{"title":"Sigma受体（无线电）配体的研究进展及其在肿瘤中的应用","authors":"Tao Wang*, Na Sun, Yanxi Ma and Song Zhang*, ","doi":"10.1021/acsptsci.4c0071110.1021/acsptsci.4c00711","DOIUrl":null,"url":null,"abstract":"<p >Cancer ranks among the top triumvirate leading causes of human deaths worldwide. The pathological mechanisms are notably intricate, demonstrating proliferative and metastatic capabilities, which complicate therapeutic interventions. The sigma-1 receptor (σ<sub>1</sub>R) plays a crucial role in tumor survival and migration, while the sigma-2 receptor (σ<sub>2</sub>R) is intimately associated with tumor proliferation. This review encapsulated the investigation concerning σ<sub>1</sub>R and σ<sub>2</sub>R in neoplasms and rigorously summarized the ligands and radio-ligands development and their tumor applications, such as antitumor cell proliferation and PET/SPECT imaging in tumors. A comprehensive classification discussion was undertaken regarding the chemical structures and emphasized the possibility of dual/multitargeted ligands. Ultimately, we discussed the effects of chiral structures and the pharmacological characteristics of ligands on affinity and pharmacokinetic features <i>in vivo</i>, particularly concerning radiopharmaceuticals. This review functions as a beneficial resource, fostering ligand deployment and stimulating the generation of innovative ideas for developing innovative radiopharmaceuticals.</p>","PeriodicalId":36426,"journal":{"name":"ACS Pharmacology and Translational Science","volume":"8 4","pages":"951–977 951–977"},"PeriodicalIF":4.9000,"publicationDate":"2025-03-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Recent Advances in the Development of Sigma Receptor (Radio)Ligands and Their Application in Tumors\",\"authors\":\"Tao Wang*, Na Sun, Yanxi Ma and Song Zhang*, \",\"doi\":\"10.1021/acsptsci.4c0071110.1021/acsptsci.4c00711\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p >Cancer ranks among the top triumvirate leading causes of human deaths worldwide. The pathological mechanisms are notably intricate, demonstrating proliferative and metastatic capabilities, which complicate therapeutic interventions. The sigma-1 receptor (σ<sub>1</sub>R) plays a crucial role in tumor survival and migration, while the sigma-2 receptor (σ<sub>2</sub>R) is intimately associated with tumor proliferation. This review encapsulated the investigation concerning σ<sub>1</sub>R and σ<sub>2</sub>R in neoplasms and rigorously summarized the ligands and radio-ligands development and their tumor applications, such as antitumor cell proliferation and PET/SPECT imaging in tumors. A comprehensive classification discussion was undertaken regarding the chemical structures and emphasized the possibility of dual/multitargeted ligands. Ultimately, we discussed the effects of chiral structures and the pharmacological characteristics of ligands on affinity and pharmacokinetic features <i>in vivo</i>, particularly concerning radiopharmaceuticals. This review functions as a beneficial resource, fostering ligand deployment and stimulating the generation of innovative ideas for developing innovative radiopharmaceuticals.</p>\",\"PeriodicalId\":36426,\"journal\":{\"name\":\"ACS Pharmacology and Translational Science\",\"volume\":\"8 4\",\"pages\":\"951–977 951–977\"},\"PeriodicalIF\":4.9000,\"publicationDate\":\"2025-03-07\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"ACS Pharmacology and Translational Science\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://pubs.acs.org/doi/10.1021/acsptsci.4c00711\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q1\",\"JCRName\":\"CHEMISTRY, MEDICINAL\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"ACS Pharmacology and Translational Science","FirstCategoryId":"1085","ListUrlMain":"https://pubs.acs.org/doi/10.1021/acsptsci.4c00711","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
Recent Advances in the Development of Sigma Receptor (Radio)Ligands and Their Application in Tumors
Cancer ranks among the top triumvirate leading causes of human deaths worldwide. The pathological mechanisms are notably intricate, demonstrating proliferative and metastatic capabilities, which complicate therapeutic interventions. The sigma-1 receptor (σ1R) plays a crucial role in tumor survival and migration, while the sigma-2 receptor (σ2R) is intimately associated with tumor proliferation. This review encapsulated the investigation concerning σ1R and σ2R in neoplasms and rigorously summarized the ligands and radio-ligands development and their tumor applications, such as antitumor cell proliferation and PET/SPECT imaging in tumors. A comprehensive classification discussion was undertaken regarding the chemical structures and emphasized the possibility of dual/multitargeted ligands. Ultimately, we discussed the effects of chiral structures and the pharmacological characteristics of ligands on affinity and pharmacokinetic features in vivo, particularly concerning radiopharmaceuticals. This review functions as a beneficial resource, fostering ligand deployment and stimulating the generation of innovative ideas for developing innovative radiopharmaceuticals.
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ACS Pharmacology & Translational Science publishes high quality, innovative, and impactful research across the broad spectrum of biological sciences, covering basic and molecular sciences through to translational preclinical studies. Clinical studies that address novel mechanisms of action, and methodological papers that provide innovation, and advance translation, will also be considered. We give priority to studies that fully integrate basic pharmacological and/or biochemical findings into physiological processes that have translational potential in a broad range of biomedical disciplines. Therefore, studies that employ a complementary blend of in vitro and in vivo systems are of particular interest to the journal. Nonetheless, all innovative and impactful research that has an articulated translational relevance will be considered.
ACS Pharmacology & Translational Science does not publish research on biological extracts that have unknown concentration or unknown chemical composition.
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