9BA8
O-GlcNAcase (OGA) inhibitor complex for the Treatment of Alzheimer's Disease
This is a non-PDB format compatible entry.
Summary for 9BA8
| Entry DOI | 10.2210/pdb9ba8/pdb |
| Related | 9BA9 |
| Descriptor | Protein O-GlcNAcase, N-[4-fluoro-5-({(2S,4S)-2-methyl-4-[(5-methyl-1,2,4-oxadiazol-3-yl)methoxy]piperidin-1-yl}methyl)-1,3-thiazol-2-yl]acetamide (3 entities in total) |
| Functional Keywords | inhibitor, complex, o-glcnacase, hydrolase |
| Biological source | Homo sapiens (human) |
| Total number of polymer chains | 2 |
| Total formula weight | 115527.54 |
| Authors | |
| Primary citation | Kielbasa, W.,Goldsmith, P.,Donnelly, K.B.,Nuthall, H.N.,Shcherbinin, S.,Fleisher, A.S.,Hendle, J.,DuBois, S.L.,Lowe, S.L.,Zhang, F.F.,Woerly, E.M.,Dreyfus, N.J.,Evans, D.,Gilmore, J.,Mancini, M.,Constantinescu, C.C.,Gunn, R.N.,Russell, D.S.,Collins, E.C.,Brys, M.,Hutton, M.L.,Mergott, D.J. Discovery and clinical translation of ceperognastat, an O-GlcNAcase (OGA) inhibitor, for the treatment of Alzheimer's disease. Alzheimers Dement (N Y), 10:e70020-e70020, 2024 Cited by PubMed Abstract: The aggregation and spread of hyperphosphorylated, pathological tau in the human brain is hypothesized to play a key role in Alzheimer's disease (AD) as well as other neurogenerative tauopathies. O-GlcNAcylation, an important post-translational modification of tau and many other proteins, is significantly decreased in brain tissue of AD patients relative to healthy controls. Increased tau O-GlcNAcylation has been shown to reduce tau pathology in mouse in vivo tauopathy models. O-GlcNAcase (OGA) catalyzes the removal of O-GlcNAc from tau thereby driving interest in OGA inhibition as a potential therapeutic approach to reduce tau pathology and slow the progression of AD. PubMed: 39748851DOI: 10.1002/trc2.70020 PDB entries with the same primary citation |
| Experimental method | X-RAY DIFFRACTION (2.54 Å) |
Structure validation
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