| Autor: |
Jasmine M. Cross, Megan E. Coulson, Joshua P. Smalley, Wiktoria A. Pytel, Ozair Ismail, Justin S. Trory, Shaun M. Cowley, James T. Hodgkinson |
| Rok vydání: |
2022 |
| Předmět: |
|
| Zdroj: |
RSC medicinal chemistry. 13(12) |
| ISSN: |
2632-8682 |
| Popis: |
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 identified class I HDAC PROTACs highlighting the importance in the choice of HDAC ligand, functional group for linker attachment and positioning in PROTAC design. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
|
