2GM9

Structure of rabbit muscle glycogen phosphorylase in complex with thienopyrrole

Summary for 2GM9

• Entry DOI: 10.2210/pdb2gm9/pdb
• Related: 2GJ4
• Descriptor: Glycogen phosphorylase, muscle form, (5-HYDROXY-4,6-DIMETHYLPYRIDIN-3-YL)METHYL DIHYDROGEN PHOSPHATE, 2-CHLORO-N-[(3R)-2-OXO-1,2,3,4-TETRAHYDROQUINOLIN-3-YL]-6H-THIENO[2,3-B]PYRROLE-5-CARBOXAMIDE, ... (4 entities in total)
• Functional Keywords: glycogen phosphorylase, transferase
• Biological source: Oryctolagus cuniculus (rabbit)
• Total number of polymer chains: 1
• Total formula weight: 95859.88

Authors

Otterbein, L.R.,Pannifer, A.D.,Tucker, J.,Breed, J.,Oikonomakos, N.G.,Minshull, C.,Rowsell, S.,Pauptit, R.A. (deposition date: 2006-04-06, release date: 2007-02-13, Last modification date: 2024-04-03)

Primary citation

Whittamore, P.R.,Addie, M.S.,Bennett, S.N.,Birch, A.M.,Butters, M.,Godfrey, L.,Kenny, P.W.,Morley, A.D.,Murray, P.M.,Oikonomakos, N.G.,Otterbein, L.R.,Pannifer, A.D.,Parker, J.S.,Readman, K.,Siedlecki, P.S.,Schofield, P.,Stocker, A.,Taylor, M.J.,Townsend, L.A.,Whalley, D.P.,Whitehouse, J.
Novel thienopyrrole glycogen phosphorylase inhibitors: synthesis, in vitro SAR and crystallographic studies.
Bioorg.Med.Chem.Lett., 16:5567-5571, 2006

PubMed Abstract: Two series of novel thienopyrrole inhibitors of recombinant human liver glycogen phosphorylase a (GPa) which are effective in reducing glucose output from rat hepatocytes are described. Representative compounds have been shown to bind at the dimer interface site of the rabbit muscle enzyme by X-ray crystallography.

PubMed: 16945526
DOI: 10.1016/j.bmcl.2006.08.047

Experimental method

X-RAY DIFFRACTION (2.3 Å)