title: Glycogen phosphorylase inhibitors: a patent review (2008 - 2012).
abstract: BACKGROUND
  Glycogen phosphorylase (GP) is the enzyme responsible for the synthesis of glucose-1-phosphate, the source of energy for muscles and the rest of the body. The binding of different ligands in catalytic or allosteric sites assures activation and deactivation of the enzyme. A description of the regulation mechanism and the implications in glycogen metabolism are given.
  
  
  METHODS
  Deregulation of GP has been observed in diseases such as diabetes mellitus or cancers. Therefore, it appears as an attractive therapeutic target for the treatment of such pathologies. Numbers of inhibitors have been published in academic literature or patented in the last two decades. This review presents the main patent claims published between 2008 and 2012.
  
  
  CONCLUSIONS
  Good inhibitors with interesting IC50 and in vivo results are presented. However, such therapeutic strategy raises questions and some answers are proposed to bring new insights in the field.
authors.affiliation: University of Athens, Department of Pharmacy and Natural Products Chemistry, Athens, Greece.
authors.forename: Nicolas
authors.initials: N
authors.lastname: Gaboriaud-Kolar
authors.forename: Alexios-Leandros
authors.initials: AL
authors.lastname: Skaltsounis
mesh_terms: D000818:Animals; D003920:Diabetes Mellitus / Q000188:drug therapy / Q000201:enzymology; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000008:administration & dosage / Q000494:pharmacology*; D005958:Glucosephosphates / Q000096:biosynthesis / Q000378:metabolism; D006003:Glycogen / Q000378:metabolism; D024981:Glycogen Phosphorylase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D006801:Humans; D020128:Inhibitory Concentration 50; D058990:Molecular Targeted Therapy; D009369:Neoplasms / Q000188:drug therapy / Q000201:enzymology; D010330:Patents as Topic
chemical_list: D004791:Enzyme Inhibitors; D005958:Glucosephosphates; D006003:Glycogen; C031590:glucose-1-phosphate; D024981:Glycogen Phosphorylase