4lwu

The 1.14A Crystal Structure of Humanized Xenopus MDM2 with RO5499252

spinqualitylabelsall models 4lwu, resolution 1.14Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 4lwu is a 1 chain structure. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Ligands: 20U, SO4 Related: 4lwt, 4lwv Resources: FirstGlance, OCA, RCSB, PDBsum Function [MDM2_XENLA] E3 ubiquitin-protein ligase that mediates ubiquitination of p53/TP53, leading to its degration by the proteasome (By similarity). Publication Abstract from PubMed The field of small-molecule inhibitors of protein-protein interactions is rapidly advancing and the specific area of inhibitors of the p53/MDM2 interaction is a prime example. Several groups have published on this topic and multiple compounds are in various stages of clinical development. Building on the strength of the discovery of RG7112, a Nutlin imidazoline-based compound, and RG7388, a pyrrolidine-based compound, we have developed additional scaffolds that provide opportunities for future development. Here, we report the discovery and optimization of a highly potent and selective series of spiroindolinone small-molecule MDM2 inhibitors, culminating in RO8994. Discovery of potent and selective spiroindolinone MDM2 inhibitor, RO8994, for cancer therapy.,Zhang Z, Ding Q, Liu JJ, Zhang J, Jiang N, Chu XJ, Bartkovitz D, Luk KC, Janson C, Tovar C, Filipovic ZM, Higgins B, Glenn K, Packman K, Vassilev LT, Graves B Bioorg Med Chem. 2014 Jun 11. pii: S0968-0896(14)00431-3. doi:, 10.1016/j.bmc.2014.05.072. PMID:24997575 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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