Literature DB >> 16945526

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

Paul R O Whittamore1, Matthew S Addie, Stuart N L Bennett, Alan M Birch, Michael Butters, Linda Godfrey, Peter W Kenny, Andrew D Morley, Paul M Murray, Nikos G Oikonomakos, Ludovic R Otterbein, Andrew D Pannifer, Jeremy S Parker, Kristy Readman, Pawel S Siedlecki, Paul Schofield, Andy Stocker, Melvyn J Taylor, Linda A Townsend, David P Whalley, Jennifer Whitehouse.   

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.

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Year:  2006        PMID: 16945526     DOI: 10.1016/j.bmcl.2006.08.047

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  6 in total

1.  Discovering protein-ligand chalcogen bonding in the protein data bank using endocyclic sulfur-containing heterocycles as ligand search subsets.

Authors:  Miguel O Mitchell
Journal:  J Mol Model       Date:  2017-09-24       Impact factor: 1.810

2.  Identification of thieno[3,2-b]pyrrole derivatives as novel small molecule inhibitors of neurotropic alphaviruses.

Authors:  Weiping Peng; Daniel C Peltier; Martha J Larsen; Paul D Kirchhoff; Scott D Larsen; Richard R Neubig; David J Miller
Journal:  J Infect Dis       Date:  2009-04-01       Impact factor: 5.226

3.  An assessment of the in vivo efficacy of the glycogen phosphorylase inhibitor GPi688 in rat models of hyperglycaemia.

Authors:  S M Poucher; S Freeman; S J G Loxham; G Convey; J B Bartlett; J De Schoolmeester; J Teague; M Walker; A V Turnbull; A D Charles; F Carey; S Berg
Journal:  Br J Pharmacol       Date:  2007-10-15       Impact factor: 8.739

4.  Glycogen phosphorylase revisited: extending the resolution of the R- and T-state structures of the free enzyme and in complex with allosteric activators.

Authors:  Demetres D Leonidas; Spyros E Zographos; Katerina E Tsitsanou; Vassiliki T Skamnaki; George Stravodimos; Efthimios Kyriakis
Journal:  Acta Crystallogr F Struct Biol Commun       Date:  2021-08-26       Impact factor: 1.072

Review 5.  Glycogen metabolism has a key role in the cancer microenvironment and provides new targets for cancer therapy.

Authors:  Christos E Zois; Adrian L Harris
Journal:  J Mol Med (Berl)       Date:  2016-02-17       Impact factor: 4.599

Review 6.  Discovery and Biotechnological Exploitation of Glycoside-Phosphorylases.

Authors:  Ao Li; Mounir Benkoulouche; Simon Ladeveze; Julien Durand; Gianluca Cioci; Elisabeth Laville; Gabrielle Potocki-Veronese
Journal:  Int J Mol Sci       Date:  2022-03-11       Impact factor: 5.923

  6 in total

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