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

Batson, Jennifer; Toop, Hamish D.; Redondo, Clara; Babaei-Jadidi, Roya; Chaikaud, Apirat; Wearmouth, Stephen F.; Gibbons, Brian; Allen, Claire; Tallant, Cynthia; Zhang, Jingxue; Du, Chunyun; Hancox, Jules C.; Hawtrey, Tom; Da Rocha, Joana; Griffith, Renate; Knapp, Stefan; Bates, David O.; Morris, Jonathan C.

Authors

Jennifer Batson

Hamish D. Toop

Clara Redondo

Apirat Chaikaud

Stephen F. Wearmouth

Brian Gibbons

Claire Allen

Cynthia Tallant

Jingxue Zhang

Chunyun Du

Jules C. Hancox

Tom Hawtrey

Joana Da Rocha

Renate Griffith

Stefan Knapp

DAVID BATES David.Bates@nottingham.ac.uk
Professor of Oncology

Jonathan C. Morris



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 helical insert of SRPK1, and trigger a backbone flip in the hinge region, that results in potent (

Citation

Batson, J., Toop, H. D., Redondo, C., Babaei-Jadidi, R., Chaikaud, A., Wearmouth, S. F., …Morris, J. C. (2017). Development of potent, selective SRPK1 inhibitors as potential topical therapeutics for neovascular eye disease. ACS Chemical Biology, 12(3), 825-832. https://doi.org/10.1021/acschembio.6b01048

Journal Article Type Article
Acceptance Date Jan 30, 2017
Online Publication Date Feb 6, 2017
Publication Date Mar 17, 2017
Deposit Date Jul 11, 2017
Publicly Available Date Mar 29, 2024
Journal ACS Chemical Biology
Print ISSN 1554-8929
Electronic ISSN 1554-8937
Publisher American Chemical Society
Peer Reviewed Peer Reviewed
Volume 12
Issue 3
Pages 825-832
DOI https://doi.org/10.1021/acschembio.6b01048
Public URL https://nottingham-repository.worktribe.com/output/838564
Publisher URL http://pubs.acs.org/doi/abs/10.1021/acschembio.6b01048

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