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sphingomyelin synthase 2

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Immunopharmacology Ligand target has curated data in GtoImmuPdb

Target id: 2521

Nomenclature: sphingomyelin synthase 2

Family: Sphingomyelin synthase

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 6 365 4q25 SGMS2 sphingomyelin synthase 2
Mouse 6 365 3 G3 Sgms2 sphingomyelin synthase 2
Rat 6 365 2q43 Sgms2 sphingomyelin synthase 2
Previous and Unofficial Names Click here for help
Phosphatidylcholine:ceramide cholinephosphotransferase 2 | SMS2
Database Links Click here for help
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ChEMBL Target
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Enzyme Reaction Click here for help
EC Number: 2.7.8.27 ceramide + phosphatidylcholine -> sphingomyelin + diacylglycerol

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Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
sphingomyelin synthase 2 inhibitor 15w Small molecule or natural product Primary target of this compound Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 7.0 pIC50 3
pIC50 7.0 (IC50 1x10-7 M) [3]
Description: Inhibition of purified human SMS2 in vitro.
compound D24 [PMID: 24374347] Small molecule or natural product Hs Inhibition 4.9 pIC50 2
pIC50 4.9 (IC50 1.24x10-5 M) [2]
Immunopharmacology Comments
Sphingomyelin synthase 2 (SMS2) is a promising therapeutic target for chronic inflammation-associated diseases, such as atherosclerosis, fatty liver and insulin resistance. Since downregulation of SMS2 activity results in protective effects against obesity, atherosclerosis and diabetes, selective SMS2 inhibitors are being explored as novel alternatives for the treatment of such metabolic diseases [1].

References

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1. Chen Y, Cao Y. (2017) The sphingomyelin synthase family: proteins, diseases, and inhibitors. Biol Chem, 398 (12): 1319-1325. [PMID:28742512]

2. Deng X, Lin F, Zhang Y, Li Y, Zhou L, Lou B, Li Y, Dong J, Ding T, Jiang X et al.. (2014) Identification of small molecule sphingomyelin synthase inhibitors. Eur J Med Chem, 73: 1-7. [PMID:24374347]

3. Mo M, Yang J, Jiang XC, Cao Y, Fei J, Chen Y, Qi X, Chu Y, Zhou L, Ye D. (2018) Discovery of 4-Benzyloxybenzo[ d]isoxazole-3-amine Derivatives as Highly Selective and Orally Efficacious Human Sphingomyelin Synthase 2 Inhibitors that Reduce Chronic Inflammation in db/ db Mice. J Med Chem, 61 (18): 8241-8254. [PMID:30074791]

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