8ahm | pdb_00008ahm

Crystal structure of tubulin in complex with C(13)/C(13')-Bis-Desmethyl-Disorazole Z

spinqualitylabelsall models 8ahm, resolution 2.42Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 8ahm is a 6 chain structure with sequence from Bos taurus, Gallus gallus and Rattus norvegicus. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Ligands: ACP, CA, DMS, GDP, GOL, GTP, M5U, MES, MG Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT Function E1BQ43_CHICK Publication Abstract from PubMed We describe the total synthesis of the macrodiolide C(13)/C(13')-bis(desmethyl)disorazole Z via double inter-/intramolecular Stille cross-coupling of a monomeric vinyl stannane/vinyl iodide precursor to achieve macrocycle formation. The key step in the synthesis of this precursor was a stereoselective aldol reaction of a formal Evans acetate aldol product with crotonaldehyde. As demonstrated by X-ray crystallography, the binding mode of C(13)/C(13')-bis(desmethyl)disorazole Z to tubulin is virtually identical with that of the natural product disorazole Z. Likewise, C(13)/C(13')-bis(desmethyl)disorazole Z inhibits tubulin assembly with at least the same potency as disorazole Z and it appears to be a more potent cell growth inhibitor. Synthesis and Biological Evaluation of C(13)/C(13')-Bis(desmethyl)disorazole Z.,Bold CP, Lucena-Agell D, Oliva MA, Diaz JF, Altmann KH Angew Chem Int Ed Engl. 2022 Oct 25. doi: 10.1002/anie.202212190. PMID:36281761 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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