Active site targeting of hedgehog precursor protein with phenylarsine oxide.

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 Ki , 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. © 2015 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

Citation

Timothy S Owen, Xie Jian Xie, Benjamin Laraway, George Ngoje, Chunyu Wang, Brian P Callahan. Active site targeting of hedgehog precursor protein with phenylarsine oxide. Chembiochem : a European journal of chemical biology. 2015 Jan 2;16(1):55-8

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PMID: 25418613

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