{"title":"Targeting BET Bromodomains in Cancer","authors":"P. Trojer","doi":"10.1146/annurev-cancerbio-070120-103531","DOIUrl":null,"url":null,"abstract":"Cancer is frequently dependent on aberrant gene expression programs that might be vulnerable to targeting with novel therapeutics. Bromodomain and extraterminal domain (BET) proteins are powerful transcriptional coregulators often found as part of oncogenic transcriptional programs. The bromodomain functionality of BET proteins is highly druggable, and several product candidates are in clinical testing. While initial clinical data created doubt about their benefit for cancer patients, more encouraging data recently reported in myelofibrosis patients may promote additional applications of BET inhibitors in oncology as monotherapy and in combination with other therapeutic agents. Moreover, a growing number of approaches to optimize the therapeutic window by tinkering with the property profiles of BET inhibitors may provide additional clinical opportunities. This review provides an update on the status of ongoing activities to exploit BET bromodomain inhibition as a mechanism for cancer therapy. Expected final online publication date for the Annual Review of Cancer Biology, Volume 6 is April 2022. Please see http://www.annualreviews.org/page/journal/pubdates for revised estimates.","PeriodicalId":54233,"journal":{"name":"Annual Review of Cancer Biology-Series","volume":"1 1","pages":""},"PeriodicalIF":4.7000,"publicationDate":"2022-01-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"9","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Annual Review of Cancer Biology-Series","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1146/annurev-cancerbio-070120-103531","RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"ONCOLOGY","Score":null,"Total":0}
引用次数: 9
Abstract
Cancer is frequently dependent on aberrant gene expression programs that might be vulnerable to targeting with novel therapeutics. Bromodomain and extraterminal domain (BET) proteins are powerful transcriptional coregulators often found as part of oncogenic transcriptional programs. The bromodomain functionality of BET proteins is highly druggable, and several product candidates are in clinical testing. While initial clinical data created doubt about their benefit for cancer patients, more encouraging data recently reported in myelofibrosis patients may promote additional applications of BET inhibitors in oncology as monotherapy and in combination with other therapeutic agents. Moreover, a growing number of approaches to optimize the therapeutic window by tinkering with the property profiles of BET inhibitors may provide additional clinical opportunities. This review provides an update on the status of ongoing activities to exploit BET bromodomain inhibition as a mechanism for cancer therapy. Expected final online publication date for the Annual Review of Cancer Biology, Volume 6 is April 2022. Please see http://www.annualreviews.org/page/journal/pubdates for revised estimates.
期刊介绍：
The Annual Review of Cancer Biology offers comprehensive reviews on various topics within cancer research, covering pivotal and emerging areas in the field. As our understanding of cancer's fundamental mechanisms deepens and more findings transition into targeted clinical treatments, the journal is structured around three main themes: Cancer Cell Biology, Tumorigenesis and Cancer Progression, and Translational Cancer Science. The current volume of this journal has transitioned from gated to open access through Annual Reviews' Subscribe to Open program, ensuring all articles are published under a CC BY license.
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