An entropically efficient supramolecular inhibition strategy for Shiga toxins

被引:25
作者
Kitov, Pavel I. [1 ]
Lipinski, Tomasz [1 ]
Paszkiewicz, Eugenia [1 ]
Solomon, Dmitry [1 ]
Sadowska, Joanna M. [1 ]
Grant, Gordon A. [1 ]
Mulvey, George L. [2 ]
Kitova, Elena N. [1 ]
Klassen, John S. [1 ]
Armstrong, Glen D. [2 ]
Bundle, David R. [1 ]
机构
[1] Univ Alberta, Dept Chem, Edmonton, AB T6G 2G2, Canada
[2] Univ Calgary, Dept Microbiol & Infect Dis, Calgary, AB T2N 4N1, Canada
关键词
aggregation; biological activity; drug design inhibitors; supramolecular chemistry;
D O I
10.1002/anie.200704064
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
(Figure Presented) A compact heterobifunctional ligand devoid of a linker between binding functionalities induces a supramolecular assembly between two pentameric proteins, Shiga toxin (blue) and serum amyloid P component, a human serum protein (turquoise). The use of an endogenous protein as a template brings about a 10 000-fold enhancement of ligand activity. © 2008 Wiley-VCH Verlag GmbH & Co. KGaA.
引用
收藏
页码:672 / 676
页数:5
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