Reaction of porcine pancreatic elastase with 7-substituted 3-alkoxy-4-chloroisocoumarins: design of potent inhibitors using the crystal structure of the complex formed with 4-chloro-3-ethoxy-7-guanidinoisocoumarin.
Reaction of porcine pancreatic elastase with 7-substituted 3-alkoxy-4-chloroisocoumarins: design of potent inhibitors using the crystal structure of the complex formed with 4-chloro-3-ethoxy-7-guanidinoisocoumarin.
复制标题
猪胰腺弹性蛋白酶与 7-取代 3-烷氧基-4-氯异香豆素的反应：利用与 4-氯-3-乙氧基-7-胍基异香豆素形成的复合物的晶体结构设计有效的抑制剂。
DOI：
10.1021/bi00464a030
复制
发表时间：
1990
期刊：
影响因子：
2.9
通讯作者：
Kam,CM
中科院分区：
文献类型：
--
作者：
Powers,JC;Oleksyszyn,J;Narasimhan,SL;Kam,CM
Sigma Chemical Co., St. Louis, MO. Hepes was purchased from Research Organics Inc., Cleveland, OH, and Suc-Ala-Ala-Ala-NA was purchased from Peninsula Laboratories, Inc., Belmont, CA. The isocoumarins, 7-amino-4-chloro-3-methoxyisocoumarin (1), 7-amino-4-chloro-3-ethoxyisocoumarin (2; Harper & Powers, 1985), 4-chloro-7-guanidino-3-methoxyisocoumarin [H2NC (= NH2+)-MIC], and 4-chloro-3-ethoxy-7-guanidinoisocoumarin [H2N (C= NH2+)-EIC; Kam et al., 1988], were prepared as previously described. X-ray Structure. PPE (Serva) was crystallized without purification. A large (0.4 X 0.4 X 0.6 mm) crystal was mounted in a thin-walled capillary in the presence of excess solid 4-chloro-3-ethoxy-7-guanidinoisocoumarin and allowed to soak for 10 h at-1 C. Data collection was begun by using the rotation method with a Huber flat-plate camera, a crystal to film distance of 47 mm, and a temperature of-1 C.
