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Molecules 2015, 20(3), 3898-3941; doi:10.3390/molecules20033898

Histone Deacetylase Inhibitors in Clinical Studies as Templates for New Anticancer Agents

RCMI Cancer Research Center, Xavier University of Louisiana, New Orleans, LA 70125, USA
Department of Chemistry, Xavier University of Louisiana, New Orleans, LA 70125, USA
College of Pharmacy, Xavier University of Louisiana, New Orleans, LA 70125, USA
Authors to whom correspondence should be addressed.
Academic Editor: Jean Jacques Vanden Eynde
Received: 26 December 2014 / Revised: 13 February 2015 / Accepted: 15 February 2015 / Published: 2 March 2015
View Full-Text   |   Download PDF [1114 KB, uploaded 2 March 2015]   |  


Histone dacetylases (HDACs) are a group of enzymes that remove acetyl groups from histones and regulate expression of tumor suppressor genes. They are implicated in many human diseases, especially cancer, making them a promising therapeutic target for treatment of the latter by developing a wide variety of inhibitors. HDAC inhibitors interfere with HDAC activity and regulate biological events, such as cell cycle, differentiation and apoptosis in cancer cells. As a result, HDAC inhibitor-based therapies have gained much attention for cancer treatment. To date, the FDA has approved three HDAC inhibitors for cutaneous/peripheral T-cell lymphoma and many more HDAC inhibitors are in different stages of clinical development for the treatment of hematological malignancies as well as solid tumors. In the intensifying efforts to discover new, hopefully more therapeutically efficacious HDAC inhibitors, molecular modeling-based rational drug design has played an important role in identifying potential inhibitors that vary in molecular structures and properties. In this review, we summarize four major structural classes of HDAC inhibitors that are in clinical trials and different computer modeling tools available for their structural modifications as a guide to discover additional HDAC inhibitors with greater therapeutic utility. View Full-Text
Keywords: HDAC inhibitors; cancer; molecular modeling; clinical trials HDAC inhibitors; cancer; molecular modeling; clinical trials

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Mottamal, M.; Zheng, S.; Huang, T.L.; Wang, G. Histone Deacetylase Inhibitors in Clinical Studies as Templates for New Anticancer Agents. Molecules 2015, 20, 3898-3941.

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