Small-Molecule Probe [68Ga]Ga-SMIC-2501 Targeting the V-Domain Immunoglobulin Suppressor of T Cell Activation Protein for Positron Emission Tomography Imaging
文献类型：期刊论文
| 作者 | Wang, Gang9,10; Cao, Rui9; Liu, Shumei8; Qian, Kun9; Sun, Luming7,9; Tian, Jin6,9; Wang, Tao5,9; Zhang, Wenqing4,9; Huang, Linghui3,9; Jiang, Yuanpeng4,9 |
| 刊名 | MOLECULAR PHARMACEUTICS
 |
| 出版日期 | 2025-06-03 |
| 页码 | 11 |
| 关键词 | VISTA immunecheckpoint immunotherapy PET tumor microenvironment molecular imaging |
| ISSN号 | 1543-8384 |
| DOI | 10.1021/acs.molpharmaceut.5c00531 |
| 通讯作者 | Qu, Chunrong(crqu@simm.ac.cn) ; Ma, Hongjuan(hongjuanma@shu.edu.cn) ; Cheng, Zhen(zcheng@simm.ac.cn) |
| 英文摘要 | V-domain immunoglobulin suppressor of T cell activation (VISTA) inhibits T-cell effector functions and helps tumor immune evasion, making it an important biomarker and therapeutic target in cancer immunotherapy. To facilitate VISTA-targeted strategy development and enable the accurate detection of tumor VISTA expression, a novel small-molecule probe [68Ga]Ga-SMIC-2501 was developed for noninvasive imaging. The radiochemical purity was over 95%, with a radiochemical yield of around 90%. [68Ga]Ga-SMIC-2501 demonstrated good in vitro stability at room temperature in physiological saline and fetal bovine serum for 2 h tested. WB results showed that VISTA expression in B16-F10 tumor cells was higher than that in CT26 and MC38 cells. [68Ga]Ga-SMIC-2501 accumulated in tumors in both high (B16-F10) and moderate (CT26) VISTA-expression animal models, with uptake levels of 2.53 +/- 0.55% and 1.89 +/- 0.38% ID/g, respectively. In blocking experiments, tumor uptake was 1.56 +/- 0.20% ID/g, and the inhibition rate reached 36%. Immunohistochemistry (IHC) analysis showed that VISTA expression levels were positively correlated with [68Ga]Ga-SMIC-2501 uptake in tumors, with a correlation coefficient greater than 0.75. [68Ga]Ga-SMIC-2501 shows high potential as a novel molecular tool for imaging VISTA-positive tumors and expression. It provides a foundation for the future development of VISTA-based cancer theranostic agents and guidance for VISTA-targeted immunotherapy. |
| WOS关键词 | IMMUNE-CHECKPOINT ; VISTA ; ANTIBODY ; THERAPY ; DISEASE |
| 资助项目 | National Natural Science Foundation of China[U2267221] ; National Natural Science Foundation of China[82472091] ; National Natural Science Foundation of China[12475346] ; Shanghai Municipal Science and Technology Major Project[TM202301H003] ; Natural Science Foundation of Shanghai[24ZR1477300] ; State Key Laboratory of Drug Research[SIMM0120231004] ; Natural Science Foundation of Ningbo Municipality[2024Z214] ; Gansu Science and Technology Major Project[23ZDFA014] ; Shandong Laboratory Program[SYS202205] |
| WOS研究方向 | Research & Experimental Medicine ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:001501782700001 |
| 出版者 | AMER CHEMICAL SOC |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/318243]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Qu, Chunrong; Ma, Hongjuan; Cheng, Zhen |
| 作者单位 | 1.Shandong First Med Univ & Shandong Acad Med Sci, Jinan 250117, Peoples R China 2.Bohai Rim Adv Res Inst Drug Discovery, Shandong Lab Yantai Drug Discovery, Yantai 264117, Shandong, Peoples R China 3.China Pharmaceut Univ, Sch Pharm, Nanjing 211198, Peoples R China 4.Univ Chinese Acad Sci, Sch Pharm, Beijing 100049, Peoples R China 5.Fudan Univ, Sch Pharm, Shanghai 201203, Peoples R China 6.Wuyi Univ, Sch Pharm & Food Engn, Jiangmen 529020, Peoples R China 7.Henan Univ, Sch Pharm, Kaifeng 475004, Peoples R China 8.Nanjing Univ Chinese Med, Sch Chinese Mat Med, Nanjing 210023, Peoples R China 9.Chinese Acad Sci, Mol Imaging Ctr, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China 10.Shanghai Univ, Shanghai Appl Radiat Inst, Sch Environm & Chem Engn, Shanghai 200444, Peoples R China |
| 推荐引用方式 GB/T 7714 | Wang, Gang,Cao, Rui,Liu, Shumei,et al. Small-Molecule Probe [68Ga]Ga-SMIC-2501 Targeting the V-Domain Immunoglobulin Suppressor of T Cell Activation Protein for Positron Emission Tomography Imaging[J]. MOLECULAR PHARMACEUTICS,2025:11. |
| APA | Wang, Gang.,Cao, Rui.,Liu, Shumei.,Qian, Kun.,Sun, Luming.,...&Cheng, Zhen.(2025).Small-Molecule Probe [68Ga]Ga-SMIC-2501 Targeting the V-Domain Immunoglobulin Suppressor of T Cell Activation Protein for Positron Emission Tomography Imaging.MOLECULAR PHARMACEUTICS,11. |
| MLA | Wang, Gang,et al."Small-Molecule Probe [68Ga]Ga-SMIC-2501 Targeting the V-Domain Immunoglobulin Suppressor of T Cell Activation Protein for Positron Emission Tomography Imaging".MOLECULAR PHARMACEUTICS (2025):11. |
入库方式： OAI收割
来源：上海药物研究所
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