O-GlcNAcase
From Proteopedia
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== Structural highlights == | == Structural highlights == | ||
| - | The 3D structure of the complex between human OGA and a transition state analog Thiamet-G shows the active site pocket at the base of a V-shaped cleft between the 2 OGA monomers. There are <scene name='86/863205/Cv/8'>numerous H-bonds</scene> formed between OGA and Thiamet-G as well as some <scene name='86/863205/Cv/9'>hydrophobic interactions</scene>. <scene name='86/863205/Cv/ | + | The 3D structure of the complex between human OGA and a transition state analog Thiamet-G shows the active site pocket at the base of a V-shaped cleft between the 2 OGA monomers. There are <scene name='86/863205/Cv/8'>numerous H-bonds</scene> formed between OGA and Thiamet-G as well as some <scene name='86/863205/Cv/9'>hydrophobic interactions</scene>. <scene name='86/863205/Cv/11'>Two Asp residues</scene> are defined as catalytic residues<ref>PMID:28346405</ref>. |
</StructureSection> | </StructureSection> | ||
Revision as of 14:07, 11 October 2020
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3D structures of O-GlcNAcase
Updated on 11-October-2020
References
- ↑ Shen DL, Gloster TM, Yuzwa SA, Vocadlo DJ. Insights into O-linked N-acetylglucosamine ([0-9]O-GlcNAc) processing and dynamics through kinetic analysis of O-GlcNAc transferase and O-GlcNAcase activity on protein substrates. J Biol Chem. 2012 May 4;287(19):15395-408. doi: 10.1074/jbc.M111.310664. Epub, 2012 Feb 6. PMID:22311971 doi:http://dx.doi.org/10.1074/jbc.M111.310664
- ↑ Selnick HG, Hess JF, Tang C, Liu K, Schachter JB, Ballard JE, Marcus J, Klein DJ, Wang X, Pearson M, Savage MJ, Kaul R, Li TS, Vocadlo DJ, Zhou Y, Zhu Y, Mu C, Wang Y, Wei Z, Bai C, Duffy JL, McEachern EJ. Discovery of MK-8719, a Potent O-GlcNAcase Inhibitor as a Potential Treatment for Tauopathies. J Med Chem. 2019 Nov 27;62(22):10062-10097. doi: 10.1021/acs.jmedchem.9b01090., Epub 2019 Sep 29. PMID:31487175 doi:http://dx.doi.org/10.1021/acs.jmedchem.9b01090
- ↑ Yuzwa SA, Shan X, Macauley MS, Clark T, Skorobogatko Y, Vosseller K, Vocadlo DJ. Increasing O-GlcNAc slows neurodegeneration and stabilizes tau against aggregation. Nat Chem Biol. 2012 Feb 26;8(4):393-9. doi: 10.1038/nchembio.797. PMID:22366723 doi:http://dx.doi.org/10.1038/nchembio.797
- ↑ Roth C, Chan S, Offen WA, Hemsworth GR, Willems LI, King DT, Varghese V, Britton R, Vocadlo DJ, Davies GJ. Structural and functional insight into human O-GlcNAcase. Nat Chem Biol. 2017 Mar 27. doi: 10.1038/nchembio.2358. PMID:28346405 doi:http://dx.doi.org/10.1038/nchembio.2358
