Structure-activity relationships of mixed?1R/?2R ligands with antiproliferative and anticancer effects

被引：4
作者：
Fallica, Antonino N. [1 ]
Ciaffaglione, Valeria [1 ]
Modica, Maria N. [1 ]
Pittala, Valeria [1 ,2 ]
Salerno, Loredana [1 ]
Amata, Emanuele [1 ]
Marrazzo, Agostino [1 ]
Romeo, Giuseppe [1 ]
Intagliata, Sebastiano [1 ]
机构：
[1] Univ Catania, Dept Drug & Hlth Sci, Viale A Doria 6, I-95125 Catania, Italy
[2] Arabian Gulf Univ, Coll Med & Med Sci, Princess Al Jawhara Ctr Mol Med, Dept Mol Med, Manama 329, Bahrain
来源：
BIOORGANIC & MEDICINAL CHEMISTRY | 2022年 / 73卷
关键词：
Receptors; 1 Receptor; 2 Receptor; Receptor ligands; Cancer; Antiproliferative activity; SIGMA(2) RECEPTOR LIGANDS; EMOPAMIL BINDING-PROTEIN; MEMBRANE COMPONENT 1; TUMOR-CELL DEATH; HIGH-AFFINITY; BIOLOGICAL EVALUATION; IN-VITRO; MEDICINAL CHEMISTRY; OPIOID ANALGESIA; BREAST-CANCER;
D O I：
10.1016/j.bmc.2022.117032
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
The overexpression of sigma receptors (sigma Rs) in various types of tumors has prompted a deep investigation of their role in cancer pathophysiology. Consequently, sigma R 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 sigma R 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, sigma R 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 sigma R ligands. In particular, herein, we describe the structure-activity relationships of structurally diverse mixed sigma 1R/sigma 2R ligands that showed promising antitumor profiles towards a variety of cancer cell lines.
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页数：20
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