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Active Site Targeting of Hedgehog Precursor Protein with Phenylarsine Oxide
Author(s) -
Owen Timothy S.,
Xie Xie Jian,
Laraway Benjamin,
Ngoje George,
Wang Chunyu,
Callahan Brian P.
Publication year - 2015
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.201402421
Subject(s) - phenylarsine oxide , hedgehog , chemistry , stereochemistry , small molecule , molecule , biochemistry , receptor , signal transduction , organic chemistry
Hedgehog proteins, signaling molecules implicated in human embryo development and cancer, can be inhibited at the stage of autoprocessing by the trivalent arsenical phenyl arsine oxide (PhAs III ). The interaction (apparent K i , 4×10 −7 M ) is characterized by an optical binding assay and by NMR spectroscopy. PhAs III appears to be the first validated inhibitor of hedgehog autoprocessing, which is unique to hedgehog proteins and essential for biological activity.