نتایج جستجو برای: hdac

تعداد نتایج: 4231  

2010
Alfonso Dueñas-Gonzalez Maria Teresa Vega Déborah Martinez-Baños Linda García-Hidalgo Pedro Sobrevilla

Histone deacetylase (HDAC) inhibitors have shown significant activity in the treatment of cutaneous T-cell lymphomas (CTCL). The epigenetic alterations of CTCL not only are limited to altered histone acetylation but also include aberrant DNA gene methylation hence, the combination of an HDAC inhibitor with a DNA demethylating agent is a promising therapy to be tested. Here we report a mycosis f...

2012
Guang Ping Cao Sundarapandian Thangapandian Shalini John Keun Woo Lee

Introduction: Histone deacetylases (HDAC) are a class of enzymes that remove acetyl groups from ε-N-acetyl lysine amino acids of histone proteins. Their action is opposite to that of histone acetyltransferase that adds acetyl groups to these lysines. Only few HDAC inhibitors are approved and used as anti-cancer therapeutics. Thus, discovery of new and potential HDAC inhibitors are necessary in ...

Journal: :Organic letters 2001
S M Sternson J C Wong C M Grozinger S L Schreiber

Seventy-two hundred potential inhibitors of the histone deacetylase (HDAC) enzyme family, based on a 1,3-dioxane diversity structure, were synthesized on polystyrene macrobeads. The compounds were arrayed for biological assays in a "one bead-one stock solution" format. Metal-chelating functional groups were used to direct the 1,3-dioxanes to HDAC enzymes, which are zinc hydrolases. Representati...

2016
Somy Yoon Gwang Hyeon Eom

Histone deacetylases (HDACs) are epigenetic regulators that regulate the histone tail, chromatin conformation, protein-DNA interaction, and even transcription. HDACs are also post-transcriptional modifiers that regulate the protein acetylation implicated in several pathophysiologic states. HDAC inhibitors have been highlighted as a novel category of anti-cancer drugs. To date, four HDAC inhibit...

Journal: :Experimental cell research 2009
Rose-Marie Catalioto Carlo Alberto Maggi Sandro Giuliani

The present study investigated the effect of HDAC inhibitors on the differentiation of human subcutaneous white adipocytes. Results showed that trichostatin A, suberoylanilide hydroxamic acid, valproic acid and MS-275 inhibited triglyceride accumulation, GPDH activity and FABP4 protein expression in adipocytes, as well as leptin and VEGF release, while cells retained a fibroblast-like morpholog...

Journal: :The Journal of pharmacology and experimental therapeutics 2016
Rink-Jan Lohman Abishek Iyer Thomas J Fairlie Adam Cotterell Praveer Gupta Robert C Reid David A Vesey Matthew J Sweet David P Fairlie

Vorinostat and other inhibitors of different histone deacetylase (HDAC) enzymes are currently being sought to modulate a variety of human conditions, including chronic inflammatory diseases. Some HDAC inhibitors are anti-inflammatory in rodent models of arthritis and colitis, usually at cytotoxic doses that may cause side effects. Here, we investigate the dose-dependent pro- and anti-inflammato...

2013
Usman Sumo Friend Tambunan Ridla Bakri Tirtana Prasetia Arli Aditya Parikesit Djati Kerami

Cervical cancer is second most common cancer in woman worldwide. Cervical cancer caused by human papillomavirus (HPV) oncogene. Inhibition of histone deacetylase (HDAC) activity has been known as a potential strategy for cancer therapy. SAHA is an HDAC inhibitor that has been used in cancer therapy but still has side effects. SAHA modification proposed to minimize side effects. Triazole attachm...

2011
Michele Cea Debora Soncini Floriana Fruscione Lizzia Raffaghello Anna Garuti Laura Emionite Eva Moran Mirko Magnone Gabriele Zoppoli Daniele Reverberi Irene Caffa Annalisa Salis Antonia Cagnetta Micaela Bergamaschi Salvatore Casciaro Ivana Pierri Gianluca Damonte Filippo Ansaldi Marco Gobbi Vito Pistoia Alberto Ballestrero Franco Patrone Santina Bruzzone Alessio Nencioni

Aberrant histone deacetylase (HDAC) activity is frequent in human leukemias. However, while classical, NAD(+)-independent HDACs are an established therapeutic target, the relevance of NAD(+)-dependent HDACs (sirtuins) in leukemia treatment remains unclear. Here, we assessed the antileukemic activity of sirtuin inhibitors and of the NAD(+)-lowering drug FK866, alone and in combination with tradi...

Journal: :Molecular and cellular biology 2007
Wei-Yi Chen Jui-Hsia Weng Chen-Che Huang Bon-Chu Chung

Histone deacetylase (HDAC) inhibitors such as trichostatin A and valproic acid modulate transcription of many genes by inhibiting the activities of HDACs, resulting in the remodeling of chromatin. Yet this effect is not universal for all genes. Here we show that HDAC inhibitors suppressed the expression of steroidogenic gene CYP11A1 and decreased steroid secretion by increasing the ubiquitinati...

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