Targeting QPCTL: An Emerging Therapeutic Opportunity
文献类型：期刊论文
| 作者 | Yu, Lei4; Sun, Yaoliang3; Xie, Longyan4; Tan, Xiao4; Wang, Ping4; Xu, Shilin1,2,3 |
| 刊名 | JOURNAL OF MEDICINAL CHEMISTRY
 |
| 出版日期 | 2025-01-02 |
| 卷号 | 68期号:2页码:929-943 |
| ISSN号 | 0022-2623 |
| DOI | 10.1021/acs.jmedchem.4c02247 |
| 通讯作者 | Wang, Ping(wangp@tongji.edu.cn) ; Xu, Shilin(slxu@simm.ac.cn) |
| 英文摘要 | Glutaminyl cyclases, including glutaminyl-peptide cyclotransferase (QPCT) and glutaminyl-peptide cyclotransferase-like protein (QPCTL), primarily catalyze the cyclization of N-terminal glutamine or glutamate to pyroglutamate (pGlu). QPCTL, in particular, modifies the N-terminus of CD47, thereby regulating its interaction with signal-regulatory protein alpha (SIRP alpha) and modulating phagocytosis of tumor cells by immune cells. Additionally, QPCTL cyclizes the N-termini of CCL2, CCL7, and CX3CL1, influencing the tumor microenvironment and inflammatory responses in cancer and other disorders. Consequently, QPCTL is considered a valuable therapeutic target for several human diseases. However, the development of QPCTL inhibitors remains in its early stages. This perspective summarizes the structural features, catalytic mechanisms, and biological functions of QPCTL, along with its recent advances in small-molecule inhibitors. It provides valuable insights into the development of novel QPCTL inhibitors. |
| WOS关键词 | HUMAN GLUTAMINYL CYCLASE ; PYROGLUTAMIC ACID ; BONE-MARROW ; PROTEIN ; CHEMOKINE ; IDENTIFICATION ; INHIBITORS ; EXPRESSION ; CELLS ; INFLAMMATION |
| 资助项目 | National Natural Science Foundation of China[22207084] ; National Natural Science Foundation of China[22277128] ; National Natural Science Foundation of China[82341028] ; National Natural Science Foundation of China[22307132] ; National Natural Science Foundation of China[2020YFA0803201] ; National Natural Science Foundation of China[2022YFC3401500] ; National Natural Science Foundation of China[2023YFA1800804] ; National Key Research and Development Program of China |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:001388640400001 |
| 出版者 | AMER CHEMICAL SOC |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/315546]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Wang, Ping; Xu, Shilin |
| 作者单位 | 1.Univ Chinese Acad Sci, Beijing 100049, Peoples R China 2.Univ Chinese Acad Sci, Hangzhou Inst Adv Study, Sch Pharmaceut Sci & Technol, Hangzhou 310024, Peoples R China 3.Chinese Acad Sci, Shanghai Inst Mat Med, Dept Med Chem, Shanghai 201203, Peoples R China 4.Tongji Univ, Tongji Univ Canc Ctr, Shanghai Peoples Hosp 10, Sch Med, Shanghai 200092, Peoples R China |
| 推荐引用方式 GB/T 7714 | Yu, Lei,Sun, Yaoliang,Xie, Longyan,et al. Targeting QPCTL: An Emerging Therapeutic Opportunity[J]. JOURNAL OF MEDICINAL CHEMISTRY,2025,68(2):929-943. |
| APA | Yu, Lei,Sun, Yaoliang,Xie, Longyan,Tan, Xiao,Wang, Ping,&Xu, Shilin.(2025).Targeting QPCTL: An Emerging Therapeutic Opportunity.JOURNAL OF MEDICINAL CHEMISTRY,68(2),929-943. |
| MLA | Yu, Lei,et al."Targeting QPCTL: An Emerging Therapeutic Opportunity".JOURNAL OF MEDICINAL CHEMISTRY 68.2(2025):929-943. |
入库方式： OAI收割
来源：上海药物研究所
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