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 …

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 …

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 …

A therapeutic perspective of HDAC8 in different diseases: an overview of selective inhibitors

A Fontana, I Cursaro, G Carullo, S Gemma… - International Journal of …, 2022 - mdpi.com
Histone deacetylases (HDACs) are epigenetic enzymes which participate in transcriptional
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 …

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 …

Lysine deacetylase inhibitors in parasites: past, present, and future perspectives

GS Hailu, D Robaa, M Forgione, W Sippl… - Journal of Medicinal …, 2017 - ACS Publications
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 …

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 …

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 …

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 …