2xj7

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BtGH84 in complex with 6-acetamido-6-deoxy-castanospermine

Structural highlights

2xj7 is a 2 chain structure with sequence from Bacteroides thetaiotaomicron VPI-5482. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Method:X-ray diffraction, Resolution 2Å
Ligands:CA, GC2
Resources:FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

OGA_BACTN Biological function unknown. Capable of hydrolyzing the glycosidic link of O-GlcNAcylated proteins.

Evolutionary Conservation

Check, as determined by ConSurfDB. You may read the explanation of the method and the full data available from ConSurf.

Publication Abstract from PubMed

To probe increased O-GlcNAc levels as an independent mechanism governing insulin resistance in 3T3-L1 adipocytes, a new class of O-GlcNAcase (OGA) inhibitor was studied. 6-Acetamido-6-deoxy-castanospermine (6-Ac-Cas) is a potent inhibitor of OGA. The structure of 6-Ac-Cas bound in the active site of an OGA homolog reveals structural features contributing to its potency. Treatment of 3T3-L1 adipocytes with 6-Ac-Cas increases O-GlcNAc levels in a dose-dependent manner. These increases in O-GlcNAc levels do not induce insulin resistance functionally, measured using a 2-deoxyglucose (2-DOG) uptake assay, or at the molecular level, determined by evaluating levels of phosphorylated IRS-1 and Akt. These results, and others described, provide a structural blueprint for improved inhibitors and collectively suggest that increased O-GlcNAc levels, brought about by inhibition of OGA, does not by itself cause insulin resistance in 3T3-L1 adipocytes.

Inhibition of O-GlcNAcase using a potent and cell-permeable inhibitor does not induce insulin resistance in 3T3-L1 adipocytes.,Macauley MS, He Y, Gloster TM, Stubbs KA, Davies GJ, Vocadlo DJ Chem Biol. 2010 Sep 24;17(9):937-48. PMID:20851343[1]

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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Citations
16 reviews cite this structure
Protein O-GlcNAcylation: emerging mechanisms and functions.
Yang et al. (2017)
15 more
25 other articles
No citations found

See Also

References

  1. ↑ Macauley MS, He Y, Gloster TM, Stubbs KA, Davies GJ, Vocadlo DJ. Inhibition of O-GlcNAcase using a potent and cell-permeable inhibitor does not induce insulin resistance in 3T3-L1 adipocytes. Chem Biol. 2010 Sep 24;17(9):937-48. PMID:20851343 doi:10.1016/j.chembiol.2010.07.006

Contents


PDB ID 2xj7

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