Results 1 to 10 of about 3,384,133 (256)

Characterization of a dual BET/HDAC inhibitor for treatment of pancreatic ductal adenocarcinoma

open access: yesInternational Journal of Cancer, 2020
Pancreatic ductal adenocarcinoma (PDAC) is resistant to virtually all chemo‐ and targeted therapeutic approaches. Epigenetic regulators represent a novel class of drug targets.
Feda H Hamdan   +2 more
exaly   +2 more sources

Re-programing Chromatin with a Bifunctional LSD1/HDAC Inhibitor Induces Therapeutic Differentiation in DIPG

open access: yesCancer Cell, 2019
H3K27M mutations resulting in epigenetic dysfunction are frequently observed in diffuse intrinsic pontine glioma (DIPGs), an incurable pediatric cancer.
Barry M Zee   +2 more
exaly   +2 more sources

HDAC Inhibitor-Induced Mitotic Arrest Is Mediated by Eg5/KIF11 Acetylation

open access: yesCell Chemical Biology, 2017
Summary Histone deacetylase 1 (HDAC1) is an epigenetic enzyme that regulates key cellular processes, such as cell proliferation, apoptosis, and cell survival, by deacetylating histone substrates.
Dhanusha A Nalawansha, Mary Kay H Pflum
exaly   +2 more sources

ZEB 1‐associated drug resistance in cancer cells is reversed by the class I HDAC inhibitor mocetinostat

open access: yesEMBO Molecular Medicine, 2015
Therapy resistance is a major clinical problem in cancer medicine and crucial for disease relapse and progression. Therefore, the clinical need to overcome it, particularly for aggressive tumors such as pancreatic cancer, is very high.
Simone Brabletz   +2 more
exaly   +2 more sources

Development of a Chimeric c-Src Kinase and HDAC Inhibitor

open access: yesACS Medicinal Chemistry Letters, 2013
On the basis of synergism observed between a selective c-Src kinase inhibitor with an HDAC inhibitor, the development of the first chimeric c-Src kinase and HDAC inhibitor is described.
Michael E Steffey, Matthew B Soellner
exaly   +2 more sources

Synthesis of a HDAC inhibitor-nanogold probe for cryo-EM visualization in class I HDAC co-repressor complexes. [PDF]

open access: yesBeilstein J Org Chem
Class I histone deacetylases (HDACs 1–3) serve as catalytic subunits within seven multiprotein co-repressor complexes, each of which has distinct functions in the cell.
Pytel WA, Schwabe JWR, Hodgkinson JT.
europepmc   +2 more sources

The HDAC inhibitor zabadinostat is a systemic regulator of adaptive immunity

open access: yesCommunications Biology, 2023
Protein acetylation plays a key role in regulating cellular processes and is subject to aberrant control in diverse pathologies. Although histone deacetylase (HDAC) inhibitors are approved drugs for certain cancers, it is not known whether they can be ...
Geng-Hung Liu   +9 more
semanticscholar   +1 more source

A Dual PI3K/HDAC Inhibitor Induces Immunogenic Ferroptosis to Potentiate Cancer Immune Checkpoint Therapy

open access: yesCancer Research, 2021
The dual PI3K/HDAC inhibitor BEBT-908 elicits potent anti-tumor responses, effectively inducing immunogenic ferroptosis of tumor cells and potentiating cancer immunotherapy.
F. Fan   +11 more
semanticscholar   +1 more source

Therapeutic potential of tucidinostat, a subtype-selective HDAC inhibitor, in cancer treatment

open access: yesFrontiers in Pharmacology, 2022
Histone deacetylase (HDAC) is one of the most characterized epigenetic modifiers, modulating chromatin structure and gene expression, which plays an important role in cell cycle, differentiation and apoptosis.
Yichen Sun   +6 more
semanticscholar   +1 more source

4-Hexylresorcinol Inhibits Class I Histone Deacetylases in Human Umbilical Cord Endothelial Cells

open access: yesApplied Sciences, 2021
Histone deacetylases (HDACs) are key enzymes for post-translational modification and influence on various cellular activities. Thus, HDACs are associated with many diseases and their inhibitors have clinical significance.
Jwa-Young Kim   +4 more
doaj   +1 more source

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