High throughput in vivo phenotypic screening for drug repurposing: Discovery of MLR-1023 a novel insulin sensitizer and novel Lyn kinase activator with clinical proof of concept

[Display omitted] Drug discovery requires the combination of medicinal chemistry and biology. In this article Chris Lipinski, the medicinal chemist, describes the chemical origins at Pfizer of Tolimidone1 the starting point for the repurposed MLR-1023 (Ochman et al., 2012). Andrew Reaume, the biolog...

Full description

Saved in:
Bibliographic Details
Published in:Bioorganic & medicinal chemistry 2020-05, Vol.28 (9), p.115425-115425, Article 115425
Main Authors: Lipinski, Christopher A., Reaume, Andrew G.
Format: Article
Language:English
Subjects:
Allosteric modulators
Drug repurposing
Fragments
Insulin sensitizer
Phenotypic screen
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:[Display omitted] Drug discovery requires the combination of medicinal chemistry and biology. In this article Chris Lipinski, the medicinal chemist, describes the chemical origins at Pfizer of Tolimidone1 the starting point for the repurposed MLR-1023 (Ochman et al., 2012). Andrew Reaume, the biologist, describes his motivation to develop a high quality (i.e. in vivo model) phenotypic screening platform as an ideal drug repositioning platform.
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2020.115425