The binding of C5-alkynyl and alkylfurano[2,3-d]pyrimidine glucopyranonucleosides to glycogen phosphorylase b: Synthesis, biochemical and biological assessment

Article ID	Journal	Published Year	Pages	File Type
7802609	European Journal of Medicinal Chemistry	2012	10 Pages	PDF

Abstract

âº Novel C5-alkynyl & furano[2,3-d]pyrimidine nucleosides have been designed and synthesized. âº All compounds except two were low Î¼M inhibitors of the enzyme. âº Three ligands induced significant conformational changes in the 280s loop. âº The most potent inhibitor was able to inhibit GPb activity in HepG2 cells in culture.

Keywords

PLP α-d-glucose 1-phosphate Glc-1-P Pd(PPh3)4 gPb Copper (I) iodide CH3CN EtOAc DMF RMSD CuI N,N-dimethylformamide Ethyl acetate Acetonitrile root-mean-square deviation Inhibitor X-ray crystallography Glycogen metabolism Methanol MeOH Diabetes type 2 pyridoxal 5′-phosphate Glycogen phosphorylase

Related Topics

Physical Sciences and Engineering Chemistry Organic Chemistry

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The binding of C5-alkynyl and alkylfurano[2,3-d]pyrimidine glucopyranonucleosides to glycogen phosphorylase b: Synthesis, biochemical and biological assessment

Authors

A.L. Kantsadi, S. Manta, A.-M.G. Psarra, A. Dimopoulou, C. Kiritsis, V. Parmenopoulou, V.T. Skamnaki, P. Zoumpoulakis, S.E. Zographos, D.D. Leonidas, D. Komiotis,