Combination therapy with histone deacetylase inhibitors (HDACi) for the treatment of cancer: achieving the full therapeutic potential of HDACi

A Suraweera, KJ O'Byrne, DJ Richard - Frontiers in oncology, 2018 - frontiersin.org
Genetic and epigenetic changes in DNA are involved in cancer development and tumor
progression. Histone deacetylases (HDACs) are key regulators of gene expression that act …

An overview of benzo [b] thiophene-based medicinal chemistry

RS Keri, K Chand, S Budagumpi, SB Somappa… - European journal of …, 2017 - Elsevier
Among sulfur containing heterocycles, benzothiophene and its derivatives are at the focus
as these candidates have structural similarities with active compounds to develop new …

Modulators of protein–protein interactions

LG Milroy, TN Grossmann, S Hennig… - Chemical …, 2014 - ACS Publications
Since Hedin's characterization of trypsin and antitrypsin in 1906,(1) arguably the first
account of a regulatory protein–protein interaction (PPI), contemporary understanding of …

Epigenetics and approaches to targeted epigenetic therapy in acute myeloid leukemia

BJ Wouters, R Delwel - Blood, The Journal of the American …, 2016 - ashpublications.org
Acute myeloid leukemia (AML) is the most common type of acute leukemia in adults. AML is
a heterogeneous malignancy characterized by distinct genetic abnormalities. Recent …

Chromatin proteins and modifications as drug targets

K Helin, D Dhanak - Nature, 2013 - nature.com
A plethora of groundbreaking studies have demonstrated the importance of chromatin-
associated proteins and post-translational modifications of histones, proteins and DNA (so …

Roles of histone deacetylases in epigenetic regulation: emerging paradigms from studies with inhibitors

GP Delcuve, DH Khan, JR Davie - Clinical epigenetics, 2012 - Springer
The zinc-dependent mammalian histone deacetylase (HDAC) family comprises 11 enzymes,
which have specific and critical functions in development and tissue homeostasis. Mounting …

HDAC inhibitors in acute myeloid leukemia

E San José-Enériz, N Gimenez-Camino, X Agirre… - Cancers, 2019 - mdpi.com
Acute myeloid leukemia (AML) is a hematological malignancy characterized by uncontrolled
proliferation, differentiation arrest, and accumulation of immature myeloid progenitors …

Structure of HDAC3 bound to co-repressor and inositol tetraphosphate

PJ Watson, L Fairall, GM Santos, JWR Schwabe - Nature, 2012 - nature.com
Histone deacetylase enzymes (HDACs) are emerging cancer drug targets. They regulate
gene expression by removing acetyl groups from lysine residues in histone tails, resulting in …

The epigenetic effects of butyrate: potential therapeutic implications for clinical practice

R Berni Canani, M Di Costanzo, L Leone - Clinical epigenetics, 2012 - Springer
Butyrate is a short chain fatty acid derived from the microbial fermentation of dietary fibers in
the colon. In the last decade, multiple beneficial effects of butyrate at intestinal and …

Small changes huge impact: the role of protein posttranslational modifications in cellular homeostasis and disease

TM Karve, AK Cheema - Journal of amino acids, 2011 - Wiley Online Library
Posttranslational modifications (PTMs) modulate protein function in most eukaryotes and
have a ubiquitous role in diverse range of cellular functions. Identification, characterization …