Histone deacetylases (HDACs): evolution, specificity, role in transcriptional complexes, and pharmacological actionability
G Milazzo, D Mercatelli, G Di Muzio, L Triboli… - Genes, 2020 - mdpi.com
Histone deacetylases (HDACs) are evolutionary conserved enzymes which operate by
removing acetyl groups from histones and other protein regulatory factors, with functional …
removing acetyl groups from histones and other protein regulatory factors, with functional …
Strategies to design selective histone deacetylase inhibitors
J Melesina, CV Simoben, L Praetorius… - …, 2021 - Wiley Online Library
This review classifies drug‐design strategies successfully implemented in the development
of histone deacetylase (HDAC) inhibitors, which have many applications including cancer …
of histone deacetylase (HDAC) inhibitors, which have many applications including cancer …
The search for potent, small‐molecule HDACIs in cancer treatment: a decade after vorinostat
C Zagni, G Floresta, G Monciino… - Medicinal research …, 2017 - Wiley Online Library
Histone deacetylases (HDACs) play a crucial role in the remodeling of chromatin, and are
involved in the epigenetic regulation of gene expression. In the last decade, inhibition of …
involved in the epigenetic regulation of gene expression. In the last decade, inhibition of …
A therapeutic perspective of HDAC8 in different diseases: an overview of selective inhibitors
Histone deacetylases (HDACs) are epigenetic enzymes which participate in transcriptional
repression and chromatin condensation mechanisms by removing the acetyl moiety from …
repression and chromatin condensation mechanisms by removing the acetyl moiety from …
[HTML][HTML] Effect of clinically approved HDAC inhibitors on Plasmodium, Leishmania and Schistosoma parasite growth
MJ Chua, MSJ Arnold, W Xu, J Lancelot… - International Journal for …, 2017 - Elsevier
Malaria, schistosomiasis and leishmaniases are among the most prevalent tropical parasitic
diseases and each requires new innovative treatments. Targeting essential parasite …
diseases and each requires new innovative treatments. Targeting essential parasite …
Targeting histone deacetylase 8 as a therapeutic approach to cancer and neurodegenerative diseases
A Chakrabarti, J Melesina, FR Kolbinger… - Future medicinal …, 2016 - Taylor & Francis
Histone deacetylase 8 (HDAC8), a unique class I zinc-dependent HDAC, is an emerging
target in cancer and other diseases. Its substrate repertoire extends beyond histones to …
target in cancer and other diseases. Its substrate repertoire extends beyond histones to …
Lysine deacetylase inhibitors in parasites: past, present, and future perspectives
Current therapies for human parasite infections rely on a few drugs, most of which have
severe side effects, and their helpfulness is being seriously compromised by the drug …
severe side effects, and their helpfulness is being seriously compromised by the drug …
Rational design and diversity-oriented synthesis of peptoid-based selective HDAC6 inhibitors
D Diedrich, A Hamacher, CGW Gertzen… - Chemical …, 2016 - pubs.rsc.org
A mini library of HDAC inhibitors with peptoid-based cap groups was synthesized using an
efficient multicomponent approach. Four compounds were identified as potent HDAC6 …
efficient multicomponent approach. Four compounds were identified as potent HDAC6 …
One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites
D Diedrich, K Stenzel, E Hesping… - European journal of …, 2018 - Elsevier
Malaria drug discovery has shifted from a focus on targeting asexual blood stage parasites,
to the development of drugs that can also target exo-erythrocytic forms and/or gametocytes …
to the development of drugs that can also target exo-erythrocytic forms and/or gametocytes …
Post-translational Modifications of Trypanosoma cruzi Canonical and Variant Histones
GFA Picchi, V Zulkievicz, MA Krieger… - Journal of proteome …, 2017 - ACS Publications
Chagas disease, caused by Trypanosoma cruzi, still affects millions of people around the
world. No vaccines nor treatment for chronic Chagas disease are available, and …
world. No vaccines nor treatment for chronic Chagas disease are available, and …