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σ2

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Target id: 2553

Nomenclature: σ2

Family: Sigma receptors

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 4 176 17q11.2 TMEM97 transmembrane protein 97 2
Mouse 4 176 11 46.74 cM Tmem97 transmembrane protein 97
Rat 4 176 10q25 Tmem97 transmembrane protein 97
Previous and Unofficial Names Click here for help
MAC30 | Meningioma-associated protein 30
Database Links Click here for help
Alphafold Q5BJF2 (Hs), Q8VD00 (Mm), Q5U3Y7 (Rn)
ChEMBL Target CHEMBL4105907 (Hs), CHEMBL4802011 (Mm), CHEMBL4105864 (Rn)
Ensembl Gene ENSG00000109084 (Hs), ENSMUSG00000037278 (Mm), ENSRNOG00000008704 (Rn)
Entrez Gene 27346 (Hs), 69071 (Mm), 303330 (Rn)
Human Protein Atlas ENSG00000109084 (Hs)
KEGG Gene hsa:27346 (Hs), mmu:69071 (Mm), rno:303330 (Rn)
OMIM 612912 (Hs)
Pharos Q5BJF2 (Hs)
RefSeq Nucleotide NM_014573 (Hs), NM_133706 (Mm), NM_001008334 (Rn)
RefSeq Protein NP_055388 (Hs), NP_598467 (Mm), NP_001008335 (Rn)
UniProtKB Q5BJF2 (Hs), Q8VD00 (Mm), Q5U3Y7 (Rn)
Wikipedia TMEM97 (Hs)

Download all structure-activity data for this target as a CSV file go icon to follow link

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
PB-28 Small molecule or natural product Hs Agonist 8.3 pKi 3
⤷ pKi 8.3 [3]
1,3-ditolylguanidine Small molecule or natural product Click here for species-specific activity table Cp Full agonist 7.4 pKi 5
⤷ pKi 7.4 (Ki 3.987x10-8 M) [5]
[3H]-di-o-tolylguanidine Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Agonist - -
⤷
View species-specific agonist tables
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
PD-144418 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Mm Antagonist 5.9 pKi 1
⤷ pKi 5.9 (Ki 1.377x10-6 M) [1]
Description: Displacement of [3H]DTG from sigma2 sites on membranes from NG 108-15 neuroblastoma X glioma rat/mouse hybrid cells
SM 21 Small molecule or natural product Hs Antagonist 7.2 pIC50 6
⤷ pIC50 7.2 [6]
View species-specific antagonist tables
Allosteric Modulators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
CT1812 Small molecule or natural product Hs Antagonist 8.1 pKi 7
⤷ pKi 8.1 (Ki 8.5x10-9 M) [7]
Other Binding Ligands
Key to terms and symbols Click column headers to sort
Ligand Sp. Action Value Parameter Reference
vanoxerine Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Binding 7.3 pIC50 4
⤷ pIC50 7.3 (IC50 4.8x10-8 M) [4]
General Comments
The sigma2 receptor has been reported to be TMEM97 [2], a 4TM protein partner of NPC1, the Niemann-Pick C1 protein, a 13TM cholesterol-binding protein.

References

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1. Akunne HC, Whetzel SZ, Wiley JN, Corbin AE, Ninteman FW, Tecle H, Pei Y, Pugsley TA, Heffner TG. (1997) The pharmacology of the novel and selective sigma ligand, PD 144418. Neuropharmacology, 36 (1): 51-62. [PMID:9144641]

2. Alon A, Schmidt HR, Wood MD, Sahn JJ, Martin SF, Kruse AC. (2017) Identification of the gene that codes for the σ2 receptor. Proc Natl Acad Sci USA, 114 (27): 7160-7165. [PMID:28559337]

3. Berardi F, Colabufo NA, Giudice G, Perrone R, Tortorella V, Govoni S, Lucchi L. (1996) New sigma and 5-HT1A receptor ligands: omega-(tetralin-1-yl)-n-alkylamine derivatives. J Med Chem, 39 (1): 176-82. [PMID:8568804]

4. Contreras PC, Bremer ME, Rao TS. (1990) GBR-12909 and fluspirilene potently inhibited binding of [3H] (+)3-PPP to sigma receptors in rat brain. Life Sci, 47 (22): PL133-7. [PMID:1980329]

5. Lever JR, Gustafson JL, Xu R, Allmon RL, Lever SZ. (2006) Sigma1 and sigma2 receptor binding affinity and selectivity of SA4503 and fluoroethyl SA4503. Synapse, 59 (6): 350-8. [PMID:16463398]

6. Mach RH, Wu L, West T, Whirrett BR, Childers SR. (1999) The analgesic tropane analogue (+/-)-SM 21 has a high affinity for sigma2 receptors. Life Sci, 64 (10): PL131-7. [PMID:10096443]

7. Rishton GM, Look GC, Ni ZJ, Zhang J, Wang Y, Huang Y, Wu X, Izzo NJ, LaBarbera KM, Limegrover CS et al.. (2021) Discovery of Investigational Drug CT1812, an Antagonist of the Sigma-2 Receptor Complex for Alzheimer's Disease. ACS Med Chem Lett, 12 (9): 1389-1395. [PMID:34531947]

How to cite this page

Sigma receptors: σ2. Last modified on 22/04/2024. Accessed on 11/10/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2553.