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Design of a Protein Surface Antagonist Based on α ‐Helix Mimicry: Inhibition of gp41 Assembly and Viral Fusion
Author(s) -
Ernst Justin T.,
Kutzki Olaf,
Debnath Asim K.,
Jiang Shibo,
Lu Hong,
Hamilton Andrew D.
Publication year - 2002
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/1521-3773(20020118)41:2<278::aid-anie278>3.0.co;2-a
Subject(s) - mimicry , schematic , gp41 , molecular mimicry , antagonist , representation (politics) , theme (computing) , computer science , chemistry , world wide web , biology , engineering , biochemistry , political science , genetics , zoology , antibody , receptor , electronic engineering , epitope , politics , law
Low micromolar inhibition of HIV‐1 fusion into host cells has been achieved by using a small molecule antagonist for the disruption of the gp41 core that was designed by mimicry of the α ‐helical 4‐3 hydrophobic repeat regions (see schematic representation).