Fragment optimization and elaboration strategies – the discovery of two lead series of PRMT5/MTA inhibitors from five fragment hits

Here we describe the early stages of a fragment-based lead discovery (FBLD) project for a recently elucidated synthetic lethal target, the PRMT5/MTA complex, for the treatment of MTAP-deleted cancers. Starting with five fragment/PRMT5/MTA X-ray co-crystal structures, we employed a two-phase fragment...

Descripción completa

Detalles Bibliográficos
Autores principales: Smith, Christopher R., Kulyk, Svitlana, Ahmad, Misbha Ud Din, Arkhipova, Valentina, Christensen, James G., Gunn, Robin J., Ivetac, Anthony, Ketcham, John M., Kuehler, Jon, Lawson, J. David, Thomas, Nicole C., Wang, Xiaolun, Marx, Matthew A.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: RSC 2022
Materias:
Chemistry
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9749961/
https://www.ncbi.nlm.nih.gov/pubmed/36545438
http://dx.doi.org/10.1039/d2md00163b

Internet

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9749961/
https://www.ncbi.nlm.nih.gov/pubmed/36545438
http://dx.doi.org/10.1039/d2md00163b

Ejemplares similares