PRMT5 is a therapeutic target in choroidal neovascularization.


Journal

Scientific reports
ISSN: 2045-2322
Titre abrégé: Sci Rep
Pays: England
ID NLM: 101563288

Informations de publication

Date de publication:
31 01 2023
Historique:
received: 15 07 2022
accepted: 16 01 2023
entrez: 31 1 2023
pubmed: 1 2 2023
medline: 3 2 2023
Statut: epublish

Résumé

Ocular neovascular diseases including neovascular age-related macular degeneration (nvAMD) are widespread causes of blindness. Patients' non-responsiveness to currently used biologics that target vascular endothelial growth factor (VEGF) poses an unmet need for novel therapies. Here, we identify protein arginine methyltransferase 5 (PRMT5) as a novel therapeutic target for nvAMD. PRMT5 is a well-known epigenetic enzyme. We previously showed that PRMT5 methylates and activates a proangiogenic and proinflammatory transcription factor, the nuclear factor kappa B (NF-κB), which has a master role in tumor progression, notably in pancreatic ductal adenocarcinoma and colorectal cancer. We identified a potent and specific small molecule inhibitor of PRMT5, PR5-LL-CM01, that dampens the methylation and activation of NF-κB. Here for the first time, we assessed the antiangiogenic activity of PR5-LL-CM01 in ocular cells. Immunostaining of human nvAMD sections revealed that PRMT5 is highly expressed in the retinal pigment epithelium (RPE)/choroid where neovascularization occurs, while mouse eyes with laser induced choroidal neovascularization (L-CNV) showed PRMT5 is overexpressed in the retinal ganglion cell layer and in the RPE/choroid. Importantly, inhibition of PRMT5 by PR5-LL-CM01 or shRNA knockdown of PRMT5 in human retinal endothelial cells (HRECs) and induced pluripotent stem cell (iPSC)-derived choroidal endothelial cells (iCEC2) reduced NF-κB activity and the expression of its target genes, such as tumor necrosis factor α (TNF-α) and VEGF-A. In addition to inhibiting angiogenic properties of proliferation and tube formation, PR5-LL-CM01 blocked cell cycle progression at G

Identifiants

pubmed: 36720900
doi: 10.1038/s41598-023-28215-w
pii: 10.1038/s41598-023-28215-w
pmc: PMC9889383
doi:

Substances chimiques

Vascular Endothelial Growth Factor A 0
PR5-LL-CM01 0
NF-kappa B 0
PRMT5 protein, human EC 2.1.1.319
Protein-Arginine N-Methyltransferases EC 2.1.1.319

Types de publication

Journal Article Research Support, N.I.H., Extramural Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

1747

Subventions

Organisme : NCATS NIH HHS
ID : UL1TR002529
Pays : United States
Organisme : NCATS NIH HHS
ID : UL1 TR002529
Pays : United States
Organisme : NEI NIH HHS
ID : R01EY025641
Pays : United States
Organisme : NEI NIH HHS
ID : R01 EY025641
Pays : United States
Organisme : NEI NIH HHS
ID : R01 EY031939
Pays : United States

Informations de copyright

© 2023. The Author(s).

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Auteurs

Anbukkarasi Muniyandi (A)

Department of Ophthalmology, Eugene and Marilyn Glick Eye Institute, Indiana University School of Medicine, Indianapolis, IN, 46202, USA.

Matthew Martin (M)

Department of Pharmacology & Toxicology, Indiana University School of Medicine, Indianapolis, IN, 46202, USA.

Kamakshi Sishtla (K)

Department of Ophthalmology, Eugene and Marilyn Glick Eye Institute, Indiana University School of Medicine, Indianapolis, IN, 46202, USA.

Aishat Motolani (A)

Department of Pharmacology & Toxicology, Indiana University School of Medicine, Indianapolis, IN, 46202, USA.

Mengyao Sun (M)

Department of Pharmacology & Toxicology, Indiana University School of Medicine, Indianapolis, IN, 46202, USA.

Nathan R Jensen (NR)

Department of Ophthalmology, Eugene and Marilyn Glick Eye Institute, Indiana University School of Medicine, Indianapolis, IN, 46202, USA.

Xiaoping Qi (X)

Department of Ophthalmology and Visual Sciences, University of Alabama at Birmingham, Birmingham, AL, 35233, USA.

Michael E Boulton (ME)

Department of Ophthalmology and Visual Sciences, University of Alabama at Birmingham, Birmingham, AL, 35233, USA.

Lakshmi Prabhu (L)

Department of Pharmacology & Toxicology, Indiana University School of Medicine, Indianapolis, IN, 46202, USA.

Tao Lu (T)

Department of Pharmacology & Toxicology, Indiana University School of Medicine, Indianapolis, IN, 46202, USA. lut@iu.edu.
Department of Biochemistry & Molecular Biology, Indiana University School of Medicine, Indianapolis, IN, 46202, USA. lut@iu.edu.
Department of Medical & Molecular Genetics, Indiana University School of Medicine, Indianapolis, IN, 46202, USA. lut@iu.edu.

Timothy W Corson (TW)

Department of Ophthalmology, Eugene and Marilyn Glick Eye Institute, Indiana University School of Medicine, Indianapolis, IN, 46202, USA. tcorson@iu.edu.
Department of Pharmacology & Toxicology, Indiana University School of Medicine, Indianapolis, IN, 46202, USA. tcorson@iu.edu.
Department of Biochemistry & Molecular Biology, Indiana University School of Medicine, Indianapolis, IN, 46202, USA. tcorson@iu.edu.

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