Advances in anti-tumor research of HDAC inhibitors and combination with PI3K inhibitors
10.16438/j.0513-4870.2022-0672
- VernacularTitle:HDAC抑制剂及其联合PI3K抑制剂抗肿瘤研究进展
- Author:
Lei HUANG
;
Xiao-guang CHEN
;
Fang-fang LAI
- Publication Type:Research Article
- Keywords:
HDAC inhibitor;
PI3K inhibitor;
combination therapy;
HDAC/PI3K dual-target inhibitor;
anti-tumor
- From:
Acta Pharmaceutica Sinica
2022;57(12):3557-3563
- CountryChina
- Language:Chinese
-
Abstract:
Histone deacetylase (HDAC) is usually abnormally overexpressed, which mainly leads to the transcriptional repression of tumor suppressor genes. Histone deacetylase inhibitors (HDIs) exert anti-tumor biological effects by regulating nucleosome structure, inhibiting HDAC activity, and controlling the expression of tumor suppressor genes. There are currently 5 drugs on the market, but only for peripheral T-cell lymphoma and cutaneous T-cell lymphoma. In solid tumors, most of the HDAC inhibitors used have failed to achieve effective therapeutic effects. Phosphoinositide 3-kinase (PI3K) is the starting node of the PI3K-AKT-mTOR signaling pathway, which plays a very important role in the proliferation, migration, invasion, and differentiation of tumor cells. The abnormal activation of PI3K is closely related to the occurrence and development of tumors, and the combined use of HDAC and PI3K inhibitors and HDAC/PI3K dual-target inhibitors show synergistic anticancer activity. This article introduces the anti-tumor clinical and preclinical research progress of representative HDAC inhibitors and PI3K inhibitors, as well as HDAC/PI3K dual-target inhibitors.
