Results 171 to 180 of about 14,237 (205)
European Journal of Pharmaceutics and Biopharmaceutics, 2022 Bromodomain and extraterminal domain protein inhibitors (BETi) for cancer treatment did not convince during their first clinical trials. Their epigenetic mechanism of action is still not well understood, even if MYC is generally considered as its main downstream target. In this context, we intended to assess two new nanoformulations of the BETi JQ1 for
Thibaut, Fourniols +9 more
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ACS Medicinal Chemistry LettersThe 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 ...
Kenneth B Guzman Rodríguez +2 more
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Synergistic antitumor activity of DHA and JQ1 in colorectal carcinoma
European Journal of Pharmacology, 2020Colon cancer is still a major disease plaguing humans. In this study, we evaluated the synergistic antitumor effects of the combination of BRD4 inhibitor JQ1 and docosahexaenoic acid (DHA) in colon cancer. We demonstrated that simultaneous exposure to JQ1 and DHA resulted in strong synergistic antiproliferative and proapoptotic effects related to ...
Wanjing, Ding +2 more
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JQ1: a novel potential therapeutic target
Die Pharmazie, 2018The bromo- and extra-terminal domain (BET) signaling pathway plays an important role in cell proliferation, immune responses, and pro-inflammatory events. JQ1 as a first-in-class potent and selective inhibitor of the BRD4 signaling pathway is widely used for tumor biology studies.
Xiaoyu Shi, Xiaoyu Shi +5 more
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2023
The Minor Planet Electronic Circulars contain information on unusual minor planets, routine data on comets and natural satellites, and occasional editorial announcements. They are published on behalf of Division F of the International Astronomical Union by the Minor Planet Center, Smithsonian Astrophysical Observatory, Cambridge, MA 02138, U.S.A.
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The Minor Planet Electronic Circulars contain information on unusual minor planets, routine data on comets and natural satellites, and occasional editorial announcements. They are published on behalf of Division F of the International Astronomical Union by the Minor Planet Center, Smithsonian Astrophysical Observatory, Cambridge, MA 02138, U.S.A.
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2023
The Minor Planet Electronic Circulars contain information on unusual minor planets, routine data on comets and natural satellites, and occasional editorial announcements. They are published on behalf of Division F of the International Astronomical Union by the Minor Planet Center, Smithsonian Astrophysical Observatory, Cambridge, MA 02138, U.S.A.
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The Minor Planet Electronic Circulars contain information on unusual minor planets, routine data on comets and natural satellites, and occasional editorial announcements. They are published on behalf of Division F of the International Astronomical Union by the Minor Planet Center, Smithsonian Astrophysical Observatory, Cambridge, MA 02138, U.S.A.
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BET-inhibition by JQ1 alleviates streptozotocin-induced diabetic cardiomyopathy
Toxicology and Applied Pharmacology, 2018Diabetic cardiomyopathy is a cascade of complex events leading to eventual heart failure in diabetes. JQ1, one of Bromodomain and extra-terminal domain (BET) protein inhibitors, has exerted therapeutic effects on cancer proliferation, inflammation and cardiovascular disease.
Miao, Guo, Hong-Xia, Wang, Wen-Jun, Chen
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The bromodomain inhibitor JQ1 is a molecular glue targeting centromeres
2023Centromeres are the position on each chromosome that orchestrates the accurate partitioning of the genome during cell division. Centromere-dependent cell-cycle checkpoints are maintained by cancer cells to prevent catastrophic chromosome segregation defects in dividing cells 1, 2 , making ...
Samuel Corless +8 more
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Effect of TNIK upregulation on JQ1-resistant human colorectal cancer HCT116 cells
Biochemical and Biophysical Research Communications, 2020JQ1 disrupts the binding of bromodomain and extra-terminal (BET) family of proteins to acetylated histones, modulates the expression of various genes, and inhibits the proliferation of cancer cells. We established two JQ1-resistant sublines from human colorectal cancer HCT116 cells. These resistant cells showed an 8- to 9-fold higher resistance to JQ1,
Chihiro Takahashi +6 more
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Synthesis, SAR, and application of JQ1 analogs as PROTACs for cancer therapy
Bioorganic & Medicinal ChemistryJQ1 is a wonder therapeutic molecule that selectively inhibits the BRD4 signaling pathway and is thus widely used in the anticancer drug discovery program. Due to its unique selective BRD4 binding property, its applications are further extended in the design and synthesis of bi-functional PROTAC molecules.
Soumik, De +3 more
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