Synthesis and biological evaluation of ortho-phenyl phenylhydroxamic acids containing phenothiazine with improved selectivity for class IIa histone deacetylases

Autor: Kai-Cheng Hsu, Yun-Yi Huang, Jung-Chun Chu, Yu-Wen Huang, Jing-Lan Hu, Tony Eight Lin, Shih-Chung Yen, Jing-Ru Weng, Wei-Jan Huang

Publikováno v: Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 39, Iss 1 (2024)

Class IIa histone deacetylases (HDACs) have been linked to tumorigenesis in various cancers. Previously, we designed phenylhydroxamic acid LH4f as a potent class IIa HDAC inhibitor. However, it also unselectively inhibited class I and class IIb HDACs

Externí odkaz: https://doaj.org/article/2d0d3d594369440e9a61c2c583b064c2

Design, synthesis, and biological evaluation of indolin-2-one derivatives as novel cyclin-dependent protein kinase 8 (CDK8) inhibitors

Autor: Jui-Yi Hsu, Kai-Cheng Hsu, Ching Sun, Ching-Hsuan Chou, Tony Eight Lin, Tzu-Ying Sung, Hui-Ju Tseng, Shih-Chung Yen, Chia-Ron Yang, Wei-Jan Huang

Publikováno v: Biomedicine & Pharmacotherapy, Vol 159, Iss , Pp 114258- (2023)

Cyclin-dependent protein kinase 8 (CDK8) plays important roles in regulating fibrotic growth factors and inflammatory signaling pathways. Long-term chronic inflammation of the lungs can lead to idiopathic pulmonary fibrosis (IPF). Abnormal alveolar e

Externí odkaz: https://doaj.org/article/69ee12bcfc574e07acf7e07b3ddb8146

Identification of a dual TAOK1 and MAP4K5 inhibitor using a structure-based virtual screening approach

Autor: Min-Wu Chao, Tony Eight Lin, Wei-Chun HuangFu, Chao-Di Chang, Huang-Ju Tu, Liang-Chieh Chen, Shih-Chung Yen, Tzu-Ying Sung, Wei-Jan Huang, Chia-Ron Yang, Shiow-Lin Pan, Kai-Cheng Hsu

Publikováno v: Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 36, Iss 1, Pp 98-108 (2021)

The STE20 kinase family is a complex signalling cascade that regulates cytoskeletal organisation and modulates the stress response. This signalling cascade includes various kinase mediators, such as TAOK1 and MAP4K5. The dysregulation of the STE20 ki

Externí odkaz: https://doaj.org/article/a23f5c3bf07c4ef483bac5eb846abc10

Identification of a dual TAOK1 and MAP4K5 inhibitor using a structure-based virtual screening approach

Autor: Kai Cheng Hsu, Tony Eight Lin, Liang Chieh Chen, Huang Ju Tu, Chia-Ron Yang, Min Wu Chao, Wei Chun HuangFu, Shiow Lin Pan, Tzu Ying Sung, Wei Jan Huang, Shih Chung Yen, Chao Di Chang

Publikováno v: Journal of Enzyme Inhibition and Medicinal Chemistry
article-version (VoR) Version of Record
Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 36, Iss 1, Pp 98-108 (2021)

The STE20 kinase family is a complex signalling cascade that regulates cytoskeletal organisation and modulates the stress response. This signalling cascade includes various kinase mediators, such as TAOK1 and MAP4K5. The dysregulation of the STE20 ki

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::aa48ff72915f71f9bb552eb8d86b042f
http://europepmc.org/articles/PMC7655034

O-methylated flavonol as a multi-kinase inhibitor of leukemogenic kinases exhibits a potential treatment for acute myeloid leukemia

Autor: Shih-Chung Yen, Yi-Wen Wu, Cheng-Chiao Huang, Min-Wu Chao, Huang-Ju Tu, Liang-Chieh Chen, Tony Eight Lin, Tzu-Ying Sung, Hui-Ju Tseng, Jung-Chun Chu, Wei-Jan Huang, Chia-Ron Yang, Wei-Chun HuangFu, Shiow-Lin Pan, Kai-Cheng Hsu

Publikováno v: Phytomedicine. 100:154061

Acute myeloid leukemia (AML) is a heterogeneous disease with poor overall survival characterized by various genetic changes. The continuous activation of oncogenic pathways leads to the development of drug resistance and limits current therapeutic ef

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::99d51d27fbbe4e480ec1f5ce4412a725
https://doi.org/10.1016/j.phymed.2022.154061