Synthesis and Binding of Stable Bisubstrate Ligands for Phosphoglycerate Kinase

D.M. Williams, D.L. Jakeman, Joseph Vyle, M.P. Williamson, G.M. Blackburn

Research output: Contribution to journalArticle

10 Citations (Scopus)

Abstract

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.
Original languageEnglish
Pages (from-to)2603-2608
Number of pages6
JournalBioorganic & Medicinal Chemistry
Volume8
Issue number18
Publication statusPublished - 22 Sep 1998

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science

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  • Cite this

    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, 8(18), 2603-2608.