Beyond Inhibition: Recent Advances of Heterobifunctional Molecules Targeting CDK9
文献类型：期刊论文
| 作者 | Yin, Junzhe3,4; Zhang, Na2; Wang, Tian1; Zhang, Xuan3,4 |
| 刊名 | JOURNAL OF MEDICINAL CHEMISTRY
 |
| 出版日期 | 2025-10-25 |
| 页码 | 21 |
| ISSN号 | 0022-2623 |
| DOI | 10.1021/acs.jmedchem.5c02127 |
| 通讯作者 | Zhang, Xuan(zhangxuan@simm.ac.cn) |
| 英文摘要 | CDK9 is a pivotal kinase in transcriptional regulatory networks. It has emerged as a promising anticancer target because of its critical role in regulating key oncoproteins such as MYC and MCL-1. While CDK9 inhibitors have shown preclinical efficacy, their clinical translation faces challenges, including narrow therapeutic windows, limited monotherapy effectiveness, and drug resistance. Targeted protein degradation (TPD) strategies, particularly PROTACs that induce CDK9 ubiquitination and degradation, offer a promising solution. These PROTACs exhibit potent and sustained antitumor effects, effectively overcoming resistance mechanisms such as MYC upregulation. Additionally, innovative approaches employing heterobifunctional molecules across various modalities have been extensively explored to target CDK9, expanding the therapeutic potential through multiple mechanisms. These advances hold promise for establishing a new paradigm in the treatment of transcriptionally addicted cancers. |
| WOS关键词 | CYCLIN-DEPENDENT KINASE ; HEMATOLOGICAL MALIGNANCIES ; SOLID TUMORS ; P-TEFB ; POTENT ; FLAVOPIRIDOL ; ENITOCICLIB ; DISCOVERY ; LYMPHOMA ; AZD4573 |
| 资助项目 | National Natural Science Foundation of China[22277131] ; National Natural Science Foundation of China ; CAS Pioneer Hundred Talents Program |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:001600365400001 |
| 出版者 | AMER CHEMICAL SOC |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/320480]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Zhang, Xuan |
| 作者单位 | 1.Nanjing Univ Chinese Med, Sch Chinese Mat Med, Nanjing 210023, Peoples R China 2.Shenyang Pharmaceut Univ, Sch Pharmaceut Engn, Shenyang 110016, Peoples R China 3.Univ Chinese Acad Sci, Beijing 100049, Peoples R China 4.Chinese Acad Sci, Shanghai Inst Mat Med, Drug Discovery & Dev Ctr, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Yin, Junzhe,Zhang, Na,Wang, Tian,et al. Beyond Inhibition: Recent Advances of Heterobifunctional Molecules Targeting CDK9[J]. JOURNAL OF MEDICINAL CHEMISTRY,2025:21. |
| APA | Yin, Junzhe,Zhang, Na,Wang, Tian,&Zhang, Xuan.(2025).Beyond Inhibition: Recent Advances of Heterobifunctional Molecules Targeting CDK9.JOURNAL OF MEDICINAL CHEMISTRY,21. |
| MLA | Yin, Junzhe,et al."Beyond Inhibition: Recent Advances of Heterobifunctional Molecules Targeting CDK9".JOURNAL OF MEDICINAL CHEMISTRY (2025):21. |
入库方式： OAI收割
来源：上海药物研究所
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