Crystal structures of salinosporamide A (NPI-0052) and B (NPI-0047) in complex with the 20S proteasome reveal important consequences of β-lactone ring opening and a mechanism for irreversible binding

Journal of the American Chemical Society

Volumn 128, Issue 15, 2006, Pages 5136-5141

  Groll, Michael ^a   Huber, Robert ^b   Potts, Barbara C M ^c  

^a UNIVERSITY OF MUNICH   (Germany)

^b MAX PLANCK INSTITUTE OF BIOCHEMISTRY   (Germany)

^c Nereus Pharmaceuticals Inc   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

BINDING ENERGY; CRYSTAL STRUCTURE; ESTERS; NUCLEIC ACIDS; PROTEINS;

ESTER LINKAGE; IRREVERSIBLE BINDING; NUCLEOPHILIC ADDITION; YEAST 20S PROTEASOME CORE PARTICLE (CP);

ORGANIC COMPOUNDS;

20S PROTEASOME; ALKYL GROUP; BETA LACTONE; CARBONYL DERIVATIVE; CHLORINE; CHLOROETHYL GROUP; ETHANE; ETHER DERIVATIVE; LACTACYSTIN BETA LACTONE; LACTONE; PROTEASOME; PROTEASOME INHIBITOR; SALINOSPORAMIDE A; SALINOSPORAMIDE B; THREONINE; UNCLASSIFIED DRUG; WATER;

ADDITION REACTION; AMINO TERMINAL SEQUENCE; ARTICLE; BINDING KINETICS; COVALENT BOND; CRYSTAL STRUCTURE; DEACYLATION; ENZYME INHIBITOR COMPLEX; INHIBITION KINETICS; IRREVERSIBLE BINDING; LIGAND BINDING; NUCLEOPHILIC ADDITION; PROTON TRANSPORT; RING OPENING; STEREOSPECIFICITY;

EID: 33646137808     PISSN: 00027863     EISSN: None     Source Type: Journal    
DOI: 10.1021/ja058320b     Document Type: Article

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