Health & Environmental Research Online (HERO)


Print Feedback Export to File
7423241 
Journal Article 
Sigma1 Pharmacology in the Context of Cancer 
Kim, FJ; Maher, CM; , 
2017 
0 
Handbook of Experimental Pharmacology
ISSN: 0171-2004 
SPRINGER-VERLAG BERLIN 
BERLIN 
SIGMA PROTEINS: EVOLUTION OF THE CONCEPT OF SIGMA RECEPTORS 
237-308 
English 
28744586 
WOS:000456455900012 
Sigma1 (also known as sigma-1 receptor, Sig1R, σ1 receptor) is a unique pharmacologically regulated integral membrane chaperone or scaffolding protein. The majority of publications on the subject have focused on the neuropharmacology of Sigma1. However, a number of publications have also suggested a role for Sigma1 in cancer. Although there is currently no clinically used anti-cancer drug that targets Sigma1, a growing body of evidence supports the potential of Sigma1 ligands as therapeutic agents to treat cancer. In preclinical models, compounds with affinity for Sigma1 have been reported to inhibit cancer cell proliferation and survival, cell adhesion and migration, tumor growth, to alleviate cancer-associated pain, and to have immunomodulatory properties. This review will highlight that although the literature supports a role for Sigma1 in cancer, several fundamental questions regarding drug mechanism of action and the physiological relevance of aberrant SIGMAR1 transcript and Sigma1 protein expression in certain cancers remain unanswered or only partially answered. However, emerging lines of evidence suggest that Sigma1 is a component of the cancer cell support machinery, that it facilitates protein interaction networks, that it allosterically modulates the activity of its associated proteins, and that Sigma1 is a selectively multifunctional drug target. 
Kim, FJ; Pasternak, GW; 
978-3-319-65851-3