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 …

Hydrazides as Inhibitors of Histone Deacetylases

MC Carreiras, J Marco-Contelles - Journal of Medicinal Chemistry, 2024 - ACS Publications
In this Perspective, we have brought together available biological evidence on hydrazides
as histone deacetylase inhibitors (HDACis) and as a distinct type of Zn-binding group (ZBG) …

Comparative Structure-Based Virtual Screening Utilizing Optimized AlphaFold Model Identifies Selective HDAC11 Inhibitor

F Baselious, S Hilscher, D Robaa, C Barinka… - International Journal of …, 2024 - mdpi.com
HDAC11 is a class IV histone deacylase with no crystal structure reported so far. The
catalytic domain of HDAC11 shares low sequence identity with other HDAC isoforms, which …

Stack-HDAC3i: a high-precision identification of HDAC3 inhibitors by exploiting a stacked ensemble-learning framework

W Shoombuatong, I Meewan, L Mookdarsanit… - Methods, 2024 - Elsevier
Epigenetics involves reversible modifications in gene expression without altering the genetic
code itself. Among these modifications, histone deacetylases (HDACs) play a key role by …

Bifunctionality and Antitumor Efficacy of ZG-126, a Vitamin D Receptor Agonist/Histone Deacetylase Inhibitor Hybrid Molecule

F Sarmadi, Z Gao, J Su, C Barbier… - Journal of Medicinal …, 2024 - ACS Publications
Analogues of hormonal vitamin D, 1, 25-dihydroxyvitamin D (1, 25D), signal through the
nuclear vitamin D receptor (VDR). They have potential in combination therapies with other …

Synthesis and antiproliferative potency of 1, 3, 4-thiadiazole and 1, 3-thiazolidine-4-one based new binary heterocyclic molecules: in vitro cell-based anticancer …

A Maji, A Himaja, S Nikhitha, S Rana, A Paul… - RSC Medicinal …, 2024 - pubs.rsc.org
Herein, we report the synthesis and anticancer properties of 21 new 1, 3, 4-thiadiazole-2-yl-
imino-thiazolidine-4-one containing binary heterocyclic molecules. Cytotoxicity of the …

Indolo[3,2-c]isoquinoline Hydroxamic Acid Derivatives as Novel Orally Topoisomerase-Histone Deacetylase Dual Inhibitors for NSCLC Therapy

B Wang, T Shi, S Jia, E Wang, X Ruan… - Journal of Medicinal …, 2024 - ACS Publications
Based on the synergistic effects of topoisomerase (Top) inhibitors and histone deacetylase
(HDAC) inhibitors in cancer therapy, a series of novel Top/HDAC dual inhibitors were …

Tubulin/HDAC dual-target inhibitors: Insights from design strategies, SARs, and therapeutic potential

Z Zhang, R Su, J Liu, K Chen, C Wu, P Sun… - European Journal of …, 2024 - Elsevier
Microtubules, one of the cytoskeletons in eukaryotic cells, maintain the proper operation of
several cellular functions. Additionally, they are regulated by the acetylation of HDAC6 and …

Derivatives of D (−)-glutamine-based MMP-2 inhibitors as an effective remedy for the management of chronic myeloid leukemia-Part-III: Synthesis, biological …

S Das, T Patel, A Himaja, S Regula, S Banerjee… - Bioorganic …, 2024 - Elsevier
Tyrosine kinase inhibitors (TKIs) have markedly improved the overall survival rate of patients
with chronic myeloid leukemia (CML), enabling them to achieve a normal life expectancy …

[HTML][HTML] Epigenetic Modulations in Triple-Negative Breast Cancer: Therapeutic Implications for Tumor Microenvironment

L Zhou, CW Yu - Pharmacological Research, 2024 - Elsevier
Triple-negative breast cancer (TNBC) is an aggressive subtype lacking estrogen receptors,
progesterone receptors and lacks HER2 overexpression. This absence of critical molecular …