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TitleCrystal Structures of Salinosporamide A (NPI-0052) and B (NPI-0047) in Complex with the 20S Proteasome Reveal Important Consequences of beta-Lactone Ring Opening and a Mechanism for Irreversible Binding.
Journal, issue, pagesJ. Am. Chem. Soc., Vol. 128, Page 5136-5141, Year 2006
Publish dateDec 7, 2005 (structure data deposition date)
AuthorsGroll, M. / Huber, R. / Potts, B.C.
External linksJ. Am. Chem. Soc. / PubMed:16608349
MethodsX-ray diffraction
Resolution2.8 Å
Structure data

PDB-2fak:
Crystal structure of Salinosporamide A in complex with the yeast 20S proteasome
Method: X-RAY DIFFRACTION / Resolution: 2.8 Å

Chemicals

ChemComp-SA1:
(3AR,6R,6AS)-6-((S)-((S)-CYCLOHEX-2-ENYL)(HYDROXY)METHYL)-6A-METHYL-4-OXO-HEXAHYDRO-2H-FURO[3,2-C]PYRROLE-6-CARBALDEHYDE / anticancer, inhibitor*YM

ChemComp-HOH:
WATER

Source
  • saccharomyces cerevisiae (brewer's yeast)
KeywordsHYDROLASE / proteasome / ubiquitin / drug design / inhibitor / protease

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