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ERG2/Sigma-1 receptor
Identifiers
Symbol
ERG2_Sigma1R
Pfam
PF04622
InterPro
IPR006716
TCDB
8.A.63
OPM superfamily
446
OPM protein
5hk1
Membranome
1025
Available protein structures:
Pfam
structures / ECOD
PDB
RCSB PDB; PDBe; PDBj
PDBsum
structure summary
Sigma intracellular receptor 2
Identifiers
Symbol
Sigma2
InterPro
IPR016964
Sigma receptors (σ-receptors) are protein cell surface 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 receptors (σ1) and sigma-2 receptors (σ2), 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]
^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.
^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.
^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.
^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.
^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.
Sigmareceptors (σ-receptors) are protein cell surface receptors that bind ligands such as 4-PPBP (4-phenyl-1-(4-phenylbutyl) piperidine), SA 4503 (cutamesine)...
as the absolute mean value. In biology, the sigmareceptor (σ–receptors) is a type of cell surface receptor. In biochemistry, the σ factor (or specificity...
hormone receptors are found in the nucleus, cytosol, and also on the plasma membrane of target cells. They are generally intracellular receptors (typically...
is a selective sigmareceptor antagonist, with a reported binding affinity of Ki = 9 ± 1 nM for the sigma-1 receptor and more than 49 times selectivity...
and cold medicines. It affects serotonin, norepinephrine, NMDA, and sigma-1 receptors in the brain, all of which have been implicated in the pathophysiology...
ligands of the sigmareceptors. Fluvoxamine is an agonist of the σ1 receptor, while sertraline is an antagonist of the σ1 receptor, and paroxetine does...
activity, the drug is a sigmareceptor agonist, and has been used widely in scientific research in studies of this receptor. Alazocine is described as...
Methamphetamine binds to and activates both sigmareceptor subtypes, σ1 and σ2, with micromolar affinity. Sigmareceptor activation may promote methamphetamine-induced...
other than the three classic opioid receptors, including the nociceptin receptor, sigmareceptor and Toll-like receptor 4, and can be counteracted in animal...
selective sigmareceptor antagonist, with a reported binding affinity of Ki = 2 ± 1 nM for the sigma-1 receptor and 4 times selectivity over the sigma-2 receptor...
hours. It is a first-generation antihistamine and works by blocking the H1 receptor. Common side effects include sleepiness, restlessness, and weakness. Other...
channel-blocking antiepileptic drugs are not, possibly on account of its sigmareceptor activity. In addition, lamotrigine shares few side effects with other...
and 5-HT2C), 5-HT6, 5-HT7, α1-adrenergic, and NMDA receptors, and as agonists at the sigmareceptors (σ1 and σ2), some of which may contribute to their...
Cutamesine (SA 4503) is a synthetic sigmareceptor agonist which is selective for the σ1 receptor, a chaperone protein mainly found in the endoplasmic...
primarily as a strong antagonist of the H1 receptor (antihistamine, Ki = 1.4 nM) and a moderate mACh receptor antagonist (anticholinergic), and also has...
9 March 2007. Retrieved 17 July 2009. "B3251 Berberine chloride form". Sigma-Aldrich. 2013. Archived from the original on 7 September 2012. Retrieved...
Ditolylguanidine is a sigmareceptor agonist. It is somewhat selective for sigmareceptors, but non-selective between the two sigmareceptor subtypes, binding...
Hashimoto K (2017). "Sigma-1 Receptor Agonists and Their Clinical Implications in Neuropsychiatric Disorders". SigmaReceptors: Their Role in Disease...
selective sigmareceptor agonist, with a reported binding affinity of Ki = 2 ± 0.5 nM for the sigma-1 receptor and 30 times selectivity over the sigma-2 receptor...
acetylcholine receptors and virtually no anticholinergic effects. Sigmareceptors are a set of proteins located in the endoplasmic reticulum. σ1 receptors play...
balanced, modest affinity D2 and 5-HT2 receptor antagonist and also possesses high affinity for the sigmareceptor. It was well tolerated and showed efficacy...
known as pyrilamine, is a first generation antihistamine, targeting the H1 receptor as an inverse agonist. Mepyramine rapidly permeates the brain, often causing...
In the field of molecular biology, nuclear receptors are a class of proteins responsible for sensing steroids, thyroid hormones, vitamins, and certain...
A receptor modulator, or receptor ligand, is a general term for a substance, endogenous or exogenous, that binds to and regulates the activity of chemical...
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