BLIP-II Is a Highly Potent Inhibitor of Klebsiella pneumoniae Carbapenemase (KPC-2)
BLIP-II Is a Highly Potent Inhibitor of Klebsiella pneumoniae Carbapenemase (KPC-2)
复制标题
DOI：
10.1128/aac.00215-13
复制
发表时间：
2013-07-01
影响因子：
4.9
通讯作者：
Palzkill, Timothy
中科院分区：
文献类型：
--
作者：
Brown, Nicholas G.;Chow, Dar-Chone;Palzkill, Timothy
β-内酰胺酶抑制蛋白II(BLIP-II)是一种有效的A类β-内酰胺酶抑制剂。KPC-2是一种能够水解碳青霉烯类抗生素的A类β-内酰胺酶，已成为革兰氏阴性菌广泛耐药的来源。BLIP-II和KPC-2结合的结合和解离速率常数的测定表明，与计算的(k(OFF)/k(ON))平衡解离常数76fM(76×10(-15)M)有非常紧密的相互作用。
beta-Lactamase inhibitory protein II (BLIP-II) is a potent inhibitor of class A beta-lactamases. KPC-2 is a class A beta-lactamase that is capable of hydrolyzing carbapenems and has become a widespread source of resistance to these drugs for Gram-negative bacteria. Determination of association and dissociation rate constants for binding between BLIP-II and KPC-2 reveals a very tight interaction with a calculated (k(off)/k(on)) equilibrium dissociation constant of 76 fM (76 x 10(-15) M).