The structure based design of dual HDAC/BET inhibitors as novel epigenetic probes

MedChemComm ◽  
2014 ◽  
Vol 5 (3) ◽  
pp. 342-351 ◽  
Author(s):  
Stephen J. Atkinson ◽  
Peter E. Soden ◽  
Davina C. Angell ◽  
Marcus Bantscheff ◽  
Chun-wa Chung ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Cell Lysate ◽  
Bet Inhibitors ◽  
Hdac Proteins

DUAL946 (1) inhibits BET and HDAC proteins in chemoproteomic cell lysate experiments and in immune and cancer cells.

BAP1 loss augments sensitivity to BET inhibitors in cancer cells

2021 ◽  
Author(s):  
Yu-yan Xu ◽  
Zhong-lu Ren ◽  
Xiao-lian Liu ◽  
Gui-ming Zhang ◽  
Si-si Huang ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Bet Inhibitors

SNAIL- and SLUG-induced side population phenotype of HCT116 human colorectal cancer cells and its regulation by BET inhibitors

2020 ◽  
Vol 521 (1) ◽  
pp. 152-157 ◽  
Author(s):  
Yu Kato ◽  
Shingo Kondo ◽  
Taira Itakura ◽  
Miku Tokunaga ◽  
Shiori Hatayama ◽  
...  
Keyword(s):  
Colorectal Cancer ◽  
Cancer Cells ◽  
Side Population ◽  
Human Colorectal Cancer ◽  
Bet Inhibitors ◽  
Colorectal Cancer Cells ◽  
Human Colorectal Cancer Cells

Human telomerase reverse transcriptase in papillary thyroid cancer: gene expression, effects of silencing and regulation by BET inhibitors in thyroid cancer cells

Endocrine ◽  
2019 ◽  
Vol 63 (3) ◽  
pp. 545-553 ◽  
Author(s):  
Valentina Maggisano ◽  
Marilena Celano ◽  
Saverio Massimo Lepore ◽  
Marialuisa Sponziello ◽  
Francesca Rosignolo ◽  
...  
Keyword(s):  
Gene Expression ◽  
Thyroid Cancer ◽  
Cancer Cells ◽  
Telomerase Reverse Transcriptase ◽  
Cancer Gene ◽  
Papillary Thyroid ◽  
Human Telomerase Reverse Transcriptase ◽  
Bet Inhibitors ◽  
Human Telomerase ◽  
Thyroid Cancer Cells

scholarly journals BET Inhibitors Potentiate Chemotherapy and Killing of SPOP-Mutant Colon Cancer Cells via Induction of DR5

2019 ◽  
Vol 79 (6) ◽  
pp. 1191-1203 ◽  
Author(s):  
Xiao Tan ◽  
Jingshan Tong ◽  
Yi-Jun Wang ◽  
Rochelle Fletcher ◽  
Robert E. Schoen ◽  
...  
Keyword(s):  
Colon Cancer ◽  
Cancer Cells ◽  
Colon Cancer Cells ◽  
Bet Inhibitors

scholarly journals Inhibition of Colorectal Cancer Cells HT-29 by Secretome and Extraction of Human Umbilical Cord Wharton’s Jelly Stem Cells

2021 ◽  
Author(s):  
Mahdieh Farhoudi Sefidan Jadid ◽  
Parisa Emami ◽  
Pouya Goleij ◽  
Vahidreza Karamad ◽  
Afshin Khorrami ◽  
...  
Keyword(s):  
Colorectal Cancer ◽  
Stem Cells ◽  
Cancer Cells ◽  
Cell Line ◽  
Conditioned Medium ◽  
Umbilical Cord ◽  
Human Umbilical Cord ◽  
Apoptosis Induction ◽  
Cell Lysate ◽  
Ht 29

Abstract Background and aim: Colorectal cancer (CC) is aggressive cancer and the major cause of death worldwide that need the development of novel and effective therapeutic methods. Recently suggested that the human Wharton’s jelly stem cells (hWJSCs) have an anti-proliferation activity against of several cancer cells through apoptosis induction. Therefore, this study aimed to investigate the effects of conditioned medium and cell lysate of human umbilical cord hWJSCs against the HT-29 cancer cell line and mechanisms of apoptosis induction.Methods: In this study, the hWJSCs conditioned medium and cell lysate were prepared from 10 human umbilical cord samples. The effects of hWJSCs conditioned medium and cell lysate were evaluated on the viability, migration, invasion, and apoptosis of HT-29 CC cell line. The expression of apoptosis related BAX, BCL2, SMAC, SURVIVIN, and Cas9 genes were evaluated in CC cells treated with hWJSCs conditioned medium and cell lysate.Results: We observed that conditioned medium and cell lysate of hWJSCs decrease CC cells viability, proliferation, migration, and invasion in a concentration- and time-dependent manner. Moreover, conditioned medium and cell lysate increased apoptosis rate of CC cells, which can be due to increase BAX, SMAC, and Cas9 genes, as well as decrease BCL2 and SURVIVIN genes.Conclusions: Our study suggest that conditioned medium and cell lysate of hWJSCs can inhibit CC cells through induction of apoptosis. However, further studies on are required to more accurate results.

scholarly journals BET inhibitors induce apoptosis through ATAD2 suppression in AR positive triple negative breast cancer cells

2017 ◽  
Vol 28 ◽  
pp. x4
Author(s):  
H. Yang ◽  
S.H. Shim ◽  
K.S. Lee ◽  
I.H. Park
Keyword(s):  
Breast Cancer ◽  
Cancer Cells ◽  
Triple Negative Breast Cancer ◽  
Breast Cancer Cells ◽  
Triple Negative ◽  
Bet Inhibitors

scholarly journals Effects of BET Inhibitor JQ1 and Interleukin-6 on Breast Cancer Cells

2021 ◽  
Author(s):  
Atefeh Sharif Hoseini ◽  
Masoud Heshmati ◽  
Amin Soltani ◽  
Hedayatollah Shirzad ◽  
Morteza Sedehi ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cancer Cells ◽  
Breast Cancer Cells ◽  
Therapeutic Targets ◽  
Surface Expression ◽  
Inhibitory Effect ◽  
Dependent Manner ◽  
Breast Cancers ◽  
Bet Inhibitors ◽  
Mcf 7

Abstract Bromodomain and extra-terminal (BET) proteins are recognized acetylated lysine of histone 4 and act as scaffolds to recruit many other proteins to promoters and at enhancers of active genes, especially at the super-enhancers of key genes, driving the transcription process and have been identified as potential therapeutic targets in breast cancer. However, the efficacy of BET inhibitors such as JQ1 in breast cancer therapy is impeded by IL-6 through an as yet defined mechanism. We investigated the interplay between IL-6 and JQ1 in MCF-7 and MDA-MB-231 human breast cancer cells. Here we demonstrate that the efficacy of JQ1 on the inhibition of cell growth and apoptosis was stronger in MDA-MB-231 cells than in MCF-7 cells. Further, MCF-7 cells, but not MDA-MB-231 cells, exhibited increased expression of CXCR4 following IL-6 treatment. JQ1 significantly reduced CXCR4 surface expression in both cell lines and diminished the effects of IL-6 pre-treatment on MCF-7 cells. While IL-6 suppressed the extension of breast cancer stem cells (BCSCs) in MCF-7 cells, JQ1 impeded its inhibitory effect. In addition, in MCF-7 cells JQ1 increased the number of senescent cells in a time-dependent manner. Analysis of gene expression indicated that JQ1 and IL-6 synergistically increase SNAIL expression and decrease c-MYC expression in MCF-7 cells. So, the BET proteins are promising, novel therapeutic targets in late-stage breast cancers.

Abstract 2989: BET inhibitors induce Rac1-dependent MNK and eIF4E phosphorylation in cancer cells

2018 ◽  
Author(s):  
Thao Pham ◽  
Brian T. Decant ◽  
Krishan Kumar ◽  
Meng Shang ◽  
Maria Matsangou ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Bet Inhibitors
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