Synthesis and Binding of Stable Bisubstrate Ligands for Phosphoglycerate Kinase
Data(s) |
22/09/1998
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Identificador |
http://www.scopus.com/inward/record.url?scp=0032558478&partnerID=8YFLogxK |
Idioma(s) |
eng |
Direitos |
info:eu-repo/semantics/restrictedAccess |
Fonte |
Williams , D M , Jakeman , D L , Vyle , J , Williamson , M P & Blackburn , G M 1998 , ' Synthesis and Binding of Stable Bisubstrate Ligands for Phosphoglycerate Kinase ' Bioorganic & Medicinal Chemistry , vol 8 , no. 18 , pp. 2603-2608 . |
Palavras-Chave | #/dk/atira/pure/subjectarea/asjc/1300/1303 #Biochemistry #/dk/atira/pure/subjectarea/asjc/1300/1312 #Molecular Biology #/dk/atira/pure/subjectarea/asjc/1600/1605 #Organic Chemistry #/dk/atira/pure/subjectarea/asjc/3000/3002 #Drug Discovery #/dk/atira/pure/subjectarea/asjc/3000/3003 #Pharmaceutical Science |
Tipo |
article |
Resumo |
Stable bisubstrate ligands of phosphoglycerate kinase (PGK) have been synthesised with AMP or ADP conjugated to hydrolytically-stable, symmetrical analogues of 1,3-bisphosphoglycerate and their binding to yeast PGK evaluated. Their Kds decrease with net negative charge, with a penta-anionic analogue 7 showing highest affinity - in accordance with its approximation to the transition state for the reaction catalysed by PGK. |