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Active site targeting of hedgehog precursor protein with phenylarsine oxide.


ABSTRACT: 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.

SUBMITTER: Owen TS 

PROVIDER: S-EPMC4430098 | biostudies-literature | 2015 Jan

REPOSITORIES: biostudies-literature

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Active site targeting of hedgehog precursor protein with phenylarsine oxide.

Owen Timothy S TS   Xie Xie Jian XJ   Laraway Benjamin B   Ngoje George G   Wang Chunyu C   Callahan Brian P BP  

Chembiochem : a European journal of chemical biology 20141121 1


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. ...[more]

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