Active site targeting of hedgehog precursor protein with phenylarsine oxide

Timothy S. Owen; Xie Jian Xie; Benjamin Laraway; George Ngoje; Chunyu Wang; Brian P. Callahan

doi:10.1002/cbic.201402421

Active site targeting of hedgehog precursor protein with phenylarsine oxide

Timothy S. Owen
, Xie Jian Xie
, Benjamin Laraway
, George Ngoje
, Chunyu Wang
, Brian P. Callahan

Chemistry

Binghamton University

Research output: Contribution to journal › Article › peer-review

14 Scopus citations

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 K_i, 4×10^-7M) 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.

Original language	English
Pages (from-to)	55-58
Number of pages	4
Journal	ChemBioChem
Volume	16
Issue number	1
DOIs	https://doi.org/10.1002/cbic.201402421
State	Published - Jan 2 2015

Keywords

Active-site probe
Arsenic
Autoprocessing
Cholesterol
Hedgehog

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10.1002/cbic.201402421

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title = "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 (PhAsIII). The interaction (apparent Ki, 4×10-7M) is characterized by an optical binding assay and by NMR spectroscopy. PhAsIII appears to be the first validated inhibitor of hedgehog autoprocessing, which is unique to hedgehog proteins and essential for biological activity.",

keywords = "Active-site probe, Arsenic, Autoprocessing, Cholesterol, Hedgehog",

author = "Owen, \{Timothy S.\} and Xie, \{Xie Jian\} and Benjamin Laraway and George Ngoje and Chunyu Wang and Callahan, \{Brian P.\}",

note = "Publisher Copyright: {\textcopyright} 2015 Wiley-VCH Verlag GmbH \& Co. KGaA, Weinheim.",

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AU - Owen, Timothy S.

AU - Xie, Xie Jian

AU - Laraway, Benjamin

AU - Ngoje, George

AU - Wang, Chunyu

AU - Callahan, Brian P.

PY - 2015/1/2

Y1 - 2015/1/2

N2 - 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 (PhAsIII). The interaction (apparent Ki, 4×10-7M) is characterized by an optical binding assay and by NMR spectroscopy. PhAsIII appears to be the first validated inhibitor of hedgehog autoprocessing, which is unique to hedgehog proteins and essential for biological activity.

AB - 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 (PhAsIII). The interaction (apparent Ki, 4×10-7M) is characterized by an optical binding assay and by NMR spectroscopy. PhAsIII appears to be the first validated inhibitor of hedgehog autoprocessing, which is unique to hedgehog proteins and essential for biological activity.

KW - Active-site probe

KW - Arsenic

KW - Autoprocessing

KW - Cholesterol

KW - Hedgehog

UR - https://www.scopus.com/pages/publications/84919724819

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DO - 10.1002/cbic.201402421

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SP - 55

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JO - ChemBioChem

JF - ChemBioChem

IS - 1

ER -

Active site targeting of hedgehog precursor protein with phenylarsine oxide

Abstract

Keywords

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