A patent review of BRD4 inhibitors (2013-2019)
文献类型：期刊论文
| 作者 | Lu, Tian3,4; Lu, Wenchao1,2,3; Luo, Cheng2,3,4
|
| 刊名 | EXPERT OPINION ON THERAPEUTIC PATENTS
 |
| 出版日期 | 2020-01-02 |
| 卷号 | 30期号:1页码:57-81 |
| 关键词 | Bromodomain-containing protein 4 (BRD4) bromodomain and extra-terminal (BET) family small molecule inhibitors cancer patent therapeutic potential |
| ISSN号 | 1354-3776 |
| DOI | 10.1080/13543776.2020.1702645 |
| 通讯作者 | Luo, Cheng(cluo@mail.shcnc.ac.cn) |
| 英文摘要 | Introduction: The bromodomain-containing protein 4 (BRD4), a member of the bromodomain and extra-terminal (BET) family, functions as an 'epigenetic reader' that binds to acetylated lysine (KAc) residues on histone tails sophisticatedly regulating chromatin structure and gene expression. Recently, emerging evidence demonstrates that BRD4 plays a significant role in the occurrence and progression of several malignant human diseases especially cancers, making it a hot target in cancer therapy. Areas covered: This review mainly summarizes the patents of BRD4 inhibitors that have been authorized from 2013 to 2019. The patents are mostly described in terms of chemical structures, molecular mechanisms of action, pharmacological activities and potential clinical applications, including combination therapies. The development of BRD4 inhibitors in the clinical phase has been highlighted. Prospects for further development of more selective BRD4 inhibitors are provided. Expert opinion: In 2013-2019, several previously known chemical scaffolds have been further developed and disclosed. Although many small molecule BRD4 inhibitors with high potency and diverse scaffolds have been developed, the selectivity of most BRD4 inhibitors still needs to be improved. Therefore, the development of more selective small molecule inhibitors or combined use of drugs such as immunotherapy may provide new ideas for drug development. |
| WOS关键词 | BET BROMODOMAIN INHIBITORS ; P-TEFB ; DRUG DESIGN ; PROTEIN ; TARGET ; MYC ; RESISTANCE ; DISCOVERY ; DOMAIN ; IDENTIFICATION |
| 资助项目 | National Natural Science Foundation of China[81625022] ; National Natural Science Foundation of China[91853205] ; National Natural Science Foundation of China[81821005] ; National Science and Technology Major Project[2018ZX09711002] ; K. C. Wong Education Foundation ; Chinese Academy of Sciences[XDA12020353] ; Chinese Academy of Sciences[XDA12050401] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000502444100001 |
| 出版者 | TAYLOR & FRANCIS LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/282191]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Luo, Cheng |
| 作者单位 | 1.Dana Farber Canc Inst, Dept Canc Biol, Boston, MA 02115 USA 2.Univ Chinese Acad Sci, Dept Pharm, Beijing, Peoples R China 3.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai, Peoples R China 4.Nanjing Univ Chinese Med, Dept Pharm, Nanjing, Jiangsu, Peoples R China |
| 推荐引用方式 GB/T 7714 | Lu, Tian,Lu, Wenchao,Luo, Cheng. A patent review of BRD4 inhibitors (2013-2019)[J]. EXPERT OPINION ON THERAPEUTIC PATENTS,2020,30(1):57-81. |
| APA | Lu, Tian,Lu, Wenchao,&Luo, Cheng.(2020).A patent review of BRD4 inhibitors (2013-2019).EXPERT OPINION ON THERAPEUTIC PATENTS,30(1),57-81. |
| MLA | Lu, Tian,et al."A patent review of BRD4 inhibitors (2013-2019)".EXPERT OPINION ON THERAPEUTIC PATENTS 30.1(2020):57-81. |
入库方式： OAI收割
来源：上海药物研究所
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