Department of Drug and Health Sciences, University of Catania, viale A. Doria 6, 95125, Catania, Italy.
Department of Drug and Health Sciences, University of Catania, viale A. Doria 6, 95125, Catania, Italy; Department of Molecular Medicine, College of Medicine and Medical Sciences, Princess Al Jawhara Centre for Molecular Medicine, Arabian Gulf University, Manama 329, Bahrain.
Bioorg Med Chem. 2022 Nov 1;73:117032. doi: 10.1016/j.bmc.2022.117032. Epub 2022 Sep 26.
The overexpression of σ receptors (σRs) in various types of tumors has prompted a deep investigation of their role in cancer pathophysiology. Consequently, σR ligands have been widely studied in vitro and in vivo for their antiproliferative effects as a novel potential class of chemotherapeutic agents, both alone and in combination with other anticancer drugs. A growing body of evidence highlights that σR ligands can inhibit cancer cells' survival, migration, and proliferation, thanks to the modulation of a wide panel of tumorigenic pathways. In addition to their antitumor activity, σR ligands are gaining momentum as radiotracers for PET and SPECT imaging applications. The purpose of this review is to report on recent advances in the development of σR ligands. In particular, herein, we describe the structure-activity relationships of structurally diverse mixed σR/σR ligands that showed promising antitumor profiles towards a variety of cancer cell lines.
σ 受体（σRs）在各种类型肿瘤中的过表达促使人们深入研究其在癌症病理生理学中的作用。因此，σR 配体已在体外和体内广泛研究，以评估其作为新型潜在化疗药物的抗增殖作用，单独使用和与其他抗癌药物联合使用。越来越多的证据表明，σR 配体可以通过调节广泛的致癌途径来抑制癌细胞的存活、迁移和增殖。除了具有抗肿瘤活性外，σR 配体还作为正电子发射断层扫描（PET）和单光子发射计算机断层扫描（SPECT）成像应用的示踪剂备受关注。本综述的目的是报告 σR 配体研究的最新进展。特别是，本文描述了结构多样的混合 σR/σR 配体的构效关系，这些配体对多种癌细胞系表现出有前景的抗肿瘤特性。
