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Photochemical probe identification of a small-molecule inhibitor binding site in Hedgehog acyltransferase (HHAT)

Abstract:

The mammalian membrane-bound O-acyltransferase (MBOAT) superfamily is involved in biological processes including growth, development and appetite sensing. MBOATs are attractive drug targets in cancer and obesity; however, information on the binding site and molecular mechanisms underlying small-molecule inhibition is elusive. This study reports rational development of a photochemical probe to interrogate a novel small-molecule inhibitor binding site in the human MBOAT Hedgehog acyltransferase...

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Publication status:
Published
Peer review status:
Peer reviewed

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Publisher copy:
10.1002/anie.202014457

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Institution:
University of Oxford
Division:
MSD
Sub department:
Pharmacology
Role:
Author
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Publisher:
Wiley Publisher's website
Journal:
Angewandte Chemie International Edition Journal website
Volume:
60
Issue:
24
Pages:
13542-13547
Publication date:
2021-03-26
Acceptance date:
2021-03-02
DOI:
EISSN:
1521-3773
ISSN:
1433-7851
Language:
English
Keywords:
Pubs id:
1169262
Local pid:
pubs:1169262
Deposit date:
2021-03-24

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