scholarly journals The mitochondrial transport protein SLC25A43 affects drug efficacy and drug-induced cell cycle arrest in breast cancer cell lines

2013 ◽  
Vol 29 (4) ◽  
pp. 1268-1274 ◽  
Author(s):  
MARIKE GABRIELSON ◽  
ELISABET TINA
Keyword(s):  
Breast Cancer ◽  
Cell Cycle ◽  
Cell Cycle Arrest ◽  
Cell Lines ◽  
Cancer Cell ◽  
Breast Cancer Cell ◽  
Drug Efficacy ◽  
Breast Cancer Cell Lines ◽  
Drug Induced ◽  
Cycle Arrest

scholarly journals Selective B-RAF V600E Inhibitor PLX4032 Inhibits the Growth of Breast Cancer Cell Lines through Cell Cycle Arrest

2016 ◽  
Vol 4 (2) ◽  
pp. 33-41
Author(s):  
Eun-Yeol Yang ◽  
Min-Young Park ◽  
Soo-Min Jung ◽  
Sang-Eun Nam ◽  
Jin-Ok Kwon ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cell Cycle ◽  
Cell Cycle Arrest ◽  
Cell Lines ◽  
Cancer Cell ◽  
Breast Cancer Cell ◽  
Cancer Cell Lines ◽  
Breast Cancer Cell Lines ◽  
Cycle Arrest

scholarly journals A tetraprenylated benzophenone 7-epiclusianone induces cell cycle arrest at G1/S transition by modulating critical regulators of cell cycle in breast cancer cell lines

2020 ◽  
Vol 68 ◽  
pp. 104927
Author(s):  
Simone da Silva Lamartine-Hanemann ◽  
Guilherme Álvaro Ferreira-Silva ◽  
Renato de Oliveira Horvath ◽  
Roseli Soncini ◽  
Ester Siqueira Caixeta ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cell Cycle ◽  
Cell Cycle Arrest ◽  
Cell Lines ◽  
Cancer Cell ◽  
Breast Cancer Cell ◽  
Cancer Cell Lines ◽  
Breast Cancer Cell Lines ◽  
Cycle Arrest

scholarly journals Structure-Based Discovery of a Selective KDM5A Inhibitor that Exhibits Anti-Cancer Activity via Inducing Cell Cycle Arrest and Senescence in Breast Cancer Cell Lines

Cancers ◽  
2019 ◽  
Vol 11 (1) ◽  
pp. 92 ◽  
Author(s):  
Guan-Jun Yang ◽  
Chung-Nga Ko ◽  
Hai-Jing Zhong ◽  
Chung-Hang Leung ◽  
Dik-Lung Ma
Keyword(s):  
Breast Cancer ◽  
Cell Cycle ◽  
Cell Cycle Arrest ◽  
Cell Lines ◽  
Cancer Cell ◽  
Breast Cancer Cell ◽  
Therapeutic Target ◽  
Breast Cancer Cell Lines ◽  
Cycle Arrest ◽  
Anti Cancer

Breast cancer is the one of the most frequent causes of female cancer mortality. KDM5A, a histone demethylase, can increase the proliferation, metastasis, and drug resistance of cancers, including breast cancer, and is thus an important therapeutic target. In the present work, we performed hierarchical virtual screening towards the KDM5A catalytic pocket from a chemical library containing 90,000 compounds. Using multiple biochemical methods, the cyclopenta[c]chromen derivative 1 was identified as the top candidate for KDM5A demethylase inhibitory activity. Compared with the well-known KDM5 inhibitor CPI-455 (18), 1 exhibited higher potency against KDM5A and much higher selectivity for KDM5A over both KDM4A and other KDM5 family members (KDM5B and KDM5C). Additionally, compound 1 repressed the proliferation of various KDM5A-overexpressing breast cancer cell lines. Mechanistically, 1 promoted accumulation of p16 and p27 by blocking KDM5A-mediated H3K4me3 demethylation, leading to cell cycle arrest and senescence. To date, compound 1 is the first cyclopenta[c]chromen-based KDM5A inhibitor reported, and may serve as a novel motif for developing more selective and efficacious pharmacological molecules targeting KDM5A. In addition, our research provides a possible anti-cancer mechanism of KDM5A inhibitors and highlights the feasibility and significance of KDM5A as a therapeutic target for KDM5A-overexpressing breast cancer.

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