Novel histone deacetylase inhibitors in clinical trials as anti-cancer agents

被引:349
作者
Tan, Jiahuai [2 ]
Cang, Shundong [3 ]
Ma, Yuehua [1 ]
Petrillo, Richard L. [2 ]
Liu, Delong [1 ]
机构
[1] New York Med Coll, Div Hematol Oncol, Valhalla, NY 10595 USA
[2] Mt Vernon Hosp, Dept Med, Mt Vernon, NY 10550 USA
[3] Henan Prov Peoples Hosp, Dept Oncol, Zhengzhou, Peoples R China
关键词
TRANS-RETINOIC ACID; CHRONIC LYMPHOCYTIC-LEUKEMIA; REFRACTORY SOLID TUMORS; ACUTE MYELOID-LEUKEMIA; ACTIVITY IN-VITRO; VALPROIC ACID; PHASE-I; HDAC INHIBITOR; BELINOSTAT PXD101; EPIGENETIC MODIFICATIONS;
D O I
10.1186/1756-8722-3-5
中图分类号
R73 [肿瘤学];
学科分类号
100214 ;
摘要
Histone deacetylases (HDACs) can regulate expression of tumor suppressor genes and activities of transcriptional factors involved in both cancer initiation and progression through alteration of either DNA or the structural components of chromatin. Recently, the role of gene repression through modulation such as acetylation in cancer patients has been clinically validated with several inhibitors of HDACs. One of the HDAC inhibitors, vorinostat, has been approved by FDA for treating cutaneous T-cell lymphoma (CTCL) for patients with progressive, persistent, or recurrent disease on or following two systemic therapies. Other inhibitors, for example, FK228, PXD101, PCI-24781, ITF2357, MGCD0103, MS-275, valproic acid and LBH589 have also demonstrated therapeutic potential as monotherapy or combination with other anti-tumor drugs in CTCL and other malignancies. At least 80 clinical trials are underway, testing more than eleven different HDAC inhibitory agents including both hematological and solid malignancies. This review focuses on recent development in clinical trials testing HDAC inhibitors as anti-tumor agents.
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页数:13
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