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Structure-activity relationships of mixed σ1R/σ2R ligands with antiproliferative and anticancer effects.
Fallica, Antonino N; Ciaffaglione, Valeria; Modica, Maria N; Pittalà, Valeria; Salerno, Loredana; Amata, Emanuele; Marrazzo, Agostino; Romeo, Giuseppe; Intagliata, Sebastiano.
Afiliación
  • Fallica AN; Department of Drug and Health Sciences, University of Catania, viale A. Doria 6, 95125, Catania, Italy.
  • Ciaffaglione V; Department of Drug and Health Sciences, University of Catania, viale A. Doria 6, 95125, Catania, Italy.
  • Modica MN; Department of Drug and Health Sciences, University of Catania, viale A. Doria 6, 95125, Catania, Italy.
  • Pittalà V; 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.
  • Salerno L; Department of Drug and Health Sciences, University of Catania, viale A. Doria 6, 95125, Catania, Italy.
  • Amata E; Department of Drug and Health Sciences, University of Catania, viale A. Doria 6, 95125, Catania, Italy.
  • Marrazzo A; Department of Drug and Health Sciences, University of Catania, viale A. Doria 6, 95125, Catania, Italy.
  • Romeo G; Department of Drug and Health Sciences, University of Catania, viale A. Doria 6, 95125, Catania, Italy.
  • Intagliata S; Department of Drug and Health Sciences, University of Catania, viale A. Doria 6, 95125, Catania, Italy.
Bioorg Med Chem ; 73: 117032, 2022 11 01.
Article en En | MEDLINE | ID: mdl-36202063
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 σ1R/σ2R ligands that showed promising antitumor profiles towards a variety of cancer cell lines.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Receptores sigma / Neoplasias / Antineoplásicos Límite: Humans Idioma: En Revista: Bioorg Med Chem Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2022 Tipo del documento: Article País de afiliación: Italia Pais de publicación: Reino Unido
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Receptores sigma / Neoplasias / Antineoplásicos Límite: Humans Idioma: En Revista: Bioorg Med Chem Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2022 Tipo del documento: Article País de afiliación: Italia Pais de publicación: Reino Unido