نتایج جستجو برای: suberoylanilide hydroxamic acid saha

تعداد نتایج: 748959  

Journal: :Molecules 2018
Kristina King Alexander-Thomas Hauser Jelena Melesina Wolfgang Sippl Manfred Jung

We designed and synthesized carbamates of the clinically-approved HDAC (histone deacetylase) inhibitor vorinostat (suberoylanilide hydroxamic acid, SAHA) in order to validate our previously-proposed hypothesis that these carbamates might serve as prodrugs for hydroxamic acid containing HDAC inhibitors. Biochemical assays proved our new compounds to be potent inhibitors of histone deacetylases i...

Journal: :The Journal of biological chemistry 2011
Basar Cenik Chantelle F Sephton Colleen M Dewey Xunde Xian Shuguang Wei Kimberley Yu Wenze Niu Giovanni Coppola Sarah E Coughlin Suzee E Lee Daniel R Dries Sandra Almeida Daniel H Geschwind Fen-Biao Gao Bruce L Miller Robert V Farese Bruce A Posner Gang Yu Joachim Herz

Progranulin (GRN) haploinsufficiency is a frequent cause of familial frontotemporal dementia, a currently untreatable progressive neurodegenerative disease. By chemical library screening, we identified suberoylanilide hydroxamic acid (SAHA), a Food and Drug Administration-approved histone deacetylase inhibitor, as an enhancer of GRN expression. SAHA dose-dependently increased GRN mRNA and prote...

2011
Yasuo NAGAOKA Manami KUBO Haruka YAMASAKU Yuta ISHII Hiroko OKITA Hiroki NAKANO Shinichi UESATO Yoshie MAITANI

that have been identified as a promising target to reverse aberrant epigenetic states associated with cancer via the regulation of acetylation levels in histone. Aberrant histone acetylation has been observed in the development of numerous malignancies, and HDAC inhibitors (HDACIs) are a promising new treatment strategy for malignant disease. The hydroxamic acid trichostatin A (TSA) have been k...

Journal: :Chemical research in toxicology 2017
Mariangela Librizzi Fabio Caradonna Ilenia Cruciata Janusz Dębski Supojjanee Sansook Michał Dadlez John Spencer Claudio Luparello

Jay Amin hydroxamic acid (JAHA; N8-ferrocenylN1-hydroxy-octanediamide) is a ferrocene-containing analogue of the histone deacetylase inhibitor (HDACi) suberoylanilide hydroxamic acid (SAHA). JAHA's cytotoxic activity on MDA-MB231 triple negative breast cancer (TNBC) cells at 72 h has been previously demonstrated with an IC50 of 8.45 μM. JAHA's lethal effect was found linked to perturbations of ...

2013
Xufeng Chen Eric H. Radany Patty Wong Shenglin Ma Kan Wu Bing Wang Jeffrey Y. C. Wong

Histone deacetylase inhibitors (HDIs) have shown promise as candidate radiosensitizer for many types of cancers. However, the mechanisms of action are not well understood, and whether they could have clinical impact on radiotherapy for leukemia is unclear. In this study, we demonstrate that suberoylanilide hydroxamic acid (SAHA) can increase radiosensitivity of acute myeloid leukemia (AML) cell...

2007
Julie Horion Geoffrey Gloire Nadia El Mjiyad Vincent Quivy Linda Vermeulen Wim Vanden Berghe Guy Haegeman Carine Van Lint Jacques Piette Yvette Habraken

Abbreviations: ALLN, N-acetylleucylleucylnorleucinal; ChIP, chromatin immunoprecipitation; EMSA, electrophoretic mobility shift assay; ERK1/2, extracellular signal-regulated kinase 1/2; HAT, histone acetyltransferase; HDAC, histone deacetylase; HIV LTR, HIV long terminal repeat; H2O2, hydrogen peroxide; IKK, IκB kinase; MAPK, mitogen-activated protein kinase; MSK1, mitogenand stress-activated p...

Journal: :Blood 2003
Nicholas Mitsiades Constantine S Mitsiades Paul G Richardson Ciaran McMullan Vassiliki Poulaki Galinos Fanourakis Robert Schlossman Dharminder Chauhan Nikhil C Munshi Teru Hideshima Victoria M Richon Paul A Marks Kenneth C Anderson

Histone acetylation modulates gene expression, cellular differentiation, and survival and is regulated by the opposing activities of histone acetyltransferases (HATs) and histone deacetylases (HDACs). HDAC inhibition results in accumulation of acetylated nucleosomal histones and induces differentiation and/or apoptosis in transformed cells. In this study, we characterized the effect of suberoyl...

Journal: :Chemistry & biology 2003
Kathryn M Koeller Stephen J Haggarty Brian D Perkins Igor Leykin Jason C Wong Ming-Chih J Kao Stuart L Schreiber

Histone deacetylase (HDAC) inhibitors are being developed as new clinical agents in cancer therapy, in part because they interrupt cell cycle progression in transformed cell lines. To examine cell cycle arrest induced by HDAC inhibitor trichostatin A (TSA), a cytoblot cell-based screen was used to identify small molecule suppressors of this process. TSA suppressors (ITSAs) counteract TSA-induce...

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