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

IF 4.9 Q1 CHEMISTRY, MEDICINAL

ACS Pharmacology and Translational Science Pub Date : 2025-03-07 DOI:10.1021/acsptsci.4c0071110.1021/acsptsci.4c00711

Tao Wang*, Na Sun, Yanxi Ma and Song Zhang*,

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Abstract

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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Sigma受体（无线电）配体的研究进展及其在肿瘤中的应用

癌症是全世界人类死亡的三大主要原因之一。病理机制非常复杂，表现出增殖和转移能力，这使治疗干预复杂化。sigma-1受体（σ1R）在肿瘤的存活和迁移中起着至关重要的作用，而sigma-2受体（σ2R）则与肿瘤的增殖密切相关。本文综述了σ1R和σ2R在肿瘤中的研究进展，并对配体和放射性配体的发展及其在肿瘤中的应用，如抗肿瘤细胞增殖和PET/SPECT成像等方面进行了综述。对其化学结构进行了全面的分类讨论，并强调了双/多靶向配体的可能性。最后，我们讨论了配体的手性结构和药理学特性对体内亲和力和药代动力学特征的影响，特别是关于放射性药物。这篇综述是一个有益的资源，促进配体的部署，并刺激创新思想的产生，以开发创新的放射性药物。

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来源期刊

ACS Pharmacology and Translational Science Medicine-Pharmacology (medical)

CiteScore

10.00

自引率

3.30%

发文量

133

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