Recent Advances in the Development of Sigma Receptor (Radio)Ligands and Their Application in Tumors

被引：0
|
作者：
Wang, Tao [1 ,2 ,3 ]
Sun, Na [1 ]
Ma, Yanxi [1 ]
Zhang, Song [1 ]
机构：
[1] Army Med Univ, XinQiao Hosp, Dept Nucl Med, Chongqing 400037, Peoples R China
[2] North Sichuan Med Coll, Sch Med Imaging, Nanchong 637100, Peoples R China
[3] North Sichuan Med Coll, Dept Nucl Med, Affiliated Hosp, Nanchong 637000, Peoples R China
来源：
ACS PHARMACOLOGY & TRANSLATIONAL SCIENCE | 2025年
关键词：
Sigma-1; receptor; Sigma-2; Medicinalchemistry; Tumor; (Radio)Ligands; LIGAND LU 28-179; IN-VIVO; BIOLOGICAL EVALUATION; BREAST-CANCER; HUMAN BRAIN; ENDOPLASMIC-RETICULUM; BENZAMIDE ANALOGS; STEROL ISOMERASE; CELL-GROWTH; BINDING;
D O I：
10.1021/acsptsci.4c00711
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
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 (sigma 1R) plays a crucial role in tumor survival and migration, while the sigma-2 receptor (sigma 2R) is intimately associated with tumor proliferation. This review encapsulated the investigation concerning sigma 1R and sigma 2R 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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页数：27
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