca(2+)-ATPase. The enzyme activities were inhibited by two contraceptive drugs--gossypol and chlorpromazine. The inhibition by the former was affected by the presence of ligand(s) and not the substrate in the incubation medium, whereas ligand(s)/substrate did not affect the inhibition by chlorpromazine. This may be explained from the fact that the binding of chlorpromazine and ligand(s)/substrate to the enzyme are independent of each other whereas in case of gossypol the ligand(s) compete with the drug at the binding site of the enzyme.
已发现从大鼠睾丸分离出的微粒体膜含有一种Mg(2+)依赖性和一种Mg(2+)非依赖性Ca(2+) -ATP酶。两种避孕药棉酚和氯丙嗪可抑制该酶的活性。前者的抑制作用受孵育介质中配体而非底物的存在影响,而配体/底物不影响氯丙嗪的抑制作用。这可以从以下事实来解释:氯丙嗪与配体/底物与酶的结合相互独立,而在棉酚的情况下,配体在酶的结合位点与药物竞争。