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Literature summary extracted from

  • Tiraidis, C.; Alexacou, K.M.; Zographos, S.E.; Leonidas, D.D.; Gimisis, T.; Oikonomakos, N.G.
    FR258900, a potential anti-hyperglycemic drug, binds at the allosteric site of glycogen phosphorylase (2007), Protein Sci., 16, 1773-1782.
    View publication on PubMed

Activating Compound

EC Number Activating Compound Comment Organism Structure
2.4.1.1 AMP physiological activator Oryctolagus cuniculus

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
2.4.1.1 crystal structure of the cocrystallized rabbit muscle glycogen phosphorylase b–FR258900 complex, 2.2 A resolution Oryctolagus cuniculus

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.4.1.1 FR258900 the inhibitor binds at the allosteric activator site, where the physiological activator AMP binds. The contacts from FR258900 to glycogen phosphorylase are dominated by nonpolar van der Waals interactions with Gln71, Gln72, Phe196, and Val459 (from the symmetry-related subunit), and also by ionic interactions from the carboxylate groups to the three arginine residues (Arg242, Arg309, and Arg310) that form the allosteric phosphate-recognition subsite. The binding of FR258900 to the protein promotes conformational changes that stabilize an inactive T-state quaternary conformation of the enzyme Oryctolagus cuniculus

Organism

EC Number Organism UniProt Comment Textmining
2.4.1.1 Oryctolagus cuniculus P00489
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.4.1.1 muscle
-
 Oryctolagus cuniculus
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.4.1.1 glycogen + glucose 1-phosphate
-
 Oryctolagus cuniculus glycogen + phosphate
-
 ?

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.4.1.1 0.00046
-
 FR258900
-
 Oryctolagus cuniculus

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.4.1.1 0.0003
-
-
 Oryctolagus cuniculus FR258900