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 …

Evolution of slow-binding inhibitors targeting histone deacetylase isoforms

A Mukherjee, F Zamani, T Suzuki - Journal of Medicinal Chemistry, 2023 - ACS Publications
Because the overexpression of histone deacetylase enzymes (HDACs) has been linked to
numerous diseases, including various cancers and neurodegenerative disorders, HDAC …

Technologies of targeting histone deacetylase in drug discovery: Current progress and emerging prospects

J Ru, Y Wang, Z Li, J Wang, C Ren, J Zhang - European Journal of …, 2023 - Elsevier
Histone deacetylases (HDACs) catalyze the hydrolysis of acetyl-l-lysine side chains in
histones and non-histones, which are key to epigenetic regulation in humans. Targeting …

Discovery of HDAC6-Selective Inhibitor NN-390 with in Vitro Efficacy in Group 3 Medulloblastoma

N Nawar, S Bukhari, AA Adile, Y Suk… - Journal of medicinal …, 2022 - ACS Publications
Histone deacetylase 6 (HDAC6) has been targeted in clinical studies for anticancer effects
due to its role in oncogenic transformation and metastasis. Through a second-generation …

Identification of histone deacetylase 10 (HDAC10) inhibitors that modulate autophagy in transformed cells

P Zeyen, Y Zeyn, D Herp, F Mahmoudi… - European journal of …, 2022 - Elsevier
Histone deacetylases (HDACs) are a family of 18 epigenetic modifiers that fall into 4 classes.
Histone deacetylase inhibitors (HDACi) are valid tools to assess HDAC functions. HDAC6 …

T-cell prolymphocytic leukemia: diagnosis, pathogenesis, and treatment

M Gutierrez, P Bladek, B Goksu… - International Journal of …, 2023 - mdpi.com
T-cell prolymphocytic leukemia (T-PLL) is a rare and aggressive neoplasm of mature T-cells.
Most patients with T-PLL present with lymphocytosis, anemia, thrombocytopenia, and …

Discovery of YSR734: A covalent HDAC inhibitor with cellular activity in acute myeloid leukemia and Duchenne muscular dystrophy

YS Raouf, A Sedighi, M Geletu, GA Frere… - Journal of Medicinal …, 2023 - ACS Publications
Histone deacetylases (HDACs) have emerged as powerful epigenetic modifiers of
histone/non-histone proteins via catalyzing the deacetylation of ε-N-acetyl lysines. The …

Discovery of Novel 1,2,3,4-Tetrahydrobenzofuro[2,3-c]pyridine Histone Deacetylase Inhibitors for Efficient Treatment of Hepatocellular Carcinoma

Z Lai, H Ni, X Hu, S Cui - Journal of Medicinal Chemistry, 2023 - ACS Publications
The development of histone deacetylase (HDAC) inhibitors for treating hematologic
malignancies has been widely investigated, while their role in hepatocellular carcinoma …

Identification of PI3K/HDAC Dual-targeted inhibitors with subtype selectivity as potential therapeutic agents against solid Tumors: Building HDAC6 potency in a …

Z Li, C Zhao, G He, Y Wang, Y Wang, X Ma - Bioorganic & medicinal …, 2022 - Elsevier
Pharmacological inhibition of PI3Kδ for battling solid tumors is relatively unexplored. Given
the potential synergism of concurrent PI3Kδ/HDAC6 inhibition, and the drawbacks of …

Development of a tetrahydroindazolone-based HDAC6 inhibitor with in-vivo anti-arthritic activity

HM Yang, C Lee, J Min, N Ha, D Bae, G Nam… - Bioorganic & Medicinal …, 2024 - Elsevier
Abstract Histone deacetylase 6 (HDAC6) induces the expression of pro-inflammatory
cytokines in macrophages; therefore, HDAC inhibitors may be beneficial for the treatment of …