ISDA: 2GM9

Deposition Date 2006-04-06

Release Date 2007-02-13

Last Version Date 2024-04-03

Entry Detail

PDB ID:

2GM9

Keywords:

TRANSFERASE

Title:

Structure of rabbit muscle glycogen phosphorylase in complex with thienopyrrole

Biological Source:

Source Organism(s):

Oryctolagus cuniculus (Taxon ID: 9986)

Method Details:

Experimental Method:

X-RAY DIFFRACTION

Resolution:

2.30 Å

R-Value Free:

0.24

R-Value Work:

0.18

R-Value Observed:

0.18

Space Group:

P 43 21 2

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Macromolecular Entities

Structures with similar UniProt ID

Protein Blast

Polymer Type:polypeptide(L)
Molecule:Glycogen phosphorylase, muscl
Gene (Uniprot):PYGM
Chain IDs:A
Chain Length:825
Number of Molecules:1
Biological Source:Oryctolagus cuniculus

UniProt ID:P00489 Pfam ID:PF00343 EC:2.4.1.1

Ligand Molecules

3TH

PLR

Primary Citation

Novel thienopyrrole glycogen phosphorylase inhibitors: synthesis, in vitro SAR and crystallographic studies.

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.Show

Bioorg.Med.Chem.Lett. 16 5567 5571 (2006)

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

Abstact

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.

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Primary Citation of related structures

Abstact

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