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.
|Number of pages||6|
|Journal||Bioorganic & Medicinal Chemistry|
|Publication status||Published - 22 Sep 1998|
ASJC Scopus subject areas
- Molecular Biology
- Organic Chemistry
- Drug Discovery
- Pharmaceutical Science
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.