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  5. Discovery and Development of the Quininib Series of Ocular Drugs
 
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Discovery and Development of the Quininib Series of Ocular Drugs

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Download Final Manuscript (Figs included).pdf404.69 KB
Author(s)
Mahon, Niamh 
Slater, Kayleigh 
O'Brien, Justine 
Alvarez, Yolanda 
Reynolds, Alison 
Kennedy, Breandán 
Uri
http://hdl.handle.net/10197/13046
Date Issued
28 January 2022
Date Available
09T07:57:46Z August 2022
Abstract
The quininib series is a novel collection of small-molecule drugs with antiangiogenic, antivascular permeability, anti-inflammatory, and antiproliferative activity. Quininib was initially identified as a drug hit during a random chemical library screen for determinants of developmental ocular angiogenesis in zebrafish. To enhance drug efficacy, novel quininib analogs were designed by applying medicinal chemistry approaches. The resulting quininib drug series has efficacy in in vitro and ex vivo models of angiogenesis utilizing human cell lines and tissues. In vivo, quininib drugs reduce pathological angiogenesis and retinal vascular permeability in rodent models. Quininib acts as a cysteinyl leukotriene (CysLT) receptor antagonist, revealing new roles of these G-protein-coupled receptors in developmental angiogenesis of the eye and unexpectedly in uveal melanoma (UM). The quininib series highlighted the potential of CysLT receptors as therapeutic targets for retinal vasculopathies (e.g., neovascular age-related macular degeneration, diabetic retinopathy, and diabetic macular edema) and ocular cancers (e.g., UM).
Sponsorship
Enterprise Ireland
European Commission Horizon 2020
Health Research Board
Irish Research Council
Science Foundation Ireland
Type of Material
Journal Article
Publisher
Mary Ann Liebert
Journal
Journal of Ocular Pharmacology and Therapeutics
Volume
38
Issue
1
Start Page
33
End Page
42
Copyright (Published Version)
2022 Mary Ann Liebert
Keywords
  • Quininib drug series

  • Ocular angiogenesis

  • Cysteinyl leukotriene...

  • Zebrafish

  • Phenotype-based drug ...

DOI
10.1089/jop.2021.0074
Language
English
Status of Item
Peer reviewed
ISSN
1557-7732
This item is made available under a Creative Commons License
https://creativecommons.org/licenses/by/3.0/ie/
Owning collection
Biomolecular and Biomedical Science Research Collection
Scopus© citations
0
Acquisition Date
Jan 28, 2023
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Jan 28, 2023
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