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 …

[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] 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 …

Recent progress in nickel-catalyzed carboboration of alkenes

Y Ye, Y Lin, ND Mao, H Yang, XY Ye… - Organic & Biomolecular …, 2022 - pubs.rsc.org
Alkenes represent one of the most useful building blocks for organic synthesis, owing to their
abundance and versatile reactivity. Transition metal (Pd, Cu, Co, Ni, Fe, etc.) catalyzed …

Identification of mercaptoacetamide-based HDAC6 inhibitors via a lean inhibitor strategy: screening, synthesis, and biological evaluation

S Geurs, D Clarisse, F Baele, J Franceus… - Chemical …, 2022 - pubs.rsc.org
Non-selective inhibition of different histone deacetylase enzymes by hydroxamic acid-based
drugs causes severe side effects when used as a (long-term) cancer treatment. In this work …

Dual targeting strategies on histone deacetylase 6 (HDAC6) and heat shock protein 90 (Hsp90)

D Bonanni, A Citarella, D Moi, L Pinzi… - Current Medicinal …, 2022 - ingentaconnect.com
The design of multi-target drugs acting simultaneously on multiple signaling pathways is a
growing field in medicinal chemistry, especially for the treatment of complex diseases, such …

Novel hydroxyl carboximates derived from β-elemene: design, synthesis and anti-tumour activities evaluation

Y Gao, ND Mao, H Che, L Xu, R Bai… - Journal of Enzyme …, 2022 - Taylor & Francis
A series of novel N-alkyl-N-hydroxyl carboximates derived from β-elemene were fortuitously
discovered. Most of them showed more potent anti-proliferative activities than their lead …

Discovery of Benzylpiperazine Derivatives as CNS-Penetrant and Selective Histone Deacetylase 6 Inhibitors

K Hashimoto, S Ide, M Arata, A Nakata… - ACS Medicinal …, 2022 - ACS Publications
Inhibition of histone deacetylase 6 (HDAC6) in the brain is a highly attractive therapeutic
target for the treatment of neurodegenerative diseases. The low blood–brain barrier …