A ‘click’ chemistry approach to novel entinostat (MS-275) based class I histone deacetylase proteolysis targeting chimeras

Click chemistry was utilised to prepare a library of PROTACs based on entinostat a class I histone deacetylase (HDAC) inhibitor in clinical trials. A novel PROTAC JMC-137 was identified as a HDAC1/2 and HDAC3 degrader in HCT116 cells. However, potency was compromised compared to previously identifie...

Descripción completa

Detalles Bibliográficos
Autores principales: Cross, Jasmine M., Coulson, Megan E., Smalley, Joshua P., Pytel, Wiktoria A., Ismail, Ozair, Trory, Justin S., Cowley, Shaun M., Hodgkinson, James T.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: RSC 2022
Materias:
Chemistry
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9749924/
https://www.ncbi.nlm.nih.gov/pubmed/36545434
http://dx.doi.org/10.1039/d2md00199c

Internet

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9749924/
https://www.ncbi.nlm.nih.gov/pubmed/36545434
http://dx.doi.org/10.1039/d2md00199c

Ejemplares similares