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Allosteric site on SHIP2 identified through fluorescent ligand screening and crystallography: a potential new target for intervention

Abstract:

Src homology 2 domain-containing inositol phosphate phosphatase 2 (SHIP2) is one of the 10 human inositol phosphate 5-phosphatases. One of its physiological functions is dephosphorylation of phosphatidylinositol 3,4,5-trisphosphate, PtdIns(3,4,5)P3. It is therefore a therapeutic target for pathophysiologies dependent on PtdIns(3,4,5)P3 and PtdIns(3,4)P2. Therapeutic interventions are limited by the dearth of crystallographic data describing ligand/inhibitor binding. An active site-directed fl...

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Publication status:
Published
Peer review status:
Peer reviewed

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Publisher copy:
10.1021/acs.jmedchem.0c01944

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MSD
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MSD
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Institution:
University of Oxford
Division:
MSD
Department:
Pharmacology
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MSD
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MSD
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Publisher:
American Chemical Society Publisher's website
Journal:
Journal of Medicinal Chemistry Journal website
Volume:
64
Issue:
7
Pages:
3813–3826
Publication date:
2021-03-16
Acceptance date:
2021-02-19
DOI:
EISSN:
1520-4804
ISSN:
0022-2623
Language:
English
Keywords:
Pubs id:
1162362
Local pid:
pubs:1162362
Deposit date:
2021-02-19

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