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Histone deacetylase inhibitors: Anticancer compounds
The International Journal of Biochemistry & Cell Biology, 2009The reversible acetylation of proteins is mediated by histone acetyltransferases which acetylate proteins and histone deacetylases that remove the acetyl groups. High levels of histone acetylation are correlated with active genes, while hypoacetylation of histones corresponds with gene repression.
Karen T, Smith, Jerry L, Workman
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Histone deacetylase inhibitors in lymphoma
Current Opinion in Oncology, 2010Although many advances have been made in the treatment of lymphoma in the past decade, the treatment of patients with relapsed and refractory disease remains challenging. Only a fraction of patients will be cured with salvage therapy and transplantation.
Amanda, Copeland +2 more
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New patented histone deacetylase inhibitors
Expert Opinion on Therapeutic Patents, 2009Following FDA approval of vorinostat in 2006, several novel HDAC inhibitors (HDACis) have entered clinical trials, and there are numerous published patent applications claiming novel HDACis which were optimized as potential drug candidates, designed for regional or systemic release, and created as dual or multifunctional inhibitors.
Haishan, Wang, Brian W, Dymock
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Histone deacetylase inhibitors: gathering pace
Current Opinion in Pharmacology, 2006Reversible histone acetylation is one of the key mechanisms involved in the epigenetic control of gene expression. A variety of recent studies has revealed a role for acetylation in a much broader repertoire of physiological processes, including proliferation control and protein folding, and has highlighted how a variety of non-histone regulatory ...
Nessa, Carey, Nicholas B, La Thangue
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Anticancer activities of histone deacetylase inhibitors
Nature Reviews Drug Discovery, 2006Histone deacetylases (HDACs) are enzymes involved in the remodelling of chromatin, and have a key role in the epigenetic regulation of gene expression. In addition, the activity of non-histone proteins can be regulated through HDAC-mediated hypo-acetylation.
Jessica E, Bolden +2 more
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A cyclodextrin-capped histone deacetylase inhibitor
Bioorganic & Medicinal Chemistry Letters, 2013We have synthesized a β-cyclodextrin (βCD)-capped histone deacetylase (HDAC) inhibitor 3 containing an alkyl linker and a zinc-binding hydroxamic acid motif. Biological evaluation (HDAC inhibition studies) of 3 enabled us to establish the effect of replacing an aryl cap (in SAHA (vorinostat,)) 1 by a large saccharidic scaffold "cap".
Jahangir, Amin +7 more
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Histone Deacetylase Inhibitors in Psoriasis Therapy
Current Drug Target -Inflammation & Allergy, 2004Psoriasis is recognised as a multifactorial disease with inflammatory, proliferative, angiogenic and genetic components contributing to the pathology. The disease, which may vary in intensity, remains clinically unmet although there have been several recent advances that have had a substantial impact on suffering.
Fiona, McLaughlin +1 more
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Histone deacetylase inhibitors in cancer therapy
Expert Opinion on Investigational Drugs, 2007Histones are a family of nuclear proteins that interact with DNA, resulting in DNA being wrapped around a core of histone octamer within the nucleosome. Acetylation/deacetylation of histones is an important mechanism that regulates gene expression and chromatin remodeling.
Walid K, Rasheed +2 more
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Histone deacetylase inhibitors: novel anticancer agents
Expert Opinion on Investigational Drugs, 1999Previous studies have established that the regulation of gene expression is dependent upon the nucleosomal integrity of nuclear DNA. To a large extent, this integrity is dictated by the acetylation status of the core histone particles. The acetylation of histones is, in turn, controlled by the combined activity of specific acetylases and deacetylases ...
Saunders, Nicholas A. +5 more
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Novel Histone Deacetylase Inhibitors
2002Abstract : Advanced breast cancer is not curable by existing treatment regimens. The purpose of this project is to discover new drugs to treat breast cancer that act to restore the differentiated and non-growing state of breast tumor cells by inhibition of histone deacetylase.
Anna R. Martirosyan, Jeannine S. Strobl
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