8skn | pdb_00008skn

Crystal structure of compound 3-bound human Dynamin-1-like protein GTPase-BSE fusion

spinqualitylabelsall models 8skn, resolution 2.41Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 8skn is a 2 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Method: X-ray diffraction, Resolution 2.41Å Ligands: 6I9, EDO Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT Function D3DUW7_HUMAN Publication Abstract from PubMed Mitochondrial dysfunction has been attributed to many disease indications, including metabolic, cardiovascular, neoplastic, and neurodegenerative diseases. Dynamin related protein 1 (DRP1) is crucial in regulating mitochondrial fission and maintaining mitochondrial homeostasis. MiD49 is a dynamic peripheral protein receptor on the surface of the mitochondrial membrane that recruits DRP1 protein to induce mitochondrial binary fission. By targeting the protein-protein interaction of DRP1/MiD49, we have discovered a novel and potent allosteric DRP1 inhibitor that inhibits mitochondria fragmentation in vitro. X-ray cocrystal structure revealed that it locked the closed DRP1 conformation by induced dimerization. Discovery of Potent Allosteric DRP1 Inhibitors by Disrupting Protein-Protein Interaction with MiD49.,Furuya T, Lin J, Afanaseva A, Molz L, Lagu B, Ma B ACS Med Chem Lett. 2023 Jul 24;14(8):1095-1099. doi: , 10.1021/acsmedchemlett.3c00223. eCollection 2023 Aug 10. PMID:37583827 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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