The zinc-binding group effect: lessons from non-hydroxamic acid vorinostat analogs
S Geurs, D Clarisse, K De Bosscher… - Journal of Medicinal …, 2023 - ACS Publications
Histone deacetylases (HDACs) are enzymes pursued as drug targets in various cancers and
several non-oncological conditions, such as inflammation and neurodegenerative disorders …
several non-oncological conditions, such as inflammation and neurodegenerative disorders …
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 …
histones and non-histones, which are key to epigenetic regulation in humans. Targeting …
Discovery of HDAC6, HDAC8, and 6/8 inhibitors and development of cell-based drug screening models for the treatment of TGF-β-induced idiopathic pulmonary …
WC Yu, TY Yeh, CH Ye, PCT Chong… - Journal of Medicinal …, 2023 - ACS Publications
Idiopathic pulmonary fibrosis is incurable, and its progression is difficult to control and thus
can lead to pulmonary deterioration. Pan-histone deacetylase inhibitors such as SAHA have …
can lead to pulmonary deterioration. Pan-histone deacetylase inhibitors such as SAHA have …
Medicinal chemistry insights into non-hydroxamate HDAC6 selective inhibitors
Faridoon, YL Zha, G Zhang, JJ Li - Medicinal Chemistry Research, 2023 - Springer
HDAC6 is predominantly found in the cytoplasm and is mainly responsible for deacetylation
of non-histone proteins including α-tubulin in microtubules, the HSP90 chaperone, cortactin …
of non-histone proteins including α-tubulin in microtubules, the HSP90 chaperone, cortactin …
Rational design of metabolically stable HDAC inhibitors: An overhaul of trifluoromethyl ketones
Epigenetic regulation of gene expression using histone deacetylase (HDAC) inhibitors is a
promising strategy for developing new anticancer agents. The most common HDAC …
promising strategy for developing new anticancer agents. The most common HDAC …
Targeting Relevant HDACs to Support the Survival of Cone Photoreceptors in Inherited Retinal Diseases: Identification of a Potent Pharmacological Tool with In Vitro …
Inherited retinal diseases, which include retinitis pigmentosa, are a family of genetic
disorders characterized by gradual rod-cone degeneration and vision loss, without effective …
disorders characterized by gradual rod-cone degeneration and vision loss, without effective …
Tailoring adipose stem cells towards high therapeutic performance: Perspectives in manipulation and manufacturing
J Song, L Zhang, B Song, G Yang - Chemical Engineering Journal, 2023 - Elsevier
Adipose tissues are broadly distributed in human bodies especially of the obese population,
which have long been considered as a surplus proportion. With the advancement of cell …
which have long been considered as a surplus proportion. With the advancement of cell …
[HTML][HTML] 2-Substituted 1, 5-benzothiazepine-based HDAC inhibitors exert anticancer activities on human solid and acute myeloid leukemia cell lines
Herein, we report the development of a new series of histone deacetylase inhibitors (HDACi)
containing a 2-substituted 1, 5-benzothiazepine scaffold. First, a virtual combinatorial library …
containing a 2-substituted 1, 5-benzothiazepine scaffold. First, a virtual combinatorial library …
Galanin 2 receptor: a novel target for a subset of pancreatic ductal adenocarcinoma
P Namsolleck, B Kofler, GN Moll - International Journal of Molecular …, 2023 - mdpi.com
Galanin is a 30 amino acid peptide that stimulates three subtype receptors (GAL1–3R).
M89b is a lanthionine-stabilized, C-terminally truncated galanin analog that specifically …
M89b is a lanthionine-stabilized, C-terminally truncated galanin analog that specifically …