Protein degradation technology: a strategic paradigm shift in drug discovery
文献类型：期刊论文
| 作者 | Li, Haobin1,2,3; Dong, Jinyun1,2; Cai, Maohua1,2,3; Xu, Zhiyuan1,2; Cheng, Xiang-Dong1,2; Qin, Jiang-Jiang1,2,3 |
| 刊名 | JOURNAL OF HEMATOLOGY & ONCOLOGY
 |
| 出版日期 | 2021-09-06 |
| 卷号 | 14 |
| 关键词 | Protein degradation Degradation pathway Degradation technology PROTAC Monomeric degraders |
| DOI | 10.1186/s13045-021-01146-7 |
| 通讯作者 | Dong, Jinyun(dongjy@ibmc.ac.cn) ; Cheng, Xiang-Dong(chengxd516@126.com) ; Qin, Jiang-Jiang(jqin@ucas.ac.cn) |
| 英文摘要 | Targeting pathogenic proteins with small-molecule inhibitors (SMIs) has become a widely used strategy for treating malignant tumors. However, most intracellular proteins have been proven to be undruggable due to a lack of active sites, leading to a significant challenge in the design and development of SMIs. In recent years, the proteolysis-targeting chimeric technology and related emerging degradation technologies have provided additional approaches for targeting these undruggable proteins. These degradation technologies show a tendency of superiority over SMIs, including the rapid and continuous target consumption as well as the stronger pharmacological effects, being a hot topic in current research. This review mainly focuses on summarizing the development of protein degradation technologies in recent years. Their advantages, potential applications, and limitations are also discussed. We hope this review would shed light on the design, discovery, and clinical application of drugs associated with these degradation technologies. |
| WOS关键词 | CYCLIN-DEPENDENT KINASES ; ANDROGEN RECEPTOR AR ; PROSTATE-CANCER ; TARGETED DEGRADATION ; RESISTANCE MECHANISMS ; NONCODING RNAS ; CDK INHIBITORS ; HIGHLY POTENT ; PROTEOLYSIS ; FAK |
| 资助项目 | Zhejiang Provincial Research Center for Upper Gastrointestinal Tract Cancer[JBZX-202006] ; Zhejiang Provincial Natural Science Foundation of China[LR21H280001] ; Zhejiang Provincial Natural Science Foundation of China[LQ21B020003] ; Program of Zhejiang Provincial TCM Sci-tech Plan[2020ZZ005] ; National Natural Science Foundation of China[81903842] ; National Natural Science Foundation of China[82103967] ; Beijing Medical Award Foundation[YXJL-2021-0388-0318] |
| WOS研究方向 | Oncology ; Hematology |
| 语种 | 英语 |
| 出版者 | BMC |
| WOS记录号 | WOS:000693259400001 |
| 资助机构 | Zhejiang Provincial Research Center for Upper Gastrointestinal Tract Cancer ; Zhejiang Provincial Natural Science Foundation of China ; Program of Zhejiang Provincial TCM Sci-tech Plan ; National Natural Science Foundation of China ; Beijing Medical Award Foundation |
| 源URL | [http://ir.hfcas.ac.cn:8080/handle/334002/125283]  |
| 专题 | 中国科学院合肥物质科学研究院 |
| 通讯作者 | Dong, Jinyun; Cheng, Xiang-Dong; Qin, Jiang-Jiang |
| 作者单位 | 1.Univ Chinese Acad Sci, Canc Hosp, Zhejiang Prov Res Ctr Upper Gastrointestinal Trac, Zhejiang Canc Hosp, Hangzhou 310022, Zhejiang, Peoples R China 2.Chinese Acad Sci, Inst Basic Med & Canc IBMC, Hangzhou 310018, Zhejiang, Peoples R China 3.Zhejiang Chinese Med Univ, Sch Pharmaceut Sci, Hangzhou 310053, Peoples R China |
| 推荐引用方式 GB/T 7714 | Li, Haobin,Dong, Jinyun,Cai, Maohua,et al. Protein degradation technology: a strategic paradigm shift in drug discovery[J]. JOURNAL OF HEMATOLOGY & ONCOLOGY,2021,14. |
| APA | Li, Haobin,Dong, Jinyun,Cai, Maohua,Xu, Zhiyuan,Cheng, Xiang-Dong,&Qin, Jiang-Jiang.(2021).Protein degradation technology: a strategic paradigm shift in drug discovery.JOURNAL OF HEMATOLOGY & ONCOLOGY,14. |
| MLA | Li, Haobin,et al."Protein degradation technology: a strategic paradigm shift in drug discovery".JOURNAL OF HEMATOLOGY & ONCOLOGY 14(2021). |
入库方式： OAI收割
来源：合肥物质科学研究院
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