sphingomyelin synthase 2 | Sphingomyelin synthase | IUPHAR/BPS Guide to PHARMACOLOGY

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sphingomyelin synthase 2

target has curated data in GtoImmuPdb

Target id: 2521

Nomenclature: sphingomyelin synthase 2

Family: Sphingomyelin synthase

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 365 4q25 SGMS2 sphingomyelin synthase 2
Mouse - 365 3 G3 Sgms2 sphingomyelin synthase 2
Rat - 365 2q43 Sgms2 sphingomyelin synthase 2
Previous and Unofficial Names
Phosphatidylcholine:ceramide cholinephosphotransferase 2 | SMS2
Database Links
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 2.7.8.27 ceramide + phosphatidylcholine -> sphingomyelin + diacylglycerol

Download all structure-activity data for this target as a CSV file

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 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] 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]

How to cite this page

Sphingomyelin synthase: sphingomyelin synthase 2. Last modified on 21/08/2018. Accessed on 22/07/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2521.