Anchor-based design of improved cholera toxin and E. coli heat-labile enterotoxin receptor binding antagonists that display multiple binding modes.
Anchor-based design of improved cholera toxin and E. coli heat-labile enterotoxin receptor binding antagonists that display multiple binding modes.
复制标题
基于锚定的改进霍乱毒素和大肠杆菌不耐热肠毒素受体结合拮抗剂的设计，显示多种结合模式。
DOI：
10.1016/s1074-5521(02)00097-2
复制
发表时间：
2002
影响因子：
--
通讯作者：
Fan,Erkang
中科院分区：
文献类型：
--
作者：
Pickens,JasonC;Merritt,EthanA;Ahn,Misol;Verlinde,ChristopheLMJ;Hol,WimGJ;Fan,Erkang
The action of cholera toxin andE. coliheat-labile enterotoxin can be inhibited by blocking their binding to the cell-surface receptor GM1. We have used anchor-based design to create 15 receptor binding inhibitors that contain the previously characterized inhibitor MNPG as a substructure. In ELISA assays, all 15 compounds exhibited increased potency relative to MNPG. Binding affinities for two compounds, each containing a morpholine ring linked to MNPG via a hydrophobic tail, were characterized by pulsed ultrafiltration (PUF) and isothermal titration calorimetry (ITC). Crystal structures for these compounds bound to toxin B pentamer revealed a conserved binding mode for the MNPG moiety, with multiple binding modes adopted by the attached morpholine derivatives. The observed binding interactions can be exploited in the design of improved toxin binding inhibitors.
登录
查看更多内容
配体-大分子相互作用的脉冲超滤分析的进一步发展。
DOI：
--
发表时间：
1995
期刊：
影响因子：
--
作者：
Shen Chen
通讯作者：
Shen Chen
影响因子：
6.8
作者：
Fan, EK;Merritt, EA;Hol, WGJ
通讯作者：
Hol, WGJ
DOI：
--
发表时间：
1998
期刊：
影响因子：
--
作者：
C. Woodbury;D. Venton
通讯作者：
D. Venton
影响因子：
2.9
作者：
WISEMAN, T;WILLISTON, S;LIN, LN
通讯作者：
LIN, LN
影响因子：
7.4
作者：
Nikolic, D;Habibi-Goudarzi, S;van Breemen, RB
通讯作者：
van Breemen, RB