Challenges in the Discovery and Optimization of mGlu(2/4) Heterodimer Positive Allosteric Modulators

BACKGROUND: This article describes the challenges in the discovery and optimization of mGlu2/4 heterodimer Positive Allosteric Modulators (PAMs). METHODS: Initial forays based on VU0155041, a PAM of both the mGlu4 homodimer and the mGlu2/4 heterodimer, led to flat, intractable SAR that precluded adv...

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Vydáno v:Lett Drug Des Discov
Hlavní autoři: Fulton, Mark Gallant, Loch, Matthew Thomas, Cuoco, Caroline Anne, Rodriguez, Alice Lambert, Days, Emily, Vinson, Paige Newton, Kozek, Krystian Andrezej, Weaver, Charles David, Blobaum, Anna Louise, Conn, Peter Jeffrey, Niswender, Colleen Marie, Lindsley, Craig William
Médium: Artigo
Jazyk:Inglês
Vydáno: Bentham Science Publishers 2019
Témata:
Letters in Drug Design & Discovery
On-line přístup:https://ncbi.nlm.nih.gov/pmc/articles/PMC7059629/
https://ncbi.nlm.nih.gov/pubmed/32201485
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.2174/1570180815666181017131349
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