[HTML][HTML] HDAC inhibitors: Targets for tumor therapy, immune modulation and lung diseases

G Shanmugam, S Rakshit, K Sarkar - Translational Oncology, 2022 - Elsevier
Histone deacetylases (HDACs) are enzymes that play a key role in the epigenetic regulation
of gene expression by remodeling chromatin. Inhibition of HDACs is a prospective …

Targeting histone deacetylases in idiopathic pulmonary fibrosis: a future therapeutic option

M Korfei, P Mahavadi, A Guenther - Cells, 2022 - mdpi.com
Idiopathic pulmonary fibrosis (IPF) is a progressive and fatal lung disease with limited
therapeutic options, and there is a huge unmet need for new therapies. A growing body of …

Pharmacological inhibition of HDAC6 improves muscle phenotypes in dystrophin-deficient mice by downregulating TGF-β via Smad3 acetylation

A Osseni, A Ravel-Chapuis, E Belotti, I Scionti… - Nature …, 2022 - nature.com
The absence of dystrophin in Duchenne muscular dystrophy disrupts the dystrophin-
associated glycoprotein complex resulting in skeletal muscle fiber fragility and atrophy …

Inhibition of histone deacetylase 6 destabilizes ERK phosphorylation and suppresses cancer proliferation via modulation of the tubulin acetylation-GRP78 interaction

O Wattanathamsan, N Chantaravisoot… - Journal of Biomedical …, 2023 - Springer
Background The leading cause of cancer-related mortality worldwide is lung cancer, and its
clinical outcome and prognosis are still unsatisfactory. The understanding of potential …

Small molecules targeting HATs, HDACs, and BRDs in cancer therapy

D Wu, Y Qiu, Y Jiao, Z Qiu, D Liu - Frontiers in oncology, 2020 - frontiersin.org
Evidence for research over the past decade shows that epigenetic regulation mechanisms
run through the development and prognosis of tumors. Therefore, small molecular …

Histone deacetylase inhibition in non-small cell lung cancer: hype or hope?

H Mamdani, SI Jalal - Frontiers in cell and developmental biology, 2020 - frontiersin.org
Epigenetic modulation, including acetylation, methylation, phosphorylation, and
ubiquitination, plays a pivotal role in regulation of gene expression. Histone acetylation—a …

Selective histone deacetylase inhibitor ACY-241 (citarinostat) plus nivolumab in advanced Non-Small cell lung cancer: Results from a phase ib study

MM Awad, Y Le Bruchec, B Lu, J Ye, JA Miller… - Frontiers in …, 2021 - frontiersin.org
Background Histone deacetylase (HDAC) overexpression has been documented in various
cancers and may be associated with worse outcomes. Data from early-phase studies of …

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 …

Accommodation of ring C expanded deoxyvasicinone in the HDAC inhibitory pharmacophore culminates into a tractable anti-lung cancer agent and pH-responsive …

R Sharma, E Chatterjee, J Mathew, S Sharma… - European Journal of …, 2022 - Elsevier
A fragment recruitment process was conducted to pinpoint a suitable fragment for installation
in the HDAC inhibitory template to furnish agents endowed with the potential to treat lung …

Histone deacetylase 6-mediated downregulation of TMEM100 expedites the development and progression of non-small cell lung cancer

Y Wang, M Ha, M Li, L Zhang, Y Chen - Human Cell, 2022 - Springer
The significance of epigenetic modulation, involving acetylation, methylation, as well as
ubiquitination has been indicated in the regulation of gene expression and tumor …