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Journal article

Development of potent, selective SRPK1 inhibitors as potential topical therapeutics for neovascular eye disease

Abstract:

Serine/arginine-protein kinase 1 (SRPK1) regulates alternative splicing of VEGF-A to pro-angiogenic isoforms and SRPK1 inhibition can restore the balance of pro/antiangiogenic isoforms to normal physiological levels. The lack of potency and selectivity of available compounds has limited development of SRPK1 inhibitors, with the control of alternative splicing by splicing factor-specific kinases yet to be translated. We present here compounds that occupy a binding pocket created by the unique ...

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Publication status:
Published
Peer review status:
Peer reviewed
Version:
Publisher's version

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Publisher copy:
10.1021/acschembio.6b01048

Authors


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ORCID:
0000-0003-4637-4764
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Institution:
University of Oxford
Division:
Medical Sciences Division
Department:
Oncology
Babaei-Jadidi, R More by this author
Chaikuad, A More by this author
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Exonate Ltd More from this funder
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Publisher:
American Chemical Society Publisher's website
Journal:
ACS Chemical Biology Journal website
Volume:
12
Issue:
3
Pages:
825-832
Publication date:
2017-01-30
Acceptance date:
2017-01-30
DOI:
EISSN:
1554-8937
ISSN:
1554-8929
Pubs id:
pubs:679106
URN:
uri:a5da418c-3a92-4789-8ab0-0f9412424a3d
UUID:
uuid:a5da418c-3a92-4789-8ab0-0f9412424a3d
Local pid:
pubs:679106

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