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Chemical Catalysis Guides Structural Identification for the Major In Vivo Metabolite of the BET Inhibitor JQ1 [PDF]

ACS Medicinal Chemistry Letters
The bromodomain inhibitor (+)-JQ1 is a highly validated chemical probe; however, it exhibits poor in vivo pharmacokinetics. To guide efforts toward improving its pharmacological properties, we identified the (+)-JQ1 primary metabolite using chemical ...
Kevin Mackenzie, Martin Matzuk, Damian Young   +2 more
exaly   +2 more sources

Synergistic Therapy for Cervical Cancer by Codelivery of Cisplatin and JQ1 Inhibiting Plk1-Mutant Trp53 Axis

Nano Letters, 2021
Zhilin Liu, Shuchun Li, Na Shen
exaly  

Bromodomain Inhibitor JQ1 Provides Novel Insights and Perspectives in Rhabdomyosarcoma Treatment

International Journal of Molecular Sciences, 2022
Francesco Paolo Fiorentino, Irène Marchesi, Milena Fais   +2 more
exaly  

BET bromodomain inhibitor JQ1 regulates spermatid development by changing chromatin conformation in mouse spermatogenesis

Genes and Diseases, 2022
Gangcai Xie, Shengnan Gong, Zhiran Li
exaly  

JQ1, a selective inhibitor of BRD4, suppresses retinoblastoma cell growth by inducing cell cycle arrest and apoptosis

Experimental Eye Research, 2021
Huang Guofu, Yanyan Zhang
exaly  

JQ1 inhibits tumour growth in combination with cisplatin and suppresses JAK/STAT signalling pathway in ovarian cancer

European Journal of Cancer, 2020
Michalis Liontos, Efstathios Kastritis, Alexandros Rodolakis   +2 more
exaly  

BRD4 inhibition by JQ1 prevents high-fat diet-induced diabetic cardiomyopathy by activating PINK1/Parkin-mediated mitophagy in vivo

Journal of Molecular and Cellular Cardiology, 2020
Donghong Zhang, Minghui Zou, Zhonglin Xie   +2 more
exaly  

Development and validation of an LC-MS/MS method to quantify the bromodomain and extra-terminal (BET) inhibitor JQ1 in mouse plasma and brain microdialysate: Application to cerebral microdialysis study

Journal of Pharmaceutical and Biomedical Analysis, 2021
Olivia Campagne, Clinton Stewart, John Schuetz   +2 more
exaly  

Co-Encapsulation of Paclitaxel and JQ1 in Zein Nanoparticles as Potential Innovative Nanomedicine

Micromachines, 2022
Diego Russo, Massimo Fresta, Donato Cosco   +2 more
exaly  

Synergistic effect of JQ1 and rapamycin for treatment of human osteosarcoma

International Journal of Cancer, 2015
H Phillip Koeffler, Jonathan Said, Jun Qi   +2 more
exaly