Colorectal cancer inhibition by BET inhibitor JQ1 is MYC-independent and not improved by nanoencapsulation

2022 ◽  
Author(s):  
Thibaut Fourniols ◽  
Valentina Maggio ◽  
Diana Rafael ◽  
Ariana Colaco ◽  
Elia García Vidal ◽  
...  
Keyword(s):  
Colorectal Cancer ◽  
Bet Inhibitor ◽  
Cancer Inhibition

Higher Farnesyl Diphosphate Synthase Activity in Human Colorectal Cancer Inhibition of Cellular Apoptosis

Oncology ◽  
2004 ◽  
Vol 67 (5-6) ◽  
pp. 351-358 ◽  
Author(s):  
Maria Notarnicola ◽  
Caterina Messa ◽  
Aldo Cavallini ◽  
Maurizio Bifulco ◽  
Mario Felice Tecce ◽  
...  
Keyword(s):  
Colorectal Cancer ◽  
Farnesyl Diphosphate ◽  
Farnesyl Diphosphate Synthase ◽  
Human Colorectal Cancer ◽  
Cellular Apoptosis ◽  
Cancer Inhibition

Application of a polyelectrolyte complex based on biocompatible polysaccharides for colorectal cancer inhibition

2020 ◽  
pp. 108194
Author(s):  
Paulo R. Souza ◽  
Bruno H. Vilsinski ◽  
Cátia S. Nunes ◽  
Letícia C. Bonkovoski ◽  
Francielle Garcia ◽  
...  
Keyword(s):  
Colorectal Cancer ◽  
Polyelectrolyte Complex ◽  
Cancer Inhibition

scholarly journals Stromal induction of BRD4 phosphorylation Results in Chromatin Remodeling and BET inhibitor Resistance in Colorectal Cancer

2021 ◽  
Vol 12 (1) ◽  
Author(s):  
Wenyu Wang ◽  
Yen-An Tang ◽  
Qian Xiao ◽  
Wee Chyan Lee ◽  
Bing Cheng ◽  
...  
Keyword(s):  
Colorectal Cancer ◽  
Chromatin Remodeling ◽  
Cancer Drug ◽  
Bet Inhibitor ◽  
Cancer Associated Fibroblast ◽  
Bet Inhibitors ◽  
Inhibitor Resistance ◽  
Bet Protein

AbstractBRD4, a Bromodomain and Extraterminal (BET) protein family member, is a promising anti-cancer drug target. However, resistance to BET inhibitors targeting BRD4 is common in solid tumors. Here, we show that cancer-associated fibroblast (CAF)-activated stromal signaling, interleukin-6/8-JAK2, induces BRD4 phosphorylation at tyrosine 97/98 in colorectal cancer, resulting in BRD4 stabilization due to interaction with the deubiquitinase UCHL3. BRD4 phosphorylation at tyrosine 97/98 also displays increased binding to chromatin but reduced binding to BET inhibitors, resulting in resistance to BET inhibitors. We further show that BRD4 phosphorylation promotes interaction with STAT3 to induce chromatin remodeling through concurrent binding to enhancers and super-enhancers, supporting a tumor-promoting transcriptional program. Inhibition of IL6/IL8-JAK2 signaling abolishes BRD4 phosphorylation and sensitizes BET inhibitors in vitro and in vivo. Our study reveals a stromal mechanism for BRD4 activation and BET inhibitor resistance, which provides a rationale for developing strategies to treat CRC more effectively.

BET inhibitor bromosporine enhances 5-FU effect in colorectal cancer cells

2020 ◽  
Vol 521 (4) ◽  
pp. 840-845 ◽  
Author(s):  
Xueyuan Cheng ◽  
Zhong Huang ◽  
Di Long ◽  
Wei Jin
Keyword(s):  
Colorectal Cancer ◽  
Cancer Cells ◽  
Bet Inhibitor ◽  
Colorectal Cancer Cells

Chemotherapy of Advanced Colorectal Cancer: Inhibition of Thymidylate Synthase

1997 ◽  
Vol 83 (1_suppl1) ◽  
pp. 79-79
Author(s):  
Alberto F. Sobrero ◽  
Alessandra Guglielmi ◽  
Alessio Tempestini ◽  
Chiara Baldo ◽  
Carlo Aschele
Keyword(s):  
Colorectal Cancer ◽  
Thymidylate Synthase ◽  
Advanced Colorectal Cancer ◽  
Cancer Inhibition
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