Clinical development of histone deacetylase inhibitors as anticancer agents

DC Drummond, CO Noble, DB Kirpotin… - Annu. Rev …, 2005 - annualreviews.org
▪ Abstract Acetylation is a key posttranslational modification of many proteins responsible for
regulating critical intracellular pathways. Although histones are the most thoroughly studied …

Histone deacetylase inhibitors

C Monneret - European journal of medicinal chemistry, 2005 - Elsevier
Histones are small basic proteins that, by complexing wtih DNA, form the nucleosome core.
Repetitive units of this nucleosome led to the chromatin in which all the human genome is …

Inhibition of histone deacetylase 6 acetylates and disrupts the chaperone function of heat shock protein 90: a novel basis for antileukemia activity of histone …

P Bali, M Pranpat, J Bradner, M Balasis… - Journal of Biological …, 2005 - ASBMB
The hydroxamic acid (HAA) analogue pan-histone deacetylase (HDAC) inhibitors (HDIs)
LAQ824 and LBH589 have been shown to induce acetylation and inhibit the ATP binding …

[图书][B] Anticancer agents from natural products

GM Cragg, DGI Kingston, DJ Newman - 2005 - taylorfrancis.com
Plants, marine organisms, and microorganisms have evolved complex chemical defense
and signaling systems that are designed to protect them from predators and provide other …

Histone deacetylase inhibitors: discovery and development as anticancer agents

PA Marks, M Dokmanovic - Expert opinion on investigational drugs, 2005 - Taylor & Francis
Histone deacetylase (HDAC) inhibitors are a new class of targeted anticancer agents.
Several HDAC inhibitors are in clinical trials and have shown significant activity against a …

Epigenetic and chromatin modifiers as targeted therapy of hematologic malignancies

KN Bhalla - Journal of Clinical Oncology, 2005 - ascopubs.org
Epigenetic regulation of gene expression is mediated through alterations in the DNA
methylation status, covalent modifications of core nucleosomal histones, rearrangement of …

Histone deacetylase-1 and-3 protein expression in human breast cancer: a tissue microarray analysis

CA Krusche, P Wülfing, C Kersting, A Vloet… - Breast cancer research …, 2005 - Springer
Impaired histone acetylation was recognized to be involved in carcinogenesis. Furthermore,
histone deacetylase (HDAC) inhibitors induce differentiation of breast cancer cells and …

Blockade of histone deacetylase inhibitor-induced RelA/p65 acetylation and NF-κB activation potentiates apoptosis in leukemia cells through a process mediated by …

Y Dai, M Rahmani, P Dent, S Grant - Molecular and cellular biology, 2005 - Taylor & Francis
NF-κB activation is reciprocally regulated by RelA/p65 acetylation and deacetylation, which
are mediated by histone acetyltransferases (HATs) and deacetylases (HDACs). Here we …

Rational development of histone deacetylase inhibitors as anticancer agents: a review

MR Acharya, A Sparreboom, J Venitz, WD Figg - Molecular pharmacology, 2005 - ASPET
The epigenome is defined by DNA methylation patterns and the associated post-
translational modifications of histones. This histone code determines the expression status …

Modulation of radiation response by histone deacetylase inhibition

P Chinnaiyan, G Vallabhaneni, E Armstrong… - International Journal of …, 2005 - Elsevier
Purpose: Histone deacetylase (HDAC) inhibitors, which modulate chromatin structure and
gene expression, represent a class of anticancer agents that hold particular potential as …