靶向癌症中的β-溴代胺

IF 4.7 2区医学 Q1 ONCOLOGY

Annual Review of Cancer Biology-Series Pub Date : 2022-01-18 DOI:10.1146/annurev-cancerbio-070120-103531

P. Trojer

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引用次数: 9

摘要

癌症经常依赖于异常基因表达程序，这些程序可能容易被新疗法靶向。溴代和末端外结构域（BET）蛋白是强大的转录辅助调节因子，通常作为致癌转录程序的一部分被发现。BET蛋白的溴结构域功能是高度可药用的，一些候选产品正在临床测试中。虽然最初的临床数据对其对癌症患者的益处产生了怀疑，但最近在骨髓纤维化患者中报道的更令人鼓舞的数据可能会促进BET抑制剂作为单一疗法和与其他治疗剂联合在肿瘤学中的更多应用。此外，越来越多的方法通过修改BET抑制剂的特性来优化治疗窗口，这可能会提供额外的临床机会。这篇综述提供了正在进行的利用BET溴结构域抑制作为癌症治疗机制的活动的最新情况。《癌症生物学年度评论》第6卷预计最终在线出版日期为2022年4月。请参阅http://www.annualreviews.org/page/journal/pubdates用于修订估算。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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Targeting BET Bromodomains in Cancer

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.

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来源期刊

Annual Review of Cancer Biology-Series Medicine-Oncology

CiteScore

14.50

自引率

1.30%

发文量

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.