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Potent Inhibition of HIV‐1 Entry with a Chemically Programmed Antibody Aided by an Efficient Organocatalytic Synthesis
Author(s) -
Gavrilyuk Julia,
Uehara Hisatoshi,
Otsubo Nobumasa,
Hessell Ann,
Burton Dennis R.,
Barbas Carlos F.
Publication year - 2010
Publication title -
chembiochem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.05
H-Index - 126
eISSN - 1439-7633
pISSN - 1439-4227
DOI - 10.1002/cbic.201000432
Subject(s) - aldol reaction , aldolase a , organocatalysis , conjugate , human immunodeficiency virus (hiv) , antibody , chemistry , computer science , combinatorial chemistry , stereochemistry , computational biology , biochemistry , virology , biology , catalysis , enzyme , enantioselective synthesis , genetics , mathematical analysis , mathematics
An organocatalytic conspiracy: Organocatalysis and an organocatalytic antibody conspire to create a novel HIV‐1 entry inhibitor. A D ‐proline catalyzed aldol reaction was used to set the key stereochemistry of CCR5 inhibitor, Aplaviroc, prior to introduction as a targeting unit for chemical programming of aldolase antibody 38C2. The resulting antibody conjugate was a potent inhibitor of HIV‐1 and SIV entry.