Histone Deacetylase HDAC Inhibitors - Biotech, Pharma and Life Science Channel
Histone deacetylase (HDAC) inhibitors are emerging as a new class of potential anticancer agents for the treatment of solid and hematological malignancies. HDAC inhibition causes acetylated nuclear histones to accumulate in both tumor and normal tissues, providing a surrogate marker for the biological activity of HDAC inhibitors in vivo. The effects of HDAC inhibitors on gene expression are highly selective, leading to transcriptional activation of certain genes such as the cyclin-dependent kinase inhibitor but repression of others. HDAC inhibition not only results in acetylation of histones but also transcription factors such as p53, GATA-1 and estrogen receptor-alpha.
HDAC inhibitors are potent antiproliferative agents with relatively little effect on normal tissues. The first generation of pan-HDAC inhibitor produced clinical benefit and the first representative of this class is already marketed for cutaneous T-cell lymphoma. The second generation inhibitors are rationally designed with improved specificity and are currently in broad clinical evaluation for a number of different cancer indications, alone and in combination.
Apart from oncology, HDAC inhibitors are also being evaluated in other indications, such as Huntington’s disease or Friedreich’s ataxia because transcriptional dysregulation has been shown to be a major pathology in Huntington's Disease. There are CNS-penetrant, orally bioavailable HDAC inhibitors which are being pursued for use as a cognition enhancing agent in neurodegenerative diseases such as Alzheimer’s disease. Other indications under evaluation are fungal infections, psoriasis and inflammatory diseases.
Source; ReportLinker (Competitor Analysis: HDAC Inhibitors)
Add HDAC Inhibitors News Channel to your RSS reader;
News Articles
SAN DIEGO, June 18, 2013 /PRNewswire/ -- MEI Pharma, Inc. (Nasdaq: MEIP), an oncology company focused on the clinical development of novel therapies for cancer, announced today that the first patients...
-- Data Presented at the 18th Congress of the European Hematology Association -- Acetylon Pharmaceuticals Inc., the leader in development of selective histone deacetyla...
SEATTLE, June 17, 2013 /PRNewswire/ -- Cell Therapeutics, Inc. (CTI) (NASDAQ and MTA: CTIC) today announced results from a pooled analysis of data from completed Phase 1 and 2 studies of pacriti...
Enanta Pharmaceuticals to Present at the Wells Fargo Securities 2013 Healthcare Conference
Enanta Pharmaceuticals, Inc., (NASDAQ: ENTA), a research and development-focused biotechnology company dedicated to creating small molecule drugs in the infectious disease field,...
The European Medicines Agency’s Pharmacovigilance Risk Assessment Committee (PRAC) has concluded that the effects of the painkiller diclofenac on the heart and circulation when given systemically (b...
Acetylon Pharmaceuticals, Inc., the leader in development of selective histone deacetylase (HDAC) inhibitors for enhanced therapeutic outcomes, today announced that it will presen...
Epizyme Enrolls First Patient in Phase 1/2 Clinical Trial of EPZ-6438, an Inhibitor of EZH2
CAMBRIDGE, Mass., June 13, 2013 /PRNewswire/ -- Epizyme, Inc., (NASDAQ: EPZM) a clinical stage biopharmaceutical company creating innovative personalized therapeutics for patients with geneticall...
NORCROSS, Ga., June 12, 2013 /PRNewswire-USNewswire/ -- Galectin Therapeutics (NASDAQ: GALT), the leading developer of therapeutics that target galectin proteins to treat fibrosis and cancer, today an...
MEI Pharma Adds Former YM BioSciences CEO Nick Glover To Board Of Directors
SAN DIEGO, June 11, 2013 /PRNewswire/ -- MEI Pharma, Inc. (Nasdaq: MEIP), an oncology company focused on the clinical development of novel therapies for cancer, announced today the appointment of Nick...
rEVO Biologics, an LFB Company, announced today that it has completed the treatment and follow up phase of a key dose ranging study of LR769, a novel recombinant form of hu...
Events
Diabetes: Secondary Complications, Regulation and Innovation Conference
SMi is very proud to present our 11th conference focusing on Diabetes and metabolic disorders taking place on 1st and 2nd Oct 2013, London.
Companies
The Angeles Clinic and Research Institute
âThe Angeles Clinic and Research Instituteâs mission is to advance cancer care through groundbreaking research and delivering innovative therapeutic options to al...
DOV is a biopharmaceutical company historically focused on the development of novel product candidates for disorders of the central nervous system. DOV has previously funded drug development and disco...
Onconova, based in Newtown, PA and Lawrenceville, NJ, discovers and develops novel patent- protected small molecule therapeutic agents for cancer, radiation protection and hematol...
Enanta Phatmaceuticals ARE A RESEARCH AND DEVELOPMENT-FOCUSED BIOTECHNOLOGY COMPANY that uses its robust chemistry-driven approach and drug discovery capabilities to create small molecule drugs in t...
NeurAxon, Inc. (www.neuraxon.com) discovers and develops next-generation pain therapeutics focused on its first-in-class selective inhibitors of neuronal nitric oxide synthase...
Founded in 2001, AB Science is a pharmaceutical company specialising in the research, development and commercialisation of protein kinase inhibitors (PKIs), a new class of targete...
Sagene Pharmaceuticals is a biopharmaceutical company developing novel applications for combinations of FDA-approved drugs to treat diseases associated with aging. Sagene h...
Tensha Therapeutics is developing small molecule bromodomain inhibitors, a new class of epigenetic modulators of gene expression, to treat cancer and other serious disorders. The...
EnVivo Pharmaceuticals, Inc. and its subsidiaries (âEnVivo Pharmaceuticalsâ or âEnVivoâ) are dedicated to discovering and developing small molecule therapeutic...
Genkyotex is developing first in class, small molecule therapeutics that specifically and selectively inhibit the NOX family of enzymes. Using a unique screening platform, Genkyot...
Clinical Trials
The purpose of this research study is to: 1) Determine the highest dose of the drug vorinostat that can be given safely in combination with carboplatin and gemcitabine and 2) determine how...
Pilot Trial to Assess Effect of CNI Conversion of Efalizumab on T Reg Cells
The purpose of this pilot trial is to determine whether a conversion from calcineurin inhibitors (CNI) and mycophenolate mofetil (MMF) to a regimen consisting of efalizumab and sirolimus i...
89Zr-trastuzumab PET for Imaging the Effect of HSP90 Inhibition
HSP90 inhibition is a potentially new targeted drug modality in the treatment of HER2 positive, trastuzumab refractory breast cancer. Little is known about the pharmacodynamics of HSP90 in...
RATIONALE: Aromatase inhibitors, such as letrozole, prevent the formation of estradiol, a female hormone. Giving letrozole together with goserelin, leuprolide, or surgery may be an effecti...
Imatinib Mesylate in Combination With Docetaxel for Advanced, Platinum-Refractory Ovarian Cancer
Imatinib mesylate is an inhibitor of the receptor tyrosine kinases for platelet-derived growth factor (PDGF) and stem cell factor (SCF), c-Kit, and inhibits PDGF- and SCF-mediated cellular...
A Study Of Nasopharyngeal Carcinoma (NPC) Treated With Celecoxib And ZD1839
EGFR and COX-2 are involved in tumorigenesis, angiogenesis and metastases and are frequently over expressed in NPC.COX-2 and EGFR inhibitors are active in NPC.There is synergistic action b...
The Effects of Anabolic Steroids and Protease Inhibitors on People Living With HIV/AIDS
The main aim of the study is to investigate the combined effects of using anabolic steroids and protease inhibitors on fat metabolism and body composition of People Living with HIV/AIDS....
Statins in Proteinuric Nephropathies
End stage renal disease (ESRD) is rapidly growing worldwide. Patients with ESRD have increased morbidity and mortality mostly because of a dramatic excess of cardiovascular disease. Thus,...
Second Line Therapy for the Cure of Helicobacter Pylori (H. Pylori) Infection
Proton pump inhibitors (PPIs) are mainly metabolized in the liver by CYP2C19, one of the cytochrome P450 isoenzymes, which shows a genetic polymorphism associated with enzyme activities. T...
Celebrex With Preoperative Chemoradiation - Rectal Cancer
Colorectal carcinoma is the third most common cause of death from cancer. Approximately, 30% of colorectal carcinomas involve the rectum. Optimizing local control in the pelvis while reduc...
PubMed Articles
Epigenetics: a new mechanism of regulation of heart failure?
Heart failure is a syndrome resulting from a complex genetic predisposition and multiple environmental factors, and is a leading cause of morbidity and mortality. It is frequently accompanied by chang...
Elevated SGK1 predicts resistance of breast cancer cells to Akt inhibitors.
The majority of human cancers harbour mutations promoting activation of the Akt protein kinase, and Akt inhibitors are being evaluated in clinical trials. An important question concerns the understand...
Engagement of NKG2D and DNAX accessory molecule-1 (DNAM-1) receptors on lymphocytes plays an important role for anticancer response and represents an interesting therapeutic target for pharmacological...
Potent, reversible inhibition of the cytochrome P450 CYP2C9 isoform was observed in a series of urea-containing nicotinamide phosphoribosyltransferase (NAMPT) inhibitors. This unwanted property was su...
Role of macrophage receptor with collagenous structure in innate immune tolerance.
Macrophages play a key role in host defense against microbes, in part, through phagocytosis. Macrophage receptor with collagenous structure (MARCO) is a scavenger receptor on the cell surface of macro...
A novel series of indole/indazole-aminopyrimidines was designed and synthesized with an aim to achieve optimal potency and selectivity for the c-Jun kinase family or JNKs. Structure guided design was...
1-(1,3,5-Triazin-yl)piperidine-4-carboxamide inhibitors of soluble epoxide hydrolase were identified from high through-put screening using encoded library technology. The triazine heterocycle proved t...
Discovery of TAK-960: An orally available small molecule inhibitor of polo-like kinase 1 (PLK1).
Using structure-based drug design, we identified and optimized a novel series of pyrimidodiazepinone PLK1 inhibitors resulting in the selection of the development candidate TAK-960. TAK-960 is current...
Discovery of new potent inhibitors for carbonic anhydrase IX by structure-based virtual screening.
Through structure-based virtual screening, some dozen of benzene sulfonamides with novel scaffolds are identified as potent inhibitors against carbonic anhydrase (CA) IX with IC50 values ranging from...
The synthesis and structure-activity relationships of a novel aryl uracil series which contains a fused 5,6-bicyclic ring unit for HCV NS5B inhibition is described. Several analogs display replicon ce...
Videos
Histone deacetylases and histone deacetylase inhibitors - Video abstract: 29965
Video abstract of review paper "Histone deacetylase inhibitors (HDACIs): multitargeted anticancer agents" published in the open access journal Biologics: Tar...
Medical and Biotech [MESH] Definitions
Taxodium
A plant genus of the family TAXODIACEAE. Members contain taxodione and taxodone, which are diterpenoid quinone methide tumor inhibitors.
Huperzia
A plant genus of the family LYCOPODIACEAE. Members contain huperzine, one of the CHOLINESTERASE INHIBITORS.
Sirtuins
A homologous family of regulatory enzymes that are structurally related to the protein silent mating type information regulator 2 (Sir2) found in Saccharomyces cerevisiae. Sirtuins contain a central catalytic core region which binds NAD. Several of the sirtuins utilize NAD to deacetylate proteins such as HISTONES and are categorized as GROUP III HISTONE DEACETYLASES. Several other sirtuin members utilize NAD to transfer ADP-RIBOSE to proteins and are categorized as MONO ADP-RIBOSE TRANSFERASES, while a third group of sirtuins appears to have both deacetylase and ADP ribose transferase activities.
Silent Information Regulator Proteins, Saccharomyces Cerevisiae
A set of nuclear proteins in SACCHAROMYCES CEREVISIAE that are required for the transcriptional repression of the silent mating type loci. They mediate the formation of silenced CHROMATIN and repress both transcription and recombination at other loci as well. They are comprised of 4 non-homologous, interacting proteins, Sir1p, Sir2p, Sir3p, and Sir4p. Sir2p, an NAD-dependent HISTONE DEACETYLASE, is the founding member of the family of SIRTUINS.
Histone Code
The specific patterns of POST-TRANSLATIONAL PROTEIN MODIFICATION of HISTONES, i.e. histone ACETYLATION; METHYLATION; PHOSPHORYLATION; and ubiquitination, at specific amino acid residues, that are involved in assembly, maintenance, and modification of different chromatin structural states, such as EUCHROMATIN and HETEROCHROMATIN.
