7UMO
Structure of Unc119-inhibitor complex.
Summary for 7UMO
| Entry DOI | 10.2210/pdb7umo/pdb |
| Descriptor | Protein unc-119 homolog A, (3s,5s,7s)-N-(4,5-dichloropyridin-2-yl)adamantane-1-carboxamide, GLYCEROL, ... (4 entities in total) |
| Functional Keywords | unc119, inhibitor, transport protein |
| Biological source | Homo sapiens (human) |
| Total number of polymer chains | 6 |
| Total formula weight | 140377.81 |
| Authors | Srivastava, D.,Sebag, J.A.,Artemyev, N.O. (deposition date: 2022-04-07, release date: 2023-07-26, Last modification date: 2023-08-30) |
| Primary citation | Yin, T.C.,Van Vranken, J.G.,Srivastava, D.,Mittal, A.,Buscaglia, P.,Moore, A.E.,Verdinez, J.A.,Graham, A.E.,Walsh, S.A.,Acevedo, M.A.,Kerns, R.J.,Artemyev, N.O.,Gygi, S.P.,Sebag, J.A. Insulin sensitization by small molecules enhancing GLUT4 translocation. Cell Chem Biol, 30:933-942.e6, 2023 Cited by PubMed Abstract: Insulin resistance (IR) is the root cause of type II diabetes, yet no safe treatment is available to address it. Using a high throughput compatible assay that measures real-time translocation of the glucose transporter glucose transporter 4 (GLUT4), we identified small molecules that potentiate insulin action. In vivo, these insulin sensitizers improve insulin-stimulated GLUT4 translocation, glucose tolerance, and glucose uptake in a model of IR. Using proteomic and CRISPR-based approaches, we identified the targets of those compounds as Unc119 proteins and solved the structure of Unc119 bound to the insulin sensitizer. This study identifies compounds that have the potential to be developed into diabetes treatment and establishes Unc119 proteins as targets for improving insulin sensitivity. PubMed: 37453421DOI: 10.1016/j.chembiol.2023.06.012 PDB entries with the same primary citation |
| Experimental method | X-RAY DIFFRACTION (2.3 Å) |
Structure validation
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