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UDP-glucose ceramide glucosyltransferase

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Target not currently curated in GtoImmuPdb

Target id: 2528

Nomenclature: UDP-glucose ceramide glucosyltransferase

Family: Ceramide glucosyltransferase

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 5 394 9q31.3 UGCG UDP-glucose ceramide glucosyltransferase
Mouse 5 394 4 B3 Ugcg UDP-glucose ceramide glucosyltransferase
Rat 5 394 5q24 Ugcg UDP-glucose ceramide glucosyltransferase
Previous and Unofficial Names Click here for help
Epcs21 | GCS | GLCT-1 | Glucosylceramide synthase | Ugcgl
Database Links Click here for help
Alphafold Q16739 (Hs), O88693 (Mm), Q9R0E0 (Rn)
BRENDA 2.4.1.80
CATH/Gene3D 3.90.550.10
ChEMBL Target CHEMBL2063 (Hs), CHEMBL6013 (Mm)
DrugBank Target Q16739 (Hs)
Ensembl Gene ENSG00000148154 (Hs), ENSMUSG00000028381 (Mm), ENSRNOG00000015644 (Rn)
Entrez Gene 7357 (Hs), 22234 (Mm), 83626 (Rn)
Human Protein Atlas ENSG00000148154 (Hs)
KEGG Enzyme 2.4.1.80
KEGG Gene hsa:7357 (Hs), mmu:22234 (Mm), rno:83626 (Rn)
OMIM 602874 (Hs)
Pharos Q16739 (Hs)
RefSeq Nucleotide NM_003358 (Hs), NM_011673 (Mm), NM_031795 (Rn)
RefSeq Protein NP_003349 (Hs), NP_035803 (Mm), NP_113983 (Rn)
UniProtKB Q16739 (Hs), O88693 (Mm), Q9R0E0 (Rn)
Wikipedia UGCG (Hs)
Enzyme Reaction Click here for help
EC Number: 2.4.1.80 UDP-glucose + ceramide = UDP + glucosylceramide

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

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
miglustat Small molecule or natural product Approved drug Primary target of this compound Ligand has a PDB structure Hs Inhibition 5.1 pKi 2
⤷ pKi 5.1 (Ki 7.4x10-6 M) [2]
T-690 Small molecule or natural product Hs Inhibition 7.8 pIC50 3
⤷ pIC50 7.8 (IC50 1.5x10-8 M) [3]
venglustat Small molecule or natural product Ligand has a PDB structure Hs Inhibition >5.3 pIC50 1
⤷ pIC50 >5.3 (IC50 <5x10-6 M) [1]
Description: Inhibition of glucosylceramide synthase activity in microsomes derived from human A375 melanoma cells, using fluorescent ceramide as substrate.
Immuno Process Associations
Immuno Process:  Cytokine production & signalling
General Comments
UDP-glucose ceramide glucosyltransferase (a.k.a. glucosylceramide synthase) is a key enzyme in glycolipid synthesis and it is a therapeutic target for the lysosomal storage disorder Gaucher's disease (GD). Inhibitors of this enzyme are predicted to reduce accumulation of glycosphingolipids (e.g. glucosylsphingosine) that are associated with disease pathologies.

References

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1. Bourque E, Celatka C, Hirth B, Metz M, Zhao Z, Skerlj R, Xiang Y, Jancisics K, Marshall J, Cheng S et al.. (2014) Glucosylceramide synthase inhibitors. Patent number: WO2012129084A2. Assignee: Genzyme Corporation. Priority date: 18/03/2011. Publication date: 24/04/2014.

2. Butters TD, van den Broek LAGM, Fleet GWJ, Krulle TM, Wormald MR, Dwek RA, Platt FM. (2000) Molecular requirements of imino sugars for the selective control of N-linked glycosylation and glycosphingolipid biosynthesis. Tetrahedron: Assymetry, 11 (1): 113-124.

3. Tanaka Y, Seto M, Kakegawa K, Takami K, Kikuchi F, Yamamoto T, Nakamura M, Daini M, Murakami M, Ohashi T et al.. (2022) Discovery of Brain-Penetrant Glucosylceramide Synthase Inhibitors with a Novel Pharmacophore. J Med Chem, 65 (5): 4270-4290. [PMID:35188773]

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