Jennifer Batson
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
Hamish D. Toop
Clara Redondo
ROYA BABAEI-JADIDI Roya.Babaei-jadidi@nottingham.ac.uk
Research Fellow
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 |
Files
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Copyright Statement
Copyright information regarding this work can be found at the following address: http://eprints.nottingham.ac.uk/end_user_agreement.pdf
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