Sigma-1 receptor

Sigma-1 receptor 1
Identifikatori
Simboli	SIGMAR1; SRBP; OPRS1; FLJ25585; MGC3851
Vanjski ID	OMIM: 601978 MGI: 1195268 HomoloGene: 39965 GeneCards: SIGMAR1 Gene
Ontologija gena
Molekularna funkcija	• vezivanje leka; • receptorska aktivnost; • aktivnost C-8 sterol izomeraze;
Celularna komponenta	• ćelijska zaštita; • nukleus; • endoplazmatični retikulum; • integralno sa ćelijskom membranom; • nukleusna unutrašnja membrana; • membrana endoplazmatičnog retikuluma; • nukleusna spoljašnja membrana; • ćelijska membrana;
Biološki proces	• lipidni transport; • proces ergosterolne biosinteze;
Ortolozi

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Sigma-1 receptor (σ₁R) je šaperonski protein na endoplazmatičnom retikulumu (ER) koji moduliše kalcijumsku signalizaciju putem IP3 receptora.^[1] Sigma-1 receptor je kod čoveka kodiran SIGMAR1 genom.^[2]^[3]

Sigma-1 receptor je transmembranski protein koji je izražen u mnogim tipovima tkiva. On je posebno koncentrovan u pojedinim regionima centralnog nervnog sistema.^[4] Za njega se smatra da učestvuje u velikom broju sistema, što obuhvata kardiovaskularne funkcije, šizofreniju, kliničku depresiju, efekte zloupotrebe kokaina, i rak.^[5]^[6] Dostupne se detaljne informacije o afinitetu vezivanja stotina sintetičkih jedinjenja za sigma-1 receptor.

Endogeni ligand sigma-1 receptora još uvek nije poznat. Trag amini i halucinogen dimetiltriptamin (DMT), kao i neuroaktivni steroidi poput dehidroepiandrosterona (DHEA) i pregnenolona, mogu da aktiviraju ovaj receptor.^[7]

↑ Hayashi T, Su TP (2007). „Sigma-1 receptor chaperones at the ER-mitochondrion interface regulate Ca²⁺ signaling and cell survival.”. Cell 131 (3): 596–610. DOI:10.1016/j.cell.2007.08.036. PMID 17981125.
↑ Kekuda R, Prasad PD, Fei YJ, Leibach FH, Ganapathy V (December 1996). „Cloning and functional expression of the human type 1 sigma receptor (hSigmaR1)”. Biochem. Biophys. Res. Commun. 229 (2): 553–8. DOI:10.1006/bbrc.1996.1842. PMID 8954936.
↑ Prasad PD, Li HW, Fei YJ, Ganapathy ME, Fujita T, Plumley LH, Yang-Feng TL, Leibach FH, Ganapathy V (February 1998). „Exon-intron structure, analysis of promoter region, and chromosomal localization of the human type 1 sigma receptor gene”. J. Neurochem. 70 (2): 443–51. DOI:10.1046/j.1471-4159.1998.70020443.x. PMID 9453537.
↑ Weissman AD, Su TP, Hedreen JC, London ED (1988). „Sigma receptors in post-mortem human brains”. J. Pharmacol. Exp. Ther. 247 (1): 29–33. PMID 2845055.
↑ Guitart X, Codony X, Monroy X (2004). „Sigma receptors: biology and therapeutic potential”. Psychopharmacology (Berl.) 174 (3): 301–19. DOI:10.1007/s00213-004-1920-9. PMID 15197533.
↑ Zhang H, Cuevas J (2005). „sigma Receptor activation blocks potassium channels and depresses neuroexcitability in rat intracardiac neurons”. J. Pharmacol. Exp. Ther. 313 (3): 1387–96. DOI:10.1124/jpet.105.084152. PMID 15764734.
↑ Fontanilla et al.; Jessett, DM; Brown, CG; Radley, DE; Jackson, M. B.; Ruoho, A. E. (2009). „The Hallucinogen N,N-Dimethyltryptamine (DMT) Is an Endogenous Sigma-1 Receptor Regulator”. Science 323 (5916): 934–937. DOI:10.1126/science.1166127. PMC 2947205. PMID 19213917.

[Hayashi-1] Hayashi T, Su TP (2007). „Sigma-1 receptor chaperones at the ER-mitochondrion interface regulate Ca²⁺ signaling and cell survival.”. Cell 131 (3): 596–610. DOI:10.1016/j.cell.2007.08.036. PMID 17981125.

[pmid8954936-2] Kekuda R, Prasad PD, Fei YJ, Leibach FH, Ganapathy V (December 1996). „Cloning and functional expression of the human type 1 sigma receptor (hSigmaR1)”. Biochem. Biophys. Res. Commun. 229 (2): 553–8. DOI:10.1006/bbrc.1996.1842. PMID 8954936.

[pmid9453537-3] Prasad PD, Li HW, Fei YJ, Ganapathy ME, Fujita T, Plumley LH, Yang-Feng TL, Leibach FH, Ganapathy V (February 1998). „Exon-intron structure, analysis of promoter region, and chromosomal localization of the human type 1 sigma receptor gene”. J. Neurochem. 70 (2): 443–51. DOI:10.1046/j.1471-4159.1998.70020443.x. PMID 9453537.

[pmid2845055-4] Weissman AD, Su TP, Hedreen JC, London ED (1988). „Sigma receptors in post-mortem human brains”. J. Pharmacol. Exp. Ther. 247 (1): 29–33. PMID 2845055.

[pmid15197533-5] Guitart X, Codony X, Monroy X (2004). „Sigma receptors: biology and therapeutic potential”. Psychopharmacology (Berl.) 174 (3): 301–19. DOI:10.1007/s00213-004-1920-9. PMID 15197533.

[pmid15764734-6] Zhang H, Cuevas J (2005). „sigma Receptor activation blocks potassium channels and depresses neuroexcitability in rat intracardiac neurons”. J. Pharmacol. Exp. Ther. 313 (3): 1387–96. DOI:10.1124/jpet.105.084152. PMID 15764734.

[Fontanilla-7] Fontanilla et al.; Jessett, DM; Brown, CG; Radley, DE; Jackson, M. B.; Ruoho, A. E. (2009). „The Hallucinogen N,N-Dimethyltryptamine (DMT) Is an Endogenous Sigma-1 Receptor Regulator”. Science 323 (5916): 934–937. DOI:10.1126/science.1166127. PMC 2947205. PMID 19213917.

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