Head D L, Yankeelov J A
Int J Pept Protein Res. 1976;8(2):155-65. doi: 10.1111/j.1399-3011.1976.tb02491.x.
The enzymatic behavior and inhibition patterns of collagenase of Clostridium histolyticum in the presence of 0.5 M and 3.4 mM CaCl2 have been examined viscosimetrically. The more concentrated salt was found to enhance the rate of digestion of calfskin collagen when either measured viscosimetrically or colorimetrically by trinitrobenzenesulfonate. However, the rate of digestion of calfskin gelatin is unaffected by 0.5 M CaCl2 as determined colorimetrically. Calcium chloride also proved to have a marked effect on the inhibitory behavior of a series of imidazole compounds. Histidine (10mM) is about three-fold more effective as an inhibitor in 0.5 M CaCl2 than in 3.4 mM CaCl2, whereas a reverse effect is true for histamine, Imidazolylpropionate (10mM) was only weakly inhibitory (16%) in 0.5 M CaCl2 and not at all in 3.4 mM CaCl2. Inhibition by 10 mM imidazole was not detectable. These observations may be useful in the design of inhibitors for tissue collagenases which share a number of common characteristics with the bacterial enzyme.
已通过粘度测定法研究了溶组织梭菌胶原酶在存在0.5 M和3.4 mM氯化钙时的酶促行为和抑制模式。当通过粘度测定法或用三硝基苯磺酸盐进行比色法测量时,发现浓度更高的盐会提高小牛皮胶原蛋白的消化速率。然而,通过比色法测定,0.5 M氯化钙对小牛皮明胶的消化速率没有影响。氯化钙还被证明对一系列咪唑化合物的抑制行为有显著影响。组氨酸(10 mM)在0.5 M氯化钙中作为抑制剂的效果比在3.4 mM氯化钙中约高三倍,而组胺则相反。咪唑基丙酸(10 mM)在0.5 M氯化钙中仅具有微弱的抑制作用(16%),在3.4 mM氯化钙中则完全没有抑制作用。10 mM咪唑的抑制作用无法检测到。这些观察结果可能有助于设计与细菌酶具有许多共同特征的组织胶原酶抑制剂。