Dual-target EZH2 inhibitor: latest advances in medicinal chemistry.
Future Med Chem
; : 1-22, 2024 Jul 31.
Article
in En
| MEDLINE
| ID: mdl-39082677
ABSTRACT
Enhancer of zeste homolog 2 (EZH2), a histone methyltransferase, plays a crucial role in tumor progression by regulating gene expression. EZH2 inhibitors have emerged as promising anti-tumor agents due to their potential in cancer treatment strategies. However, single-target inhibitors often face limitations such as drug resistance and side effects. Dual-target inhibitors, exemplified by EZH1/2 inhibitor HH-2853(28), offer enhanced efficacy and reduced adverse effects. This review highlights recent advancements in dual inhibitors targeting EZH2 and other proteins like BRD4, PARP1, and EHMT2, emphasizing rational design, structure-activity relationships, and safety profiles, suggesting their potential in clinical applications.
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Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Language:
En
Journal:
Future Med Chem
Year:
2024
Document type:
Article
Affiliation country:
China