Annual review of PROTAC degraders as anticancer agents in 2022

X Wang, ZL Qin, N Li, MQ Jia, QG Liu, YR Bai… - European Journal of …, 2024 - Elsevier
Following nearly two decades of development, significant advancements have been
achieved in PROTAC technology. As of the end of 2022, more than 20 drugs have entered …

Histone deacetylase (HDAC) inhibitors in cancer: a patent review (2017-present)

C Zhao, H Dong, Q Xu, Y Zhang - Expert opinion on therapeutic …, 2020 - Taylor & Francis
Introduction: Histone deacetylase (HDAC) inhibitors play a crucial role in restoring the
balance of acetylation and deacetylation of lysine residues of histones and non-histone …

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 …

[HTML][HTML] 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 …

Structure-based discovery of selective histone deacetylase 8 degraders with potent anticancer activity

J Huang, J Zhang, W Xu, Q Wu, R Zeng… - Journal of Medicinal …, 2022 - ACS Publications
Inducing protein degradation by proteolysis targeting chimeras has gained tremendous
momentum as a promising novel therapeutic strategy. Here, we report the design, synthesis …

Characterization of histone deacetylase 8 (HDAC8) selective inhibition reveals specific active site structural and functional determinants

M Marek, TB Shaik, T Heimburg… - Journal of medicinal …, 2018 - ACS Publications
Metal-dependent histone deacetylases (HDACs) are key epigenetic regulators that
represent promising therapeutic targets for the treatment of numerous human diseases. Yet …

Are inhibitors of histone deacetylase 8 (HDAC8) effective in hematological cancers especially acute myeloid leukemia (AML) and acute lymphoblastic leukemia (ALL) …

SA Amin, S Khatun, S Gayen, S Das, T Jha - European Journal of Medicinal …, 2023 - Elsevier
Abstract Histone deacetylase 8 (HDAC8) aberrantly deacetylates histone and non-histone
proteins. These include structural maintenance of chromosome 3 (SMC3) cohesin protein …

Synthesis, molecular docking and biological characterization of pyrazine linked 2-aminobenzamides as new class I selective histone deacetylase (HDAC) inhibitors …

HS Ibrahim, M Abdelsalam, Y Zeyn, M Zessin… - International journal of …, 2021 - mdpi.com
Class I histone deacetylases (HDACs) are key regulators of cell proliferation and they are
frequently dysregulated in cancer cells. We report here the synthesis of a novel series of …

Overview of class I HDAC modulators: Inhibitors and degraders

Z Huang, L Zeng, B Cheng, D Li - European Journal of Medicinal Chemistry, 2024 - Elsevier
Class I histone deacetylases (HDACs) are closely associated with the development of a
diverse array of diseases, including cancer, neurodegenerative disorders, HIV, and …

Design and synthesis of triazole-containing HDAC inhibitors that induce antitumor effects and immune response

N Sun, K Yang, W Yan, M Yao, C Yu… - Journal of Medicinal …, 2023 - ACS Publications
Histone deacetylase (HDAC) is an epigenetic antitumor drug target, but most existing HDAC
inhibitors show limited antitumor activity and their use is often accompanied by serious …