Histone deacetylase inhibitors as novel anticancer therapeutics
نویسندگان
چکیده
Histone deacetylase inhibitors represent a promising new class of compounds for the treatment of cancer. Inhibitors of this kind currently under clinical evaluation mainly target the classical (Rpd3/Hda1) family of histone deacetylases. Of particular note, the U.S. Food and Drug Administration recently approved the first histone deacetylase inhibitor (Zolinza: Merck and Co., Whitehouse Station, NJ, U.S.A.) for the treatment of cutaneous T-cell lymphoma. Dozens of such inhibitors are now in phase ii-iii clinical trials, sometimes in combination with other chemotherapy drugs, for diverse cancer types, including both hematologic and solid tumours. In this mini-review, we provide an overview of the histone deacetylase superfamily, highlight the positive results of deacetylase inhibitors in cancer clinical trials, and comment on the prospects for the next generation of such inhibitors.
منابع مشابه
Search for the Pharmacophore of Histone Deacetylase Inhibitors Using Pharmacophore Query and Docking Study
Histone deacetylase inhibitors have gained a great deal of attention recently for the treatment of cancers and inflammatory diseases. So design of new inhibitors is of great importance in pharmaceutical industries and labs. Creating pharmacophor models in order to design new molecules or search a library for finding lead compounds is of great interest. This approach reduces the overall cost ass...
متن کاملSearch for the Pharmacophore of Histone Deacetylase Inhibitors Using Pharmacophore Query and Docking Study
Histone deacetylase inhibitors have gained a great deal of attention recently for the treatment of cancers and inflammatory diseases. So design of new inhibitors is of great importance in pharmaceutical industries and labs. Creating pharmacophor models in order to design new molecules or search a library for finding lead compounds is of great interest. This approach reduces the overall cost ass...
متن کاملHistone tail modifications and noncanonical functions of histones: perspectives in cancer epigenetics.
Over the past few years, the histone deacetylase (HDAC) inhibitors have occupied an important place in the effort to develop novel, but less toxic, anticancer therapy. HDAC inhibitors block HDACs, which are the enzymes responsible for histone deacetylation, and therefore they modulate gene expression. The cellular effects of HDAC inhibitors include growth arrest and the induction of differentia...
متن کاملTranscriptional induction of GRP78/BiP by histone deacetylase inhibitors and resistance to histone deacetylase inhibitor-induced apoptosis.
Histone deacetylase (HDAC) inhibitors are emerging as effective therapies in the treatment of cancer, and the role of HDACs in the regulation of promoters is rapidly expanding. GRP78/BiP is a stress inducible endoplasmic reticulum (ER) chaperone with antiapoptotic properties. We present here the mechanism for repression of the Grp78 promoter by HDAC1. Our studies reveal that HDAC inhibitors spe...
متن کاملNovel N-hydroxybenzamide histone deacetylase inhibitors as potential anti-cancer agents.
Histone deacetylases (HDACs) are a class of Zn(2+) dependent metalloproteases that play an important role in tumorigenesis. Inhibition of HDACs may be a potential strategy for cancer therapy. This study designed and synthesized a series of novel N-hydroxybenzamide histone deacetylase inhibitors based on the structural features of suberoylanilide hydroxamic acid (SAHA), the first HDAC inhibitor ...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
عنوان ژورنال:
- Current Oncology
دوره 15 شماره
صفحات -
تاریخ انتشار 2008