4q1s | pdb_00004q1s

Yeast 20S proteasome in Complex with Kendomycin

spinqualitylabelsall models 4q1s, resolution 2.60Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 4q1s is a 28 chain structure with sequence from Saccharomyces cerevisiae. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Ligands: 2YD Related: 1ryp Activity: Proteasome endopeptidase complex, with EC number 3.4.25.1 Resources: FirstGlance, OCA, RCSB, PDBsum Publication Abstract from PubMed Natural products are a valuable source for novel lead structures in drug discovery, but for the majority of isolated bioactive compounds the cellular targets are unknown. The structurally unique ansa-polyketide kendomycin was reported to exert its potent cytotoxic effects via impairment of the ubiquitin proteasome system, but the exact mode of action remained unclear. Here, we present a systematic biochemical characterization of kendomycin-proteasome interactions in vitro as well as in vivo, including complex structures of wildtype and mutant yeast 20S proteasome with kendomycin. Our results provide evidence for a polypharmacological mode of action for kendomycin's cytotoxic effect on cancer cells. Structural and biochemical characterization of the natural product kendomycin and the 20S proteasome.,Beck P, Heinemeyer W, Spath AL, Elnakady Y, Muller R, Groll M J Mol Biol. 2014 Jul 16. pii: S0022-2836(14)00335-0. doi:, 10.1016/j.jmb.2014.06.019. PMID:25038530 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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