Histone modifications in epigenetic regulation of cancer: Perspectives and achieved progress

ME Neganova, SG Klochkov, YR Aleksandrova… - Seminars in Cancer …, 2022 - Elsevier
Epigenetic changes associated with histone modifications play an important role in the
emergence and maintenance of the phenotype of various cancer types. In contrast to direct …

Medicinal chemistry updates of novel HDACs inhibitors (2020 to present)

X He, Z Hui, L Xu, R Bai, Y Gao, Z Wang, T Xie… - European Journal of …, 2022 - Elsevier
Epigentic enzymes histone deacetylases (HDACs) catalyze the removal of acetyl groups
from the ε-N-acetylated lysine residues of various protein substrates including both histone …

Dual inhibitors of histone deacetylases and other cancer-related targets: A pharmacological perspective

Y Gao, H Zhang, F Lirussi, C Garrido, XY Ye… - Biochemical …, 2020 - Elsevier
Epigenetic enzymes histone deacetylases (HDACs) are clinically validated anticancer drug
targets which have been studied intensively in the past few decades. Although several drugs …

The zinc-binding group effect: lessons from non-hydroxamic acid vorinostat analogs

S Geurs, D Clarisse, K De Bosscher… - Journal of Medicinal …, 2023 - ACS Publications
Histone deacetylases (HDACs) are enzymes pursued as drug targets in various cancers and
several non-oncological conditions, such as inflammation and neurodegenerative disorders …

Selective and Bioavailable HDAC6 2-(Difluoromethyl)-1, 3, 4-oxadiazole Substrate Inhibitors and Modeling of Their Bioactivation Mechanism

L Ripa, J Sandmark, G Hughes… - Journal of Medicinal …, 2023 - ACS Publications
Histone deacetylase 6 (HDAC6) is a unique member of the HDAC family mainly targeting
cytosolic nonhistone substrates, such as α-tubulin, cortactin, and heat shock protein 90 to …

[HTML][HTML] Difluoromethyl-1, 3, 4-oxadiazoles are slow-binding substrate analog inhibitors of histone deacetylase 6 with unprecedented isotype selectivity

E Cellupica, G Caprini, P Cordella, C Cukier… - Journal of Biological …, 2023 - ASBMB
Histone deacetylase 6 (HDAC6) is an attractive drug development target because of its role
in the immune response, neuropathy, and cancer. Knockout mice develop normally and …

[HTML][HTML] Targeting epigenetic regulatory enzymes for cancer therapeutics: novel small-molecule epidrug development

Y Jin, T Liu, H Luo, Y Liu, D Liu - Frontiers in oncology, 2022 - frontiersin.org
Dysregulation of the epigenetic enzyme-mediated transcription of oncogenes or tumor
suppressor genes is closely associated with the occurrence, progression, and prognosis of …

[HTML][HTML] Oxadiazole derivatives: Histone deacetylase inhibitors in anticancer therapy and drug discovery

BW Matore, P Banjare, T Guria, PP Roy… - European Journal of …, 2022 - Elsevier
Heterocycles are being playing an important role in cancer treatment for years. Currently, a
number of anticancer agents are available on market, but concerns such as less …

[HTML][HTML] Role of selective histone deacetylase 6 inhibitor ACY-1215 in cancer and other human diseases

J Li, M Yu, S Fu, D Liu, Y Tan - Frontiers in Pharmacology, 2022 - frontiersin.org
The deacetylation process regulated by histone deacetylases (HDACs) plays an important
role in human health and diseases. HDAC6 belongs to the Class IIb of HDACs family, which …

[HTML][HTML] Balancing the interplay of histone deacetylases and non-coding genomes: a step closer to understand the landscape of cancer treatment

J Pu, T Liu, A Sharma, IGH Schmidt-Wolf - BMC medical genomics, 2023 - Springer
Histone deacetylase (HDAC) inhibitors have enormous therapeutic potential as effective
epigenetic regulators, and now with the focus on the selective HDAC6 inhibitor in ongoing …