Sarcoma treatment in the era of molecular medicine

TGP Grünewald, M Alonso, S Avnet… - EMBO molecular …, 2020 - embopress.org
Sarcomas are heterogeneous and clinically challenging soft tissue and bone cancers.
Although constituting only 1% of all human malignancies, sarcomas represent the second …

Histone deacetylases and their inhibitors in cancer, neurological diseases and immune disorders

KJ Falkenberg, RW Johnstone - Nature reviews Drug discovery, 2014 - nature.com
Epigenetic aberrations, which are recognized as key drivers of several human diseases, are
often caused by genetic defects that result in functional deregulation of epigenetic proteins …

Organic carbamates in drug design and medicinal chemistry

AK Ghosh, M Brindisi - Journal of medicinal chemistry, 2015 - ACS Publications
The carbamate group is a key structural motif in many approved drugs and prodrugs. There
is an increasing use of carbamates in medicinal chemistry and many derivatives are …

Anticancer activities of histone deacetylase inhibitors

JE Bolden, MJ Peart, RW Johnstone - Nature reviews Drug discovery, 2006 - nature.com
Histone 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 …

HDAC family: What are the cancer relevant targets?

O Witt, HE Deubzer, T Milde, I Oehme - Cancer letters, 2009 - Elsevier
Histone deacetylases comprise a family of 18 genes, which are grouped into classes I–IV
based on their homology to their respective yeast orthologues. Classes I, II, and IV consist of …

Histone deacetylases: unique players in shaping the epigenetic histone code

SAM Thiagalingam, KH CHENG, HJ Lee… - Annals of the New …, 2003 - Wiley Online Library
The epigenome is defined by DNA methylation patterns and the associated posttranslational
modifications of histones. This histone code determines the expression status of individual …

Histone deacetylase inhibitors

TA Miller, DJ Witter, S Belvedere - Journal of medicinal chemistry, 2003 - ACS Publications
Histone deacetylase enzymes, which have been divided into three distinct structural classes,
operate by zinc-dependent (class I/II) or NAD-dependent (class III) mechanisms. Class I/II …

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 …

The histone deacetylase inhibitor MS-275 promotes differentiation or apoptosis in human leukemia cells through a process regulated by generation of reactive oxygen …

RR Rosato, JA Almenara, S Grant - Cancer research, 2003 - AACR
Abstract Effects of the histone deacetylase (HDAC) inhibitor MS-275 have been examined in
human leukemia and lymphoma cells (U937, HL-60, K562, and Jurkat) as well as in primary …

Histone deacetylase inhibitors in cancer therapy: is transcription the primary target?

RW Johnstone, JD Licht - Cancer cell, 2003 - cell.com
Characterization of transcriptional repressor fusion proteins in acute leukemia and growing
evidence of the importance of epigenetic changes in cancer onset and progression have …