Bromodomain inhibitors and therapeutic applications

BK Gajjela, MM Zhou - Current opinion in chemical biology, 2023 - Elsevier
The bromodomain acts to recognize acetylated lysine in histones and transcription proteins
and plays a fundamental role in chromatin-based cellular processes including gene …

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 …

BET–HDAC dual inhibitors for combinational treatment of breast cancer and concurrent candidiasis

Y Huang, N Liu, Z Pan, Z Li… - Journal of Medicinal …, 2023 - ACS Publications
Breast cancer is susceptible to Candida infections, and candidiasis has an enhancing effect
on the progression and metastasis of tumor. Breast cancer and concurrent candidiasis …

Discovery of BRD4–HDAC Dual Inhibitors with Improved Fungal Selectivity and Potent Synergistic Antifungal Activity against Fluconazole-Resistant Candida albicans

Z Li, Y Huang, J Tu, W Yang, N Liu… - Journal of Medicinal …, 2023 - ACS Publications
Over the past several decades, invasive fungal infections, especially candidiasis, have
caused dramatic morbidity and mortality due to ineffective antifungal drugs and severe drug …

Discovery of the Diphenyl 6-Oxo-1, 6-dihydropyridazine-3-carboxylate/carboxamide Analogue J27 for the Treatment of Acute Lung Injury and Sepsis by Targeting …

J Liao, J Yang, X Li, C Hu, W Zhu, Y Zhou… - Journal of Medicinal …, 2023 - ACS Publications
Acute lung injury (ALI) and sepsis are both serious and complex conditions associated with
high mortality, yet there are no effective treatments. Herein, we designed and synthesized a …

Development of potent dual BET/HDAC inhibitors via pharmacophore merging and structure-guided optimization

N Bauer, DI Balourdas, JR Schneider… - ACS chemical …, 2024 - ACS Publications
Bromodomain and extra-terminal domain (BET) proteins and histone deacetylases (HDACs)
are prime targets in cancer therapy. Recent research has particularly focused on the …

Molecular hybridization: a powerful tool for multitarget drug discovery

P de Sena Murteira Pinheiro, LS Franco… - Expert Opinion on …, 2024 - Taylor & Francis
Introduction The current drug discovery paradigm of 'one drug, multiple targets' has gained
attention from both the academic medicinal chemistry community and the pharmaceutical …

Design and synthesis of fibroblast growth factor receptor (FGFR) and histone deacetylase (HDAC) dual inhibitors for the treatment of cancer

G Wan, Z Feng, Q Zhang, X Li, K Ran… - Journal of Medicinal …, 2022 - ACS Publications
The activation of the STAT signal after incubation with the HDAC inhibitor represents a key
mechanism causing resistance to HDAC inhibitors in some solid tumor cells, while the FGFR …

In the quest for histone deacetylase inhibitors: Current trends in the application of multilayered computational methods

AI Uba, G Zengin - Amino Acids, 2023 - Springer
Histone deacetylase (HDAC) inhibitors have gained attention over the past three decades
because of their potential in the treatment of different diseases including various forms of …

Groebke Blackburn Bienaymé-mediated multi-component synthesis of selective HDAC6 inhibitors with anti-inflammatory properties

FB Kraft, J Enns, I Honin, J Engelhardt, A Schöler… - Bioorganic …, 2024 - Elsevier
Histone deacetylases (HDACs) are a class of enzymes that cleave acyl groups from lysine
residues of histone and non-histone proteins. There are 18 human HDAC isoforms with …