| Autor: |
Cross, Jasmine M., Coulson, Megan E., Smalley, Joshua P., Pytel, Wiktoria A., Ismail, Ozair, Trory, Justin S., Cowley, Shaun M., Hodgkinson, James T. |
| Zdroj: |
MedChemComm; 2022, Vol. 13 Issue: 12 p1634-1639, 6p |
| Abstrakt: |
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: |
Supplemental Index |
| Externí odkaz: |
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