Abstract：
UNASSIGNED: Bromodomain and ExtraTerminal (BET) domain proteins are transcriptional cofactors that, recognizing acetylated lysines of histone and non-histone proteins, can modulate gene expression. The BET family consists of four members, each of which contains two bromodomains (BD1 and BD2) able to recognize the acetylated mark. Pan-BET inhibitors (BETi) have shown a promising anticancer potential in many clinical trials; however, their further development has been in part hampered by the side effects due to their lack of selectivity. Mounting evidence suggests that BD1 is primarily involved in cancer and that its selective inhibition can phenocopy the anticancer effects of pan-BETi with increased tolerability. Therefore, the development of BD1 selective inhibitors is highly pursed in both academia and industry.
UNASSIGNED: This review aims at giving an overview of the patent literature of BD1-selective BETi between 2014 and 2023. WIPO, USPTO, EPO, and SciFinder® databases were used for the search of patents.
UNASSIGNED: The development of BD1-selective BETi, despite challenging, is highly desirable as it could have a great impact on the development of new safer anticancer therapeutics. Several strategies could be applied to discover potent and selective compounds with limited side effects.
UNASSIGNED: This review aims at giving an overview of the patent literature of BD1-selective BETi between 2014 and 2023. WIPO, USPTO, EPO, and SciFinder® databases were used for the search of patents.
UNASSIGNED: The development of BD1-selective BETi, despite challenging, is highly desirable as it could have a great impact on the development of new safer anticancer therapeutics. Several strategies could be applied to discover potent and selective compounds with limited side effects.
摘要：
■溴结构域和末端外（BET）结构域蛋白是转录辅因子，识别组蛋白和非组蛋白蛋白的乙酰化赖氨酸，可以调节基因表达。BET家族由四名成员组成，每个都包含两个能够识别乙酰化标记的溴结构域（BD1和BD2）。Pan-BET抑制剂（BETi）在许多临床试验中显示出有希望的抗癌潜力；然而，由于缺乏选择性，它们的进一步发展部分受到副作用的阻碍。越来越多的证据表明，BD1主要参与癌症，其选择性抑制可以通过增加的耐受性来表现pan-BETi的抗癌作用。因此,BD1选择性抑制剂的开发在学术界和工业界都受到高度关注。
■这篇综述旨在概述BD1-选择性BETi在2014年至2023年之间的专利文献。WIPO,美国专利商标局,EPO,和SciFinder®数据库用于专利检索。
■BD1选择性BETi的发展，尽管具有挑战性，是非常可取的，因为它可能对开发新的更安全的抗癌疗法产生重大影响。可以应用几种策略来发现具有有限副作用的有效和选择性化合物。
■这篇综述旨在概述BD1-选择性BETi在2014年至2023年之间的专利文献。WIPO,美国专利商标局,EPO,和SciFinder®数据库用于专利检索。
■BD1选择性BETi的发展，尽管具有挑战性，是非常可取的，因为它可能对开发新的更安全的抗癌疗法产生重大影响。可以应用几种策略来发现具有有限副作用的有效和选择性化合物。
