Literature DB >> 28062533

BET Bromodomain Proteins as Cancer Therapeutic Targets.

Shaokun Shu1, Kornelia Polyak1.   

Abstract

Epigenetic regulators are emerging therapeutic targets in a wide variety of human cancers. BET bromodomain proteins have been identified as key regulators of oncogenic transcription factors including MYC; therefore, their inhibition might provide a way to block these "undruggable" targets. Several BET bromodomain inhibitors are in clinical development with promising preliminary findings. However, tumors acquire resistance to these agents in several different ways. In this review, we summarize the role that BET bromodomain proteins play in tumorigenesis as well as the molecular mechanisms underlying therapeutic responses and resistance to their inhibition with emphasis on BRD4 and breast cancer.
© 2016 Shu and Polyak; Published by Cold Spring Harbor Laboratory Press.

Entities:  

Mesh：

Substances：

Year:  2017        PMID： 28062533     DOI： 10.1101/sqb.2016.81.030908

Source DB:  PubMed          Journal:  Cold Spring Harb Symp Quant Biol        ISSN： 0091-7451


  28 in total

1.  Normal Breast-Derived Epithelial Cells with Luminal and Intrinsic Subtype-Enriched Gene Expression Document Interindividual Differences in Their Differentiation Cascade.

Authors:  Brijesh Kumar; Mayuri Prasad; Poornima Bhat-Nakshatri; Manjushree Anjanappa; Maitri Kalra; Natascia Marino; Anna Maria Storniolo; Xi Rao; Sheng Liu; Jun Wan; Yunlong Liu; Harikrishna Nakshatri
Journal:  Cancer Res       Date:  2018-07-11       Impact factor: 12.701

2.  Dual Inhibition of TAF1 and BET Bromodomains from the BI-2536 Kinase Inhibitor Scaffold.

Authors:  David Remillard; Dennis L Buckley; Hyuk-Soo Seo; Fleur M Ferguson; Sirano Dhe-Paganon; James E Bradner; Nathanael S Gray
Journal:  ACS Med Chem Lett       Date:  2019-09-13       Impact factor: 4.345

Review 3.  Twenty years of menin: emerging opportunities for restoration of transcriptional regulation in MEN1.

Authors:  Koen M A Dreijerink; H T Marc Timmers; Myles Brown
Journal:  Endocr Relat Cancer       Date:  2017-08-15       Impact factor: 5.678

4.  Modeling combination therapy for breast cancer with BET and immune checkpoint inhibitors.

Authors:  Xiulan Lai; Andrew Stiff; Megan Duggan; Robert Wesolowski; William E Carson; Avner Friedman
Journal:  Proc Natl Acad Sci U S A       Date:  2018-05-07       Impact factor: 11.205

5.  Synthetic Lethal and Resistance Interactions with BET Bromodomain Inhibitors in Triple-Negative Breast Cancer.

Authors:  Shaokun Shu; Hua-Jun Wu; Jennifer Y Ge; Rhamy Zeid; Isaac S Harris; Bojana Jovanović; Katherine Murphy; Binbin Wang; Xintao Qiu; Jennifer E Endress; Jaime Reyes; Klothilda Lim; Alba Font-Tello; Sudeepa Syamala; Tengfei Xiao; Chandra Sekhar Reddy Chilamakuri; Evangelia K Papachristou; Clive D'Santos; Jayati Anand; Kunihiko Hinohara; Wei Li; Thomas O McDonald; Adrienne Luoma; Rebecca J Modiste; Quang-De Nguyen; Brittany Michel; Paloma Cejas; Cigall Kadoch; Jacob D Jaffe; Kai W Wucherpfennig; Jun Qi; X Shirley Liu; Henry Long; Myles Brown; Jason S Carroll; Joan S Brugge; James Bradner; Franziska Michor; Kornelia Polyak
Journal:  Mol Cell       Date:  2020-05-15       Impact factor: 17.970

Review 6.  MYC and RAF: Key Effectors in Cellular Signaling and Major Drivers in Human Cancer.

Authors:  Eduard Stefan; Klaus Bister
Journal:  Curr Top Microbiol Immunol       Date:  2017       Impact factor: 4.291

7.  BRD4 Regulates Transcription Factor ΔNp63α to Drive a Cancer Stem Cell Phenotype in Squamous Cell Carcinomas.

Authors:  Matthew L Fisher; Seamus Balinth; Yon Hwangbo; Caizhi Wu; Carlos Ballon; John E Wilkinson; Gary L Goldberg; Alea A Mills
Journal:  Cancer Res       Date:  2021-10-25       Impact factor: 13.312

Review 8.  The Role of Bromodomain Testis-Specific Factor, BRDT, in Cancer: A Biomarker and A Possible Therapeutic Target.

Authors:  Ekaterina Bourova-Flin; Florent Chuffart; Sophie Rousseaux; Saadi Khochbin
Journal:  Cell J       Date:  2017-05-17       Impact factor: 2.479

9.  Bidirectional Regulatory Cross-Talk between Cell Context and Genomic Aberrations Shapes Breast Tumorigenesis.

Authors:  Brijesh Kumar; Poornima Bhat-Nakshatri; Calli Maguire; Max Jacobsen; Constance J Temm; George Sandusky; Harikrishna Nakshatri
Journal:  Mol Cancer Res       Date:  2021-07-20       Impact factor: 5.852

10.  Nitric oxide antagonism to glioblastoma photodynamic therapy and mitigation thereof by BET bromodomain inhibitor JQ1.

Authors:  Jonathan M Fahey; Jennifer S Stancill; Brian C Smith; Albert W Girotti
Journal:  J Biol Chem       Date:  2018-02-12       Impact factor: 5.486
View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.