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TitleSynthesis and evaluation of novel orally active p53-MDM2 interaction inhibitors
Journal, issue, pagesBioorg. Med. Chem., Vol. 21, Page 4319-4331, Year 2013
Publish dateFeb 12, 2013 (structure data deposition date)
AuthorsMiyazaki, M. / Naito, H. / Sugimoto, Y. / Yoshida, K. / Kawato, H. / Okayama, T. / Shimizu, H. / Kitagawa, M. / Seki, T. / Fukutake, S. ...Miyazaki, M. / Naito, H. / Sugimoto, Y. / Yoshida, K. / Kawato, H. / Okayama, T. / Shimizu, H. / Kitagawa, M. / Seki, T. / Fukutake, S. / Shiose, Y. / Aonuma, M. / Soga, T.
External linksBioorg. Med. Chem. / PubMed:23685175
MethodsX-ray diffraction
Resolution1.9 Å
Structure data

PDB-3w69:
Crystal structure of human mdm2 with a dihydroimidazothiazole inhibitor
Method: X-RAY DIFFRACTION / Resolution: 1.9 Å

Chemicals

ChemComp-LTZ:
(5R,6S)-2-[((2S,5R)-2-{[(3R)-4-acetyl-3-methylpiperazin-1-yl]carbonyl}-5-ethylpyrrolidin-1-yl)carbonyl]-5,6-bis(4-chlorophenyl)-3-isopropyl-6-methyl-5,6-dihydroimidazo[2,1-b][1,3]thiazole

ChemComp-SO4:
SULFATE ION

ChemComp-HOH:
WATER

Source
  • homo sapiens (human)
KeywordsLIGASE/LIGASE INHIBITOR / Ubiquitin-protein ligase E3 Mdm2 / p53 / LIGASE-LIGASE INHIBITOR complex

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