Histone deacetylase inhibitors (HDACi) comprise structurally diverse compounds that are a group of targeted anticancer agents. The first of these new HDACi, vorinostat (suberoylanilide hydroxamic acid), has received Food and Drug Administration approval for treating patients with cutaneous T-cell lymphoma. This review focuses on the activities of the 11 zinc-containing HDACs, their histone and ...

Histone deacetylase (HDAC) enzymes play a critical role in the epigenetic regulation of cellular functions and signaling pathways in many cancers. HDAC inhibitors (HDACi) have been validated for single use or in combination with other drugs in oncologic therapeutics. An even more novel combination therapy with HDACi is to use them with an oncolytic virus. HDACi may lead to an amplification of t...

We examined whether the multikinase inhibitor sorafenib and histone deacetylase inhibitors (HDACI) interact to kill pancreatic carcinoma cells and determined the impact of inhibiting BCL-2 family function on sorafenib and HDACI lethality. The lethality of sorafenib was enhanced in pancreatic tumor cells in a synergistic fashion by pharmacologically achievable concentrations of the HDACIs vorino...

Histone deacetylase inhibitors (HDACi) have received high interest as anticancer agents recently. HDACi may influence tumor growth by an inhibition of angiogenesis as well as by increasing tumor cell immunogenicity [1]. In many clinical trials the effect of several HDACi on different tumors are studied at the moment [2]. The purpose of this work has been to improve and validate an in vitro HDAC...

It has been found that the epigenetic silence of tumor suppressor genes induced by overexpression of histone deacetylases (HDACs) plays an important role in carcinogenesis. HDAC inhibitors (HDACi) that block the activity of specific HDACs have emerged as the accessory therapeutic agents for multiple human cancers. To better understand the effects of HDACi in cancer treatment, we carried out a r...

Histone deacetylase inhibitors (HDACi) were identified nearly four decades ago based on their ability to induce cellular differentiation. However, the clinical development of these compounds as cancer therapies has focused on their capacity to induce apoptosis in hematologic and lymphoid malignancies, often in combination with conventional cytotoxic agents. In many cases, HDACi doses necessary ...

Histone deacetylase inhibitors (HDACi) are a new group of anticancer drugs with tumor selective toxicity. Normal cells are relatively resistant to HDACi-induced cell death compared with cancer cells. Previously, we found that vorinostat induces DNA breaks in normal and transformed cells, which normal but not cancer cells can repair. In this study, we found that checkpoint kinase 1 (Chk1), a com...

THE RESULTS OBTAINED IN THE PRECEDING EXPERIMENTS MAY BE BRIEFLY SUMMARIZED AS FOLLOWS: 1. Nucleohiston does not protect against a separate and subcutaneous injection of tetanus toxin, diphtheria toxin, hog-cholera bacillus, or anthrax bacillus. 2. Mixtures of nucleohiston and either tetanus toxin or diphtheria toxin lose their specific toxic action-the latter much more rapidly than the former....

Histone deacetylase inhibitors (HDACi) and DNA methyltransferase inhibitors (DNMTi) are in early clinical development for multiple myeloma (MM) therapy. Despite all encouraging pre-clinical data, clinical activity of HDACi and DNMTi is mostly lacking. To optimize the trials, characterization of the in vivo response towards HDACi and DNMTi will be crucial. Therefore, we investigated the transcri...

BACKGROUND DNA topoisomerase II inhibitors and poisons are among the most efficacious drugs for the treatment of cancer. Sensitivity of cancer cells to the cytotoxic effects of topoisomerase II targeting agents is thought to depend on the expression of the topoisomerase IIalpha isoform, and drug resistance is often associated with loss or mutation of topoisomerase IIalpha. Histone deacetylase i...