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A Metal‐Based Inhibitor of Tumor Necrosis Factor‐α
Author(s) -
Leung ChungHang,
Zhong HaiJing,
Yang Hui,
Cheng Zhen,
Chan Daniel ShiuHin,
Ma Victor PuiYan,
Abagyan Ruben,
Wong ChunYuen,
Ma DikLung
Publication year - 2012
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/anie.201202937
Subject(s) - iridium , trimer , tumor necrosis factor alpha , enantiomer , in vitro , interface (matter) , chemistry , computational biology , cancer research , information retrieval , computer science , combinatorial chemistry , stereochemistry , molecule , biochemistry , dimer , medicine , biology , organic chemistry , catalysis , gibbs isotherm
Staying in the pocket : A cyclometalated iridium(III) biquinoline complex targets the protein–protein interface (see picture; C yellow, N blue, Ir dark green) of the tumor necrosis factor‐α (TNF‐α) trimer. Molecular‐modeling studies confirm the nature of this interaction. Both enantiomers of the iridium complex display comparable in vitro potency to the strongest small‐molecule inhibitor of TNF‐α.