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Bromodomain Inhibitor JQ1 Provides Novel Insights and Perspectives in Rhabdomyosarcoma Treatment

open access: yesInternational Journal of Molecular Sciences, 2022
Rhabdomyosarcoma (RMS) is the most common type of pediatric soft tissue sarcoma. It is classified into two main subtypes: embryonal (eRMS) and alveolar (aRMS). MYC family proteins are frequently highly expressed in RMS tumors, with the highest levels correlated with poor prognosis.
Francesco Paolo Fiorentino   +2 more
exaly   +3 more sources
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Synergistic antitumor activity of DHA and JQ1 in colorectal carcinoma

European Journal of Pharmacology, 2020
Colon 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
openaire   +2 more sources

JQ1: a novel potential therapeutic target

Die Pharmazie, 2018
The 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
openaire   +2 more sources

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

open access: yesACS 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 R MacKenzie   +2 more
exaly   +2 more sources

MPEC 2023-J126 : 2023 JQ1

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.
openaire   +1 more source

MPEC 2023-M54 : 2022 JQ1

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.
openaire   +1 more source

The bromodomain inhibitor JQ1 is a molecular glue targeting centromeres

2023
Centromeres 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
openaire   +1 more source

BET-inhibition by JQ1 alleviates streptozotocin-induced diabetic cardiomyopathy

Toxicology and Applied Pharmacology, 2018
Diabetic 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
openaire   +2 more sources

Synthesis, SAR, and application of JQ1 analogs as PROTACs for cancer therapy

Bioorganic and Medicinal Chemistry
JQ1 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.
Raghaba Sahu, Shubhendu Palei, Soumik De
exaly   +3 more sources

SOX9 is controlled by the BRD4 inhibitor JQ1 via multiple regulation mechanisms

Biochemical and Biophysical Research Communications, 2019
SOX9 is a key transcription factor during cell differentiation, sex determination, and tumorigenesis. However, the detailed mechanisms of its targeting strategy remain elusive. To investigate possibilities of targeting SOX9 with epigenetic drugs and the precise underlying mechanisms, two human cancer cell lines were chosen as model systems, which ...
Seong Hwi Hong, Jueng Soo You
openaire   +2 more sources

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