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Bioorg Med Chem. 2020 Mar 16:115425. doi: 10.1016/j.bmc.2020.115425. [Epub ahead of print]

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.

Author information

1
Melior Discovery, Inc., 860 Springdale Drive, Exton, PA 19087, United States.
2
Melior Discovery, Inc., 860 Springdale Drive, Exton, PA 19087, United States. Electronic address: areaume@meliordiscovery.com.

Abstract

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.

KEYWORDS:

Allosteric modulators; Drug repurposing; Fragments; Insulin sensitizer; Phenotypic screen

PMID:
32201192
DOI:
10.1016/j.bmc.2020.115425
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Conflict of interest statement

Declaration of Competing Interest The authors declare the following financial interests/personal relationships which may be considered as potential competing interests: Andrew Reaume is an employee and shareholder of Melior Discovery, Inc and Melior Pharmaceuticals I, Inc which is developing MLR-1023 for profit. Chris Lipinski declares that he has no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.

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