Sigma receptor

ERG2/Sigma-1 receptor
Identifiers
SymbolERG2_Sigma1R
PfamPF04622
InterProIPR006716
TCDB8.A.63
OPM superfamily446
OPM protein5hk1
Membranome1025
Available protein structures:
Pfam  structures / ECOD  
PDBRCSB PDB; PDBe; PDBj
PDBsumstructure summary
Sigma intracellular receptor 2
Identifiers
SymbolSigma2
InterProIPR016964

Sigma receptors (σ-receptors) are protein receptors that bind ligands such as 4-PPBP (4-phenyl-1-(4-phenylbutyl) piperidine),[1] SA 4503 (cutamesine), ditolylguanidine, dimethyltryptamine,[2] and siramesine.[3] There are two subtypes, sigma-1 receptors1) and sigma-2 receptors2), which are classified as sigma receptors for their pharmacological similarities, even though they are evolutionarily unrelated.

The fungal protein ERG2, a C-8 sterol isomerase, falls into the same protein family as sigma-1. Both localize to the ER membrane, although sigma-1 is also reported to be a cell surface receptor. Sigma-2 is an EXPREA domain protein[4] with a mostly intracellular (ER membrane) localization.[5]

  1. ^ Yang S, Bhardwaj A, Cheng J, Alkayed NJ, Hurn PD, Kirsch JR (May 2007). "Sigma receptor agonists provide neuroprotection in vitro by preserving bcl-2". Anesthesia and Analgesia. 104 (5): 1179–84, tables of contents. doi:10.1213/01.ane.0000260267.71185.73. PMC 2596726. PMID 17456670.
  2. ^ Fontanilla D, Johannessen M, Hajipour AR, Cozzi NV, Jackson MB, Ruoho AE (February 2009). "The hallucinogen N,N-dimethyltryptamine (DMT) is an endogenous sigma-1 receptor regulator". Science. 323 (5916): 934–7. Bibcode:2009Sci...323..934F. doi:10.1126/science.1166127. PMC 2947205. PMID 19213917.
  3. ^ Skuza G, Rogóz Z (June 2006). "The synergistic effect of selective sigma receptor agonists and uncompetitive NMDA receptor antagonists in the forced swim test in rats". Journal of Physiology and Pharmacology. 57 (2): 217–29. PMID 16845227.
  4. ^ Sanchez-Pulido L, Ponting CP (2014). "TM6SF2 and MAC30, new enzyme homologs in sterol metabolism and common metabolic disease". Frontiers in Genetics. 5: 439. doi:10.3389/fgene.2014.00439. PMC 4263179. PMID 25566323.
  5. ^ Bartz F, Kern L, Erz D, Zhu M, Gilbert D, Meinhof T, Wirkner U, Erfle H, Muckenthaler M, Pepperkok R, Runz H (July 2009). "Identification of Cholesterol-Regulating Genes by Targeted RNAi Screening". Cell Metabolism. 10 (1): 63–75. doi:10.1016/j.cmet.2009.05.009. PMID 19583955.