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...

Descripción completa

Detalles Bibliográficos
Autores principales: 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
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Bentham Science Publishers 2019
Materias:
Letters in Drug Design & Discovery
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7059629/
https://www.ncbi.nlm.nih.gov/pubmed/32201485
http://dx.doi.org/10.2174/1570180815666181017131349

Internet

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7059629/
https://www.ncbi.nlm.nih.gov/pubmed/32201485
http://dx.doi.org/10.2174/1570180815666181017131349

Ejemplares similares