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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...

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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

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