首页|靶向人滋养层细胞表面糖蛋白抗原2的抗肿瘤药物研究进展

靶向人滋养层细胞表面糖蛋白抗原2的抗肿瘤药物研究进展

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目的 探讨人滋养层细胞表面糖蛋白抗原2(Trop2)结构与其在肿瘤增殖、迁移、侵袭和转移有关的信号通路中的功能,以及靶向Trop 2的抗肿瘤药物研究进展.方法 以"人滋养层细胞表面糖蛋白抗原2、靶向治疗、肿瘤、抗体偶联药物、放射免疫治疗"为中文关键词,以"Trop 2、targeted therapy、tumors、antibody-drug conjugates、radioimmunotherapy"为英文关键词,检索中国知网、PubMed数据库1997-2023年发表的相关文献,纳入标准:(1)Trop 2结构及功能;(2)靶向Trop 2的抗体偶联类药物;(3)放射性标记靶向Trop 2的药物;(4)靶向Trop 2的光免疫疗法.排除标准:(1)与肿瘤相关性差;(2)无法得到全文;(3)临床前抗体偶联类药物(ADCs)的相关文献.最终纳入65篇文献.结果 Trop 2是一种跨膜蛋白,不仅可以作为多种癌症的预测因子,通过各种信号通路控制细胞生长和扩散,还在多种实体瘤肿瘤细胞表面高表达,在正常组织中的表达极低.靶向Trop 2的ADCs主要有Sacituzumab govitecan、Datopotamab、deruxtecan(DS-1062)、SKB-264、DAC-002(JS-108)、ESG-401、FDA018、BAT-8003、RN927C(PF-06664178),主要用于治疗晚期或转移性三阴性乳腺癌,泌尿道上皮癌、非小细胞肺癌,乳腺癌、胃癌、小细胞肺癌和胰腺癌等实体肿瘤.靶向Trop 2的非ADCs主要包括(Rap)2-E1-(Rap)2、放射性标记药物和光免疫疗法等.Trop 2已成为精准医学的新靶点,如放射性核素、毒素和特异性抗体偶联结合成的药物等.结论 靶向Trop 2的抗肿瘤药物研究在ADCs、放射性药物、光免疫疗法等方面取得了一定进展,目前多种药物已获批上市或处于临床试验阶段.同时,靶向Trop 2的药物联合治疗展现出良好的研究前景.
Research progress of anti-tumor drugs targeting trophoblast cell surface antigen 2
Objective To investigate the structure of trophoblast cell surface antigen 2(Trop 2)and its signaling pathways involved in tumor proliferation,migration,invasion and metastasis,and the development of anti-tumor drugs targeting Trop 2.Methods The key words such as"Trop 2,targeted therapy,tumors,antibody-drug conjugates,radioimmunotherapy"were retrieved in CNKI,PubMed databases,mainly focusing on the related literature from 1997 to 2023.The criteria for selection were:(1)The structure and function of Trop 2;(2)Antibody-drug conjugates targeting Trop 2;(3)Radiolabeled drugs targeting Trop 2;(4)Photoimmunotherapy targeting Trop 2.The exclusion criteria were:(1)Poor correlation with tumor;(2)Unfull text;(3)Pre-clinical ADC drugs,and 65 articles were included.Results Trop 2 is a transmembrane protein that not only serves as a predictive factor for various types of cancer,controlling cell growth and diffusion through various signaling pathways,but also has high ex-pression on the surface of various solid tumor cells and extremely low expression in normal tissues.ADCs targeting Trop 2 mainly include Sacituzumab govitecan,Datopotamab,deruxtecan(DS-1062),SKB-264,DAC-002(JS-108),ESG-401,FDA018,BAT-8003 and RN927C(PF-06664178),which are mainly used to treat advanced or metastatic triple negative breast cancer,upper u-rinary tract cancer,non small cell lung cancer,breast cancer,gastric cancer,small cell lung cancer,pancreatic cancer and other solid tumors.The non ADC drugs targeting Trop 2 mainly include(Rap)2-E1-(Rap)2,radiopharmaceuticals,and photoimmuno-therapy.Trop 2 has become a new target for precision medicine,such as drugs synthesized by coupling radioactive isotopes,tox-ins,and specific antibodies.Conclusion The research on anti-tumor drugs targeting Trop 2 has made some achievements in ADCs,radiopharmaceuticals,photoimmunotherapy.At present,several drugs have been approved for marketing or are in clini-cal trials.At the same time,the drug combination therapy targeting Trop 2 shows a good research prospect.

trophoblast cell surface antigen 2targeted therapytumorsantibody-drug conjugatesradioimmunotherapy

鲍莹、樊彩云、唐显

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中国原子能科学研究院核技术综合研究所,北京 102413

人滋养层细胞表面糖蛋白抗原2 靶向治疗 肿瘤 抗体偶联药物 放射免疫治疗

2024

中华肿瘤防治杂志
中华预防医学会 山东省肿瘤防治研究院

中华肿瘤防治杂志

CSTPCD北大核心
影响因子:1.292
ISSN:1673-5269
年,卷(期):2024.31(18)