Institute of Organic and Pharmaceutical Chemistry

The National Hellenic Research Foundation

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Publications

Peer-Reviewed Journal Articles from Members of SBCG

  1. 1-(3-Deoxy-3-fluoro-beta-d-glucopyranosyl) pyrimidine derivatives as inhibitors of glycogen phosphorylase b: Kinetic, crystallographic and modelling studies. Tsirkone VG, Tsoukala E, Lamprakis C, Manta S, Hayes JM, Skamnaki VT, Drakou C, Zographos SE, Komiotis D, Leonidas DD (2010) Biorg. Med. Chem. 18, 3413-3425

  2. Glucose-based spiro-isoxazolines: a new family of potent glycogen phosphorylase inhibitors.Benltifa M, Hayes JM, Vidal S, Gueyrard D, Goekjian PG, Praly JP, Kizilis G, Tiraidis C, Alexacou KM, Chrysina ED, Zographos SE, Leonidas DD, Archontis G, Oikonomakos NG.(2009) Biorg. Med. Chem. 17,7368-7380.

  3. Mapping the ribonucleolytic active site of bovine seminal ribonuclease. The binding of pyrimidinyl phosphonucleotide inhibitors.  K Dossi, V.G. Tsirkone, J.M. Hayes, J. Matoušek, P. Poučková, J. Souček, M. Zadinova, S.E. Zographos, and D.D. Leonidas (2009) Eur. J. Med. Chem. 44, 4496-4508

  4. Inhibitor design to Ribonuclease A: The binding of two 5´phosphate uridine analogues V.G. Tsirkone, K. Dossi, C. Drakou, S.E. Zographos, M. Kontou and D.D. Leonidas (2009) Acta Crystallogr. F65, 671-677. Cover Story

  5. Amide-1,2,3-triazole bioisosterism: the glycogen phosphorylase case. E.D. Chrysina, É. Bokor; K.-M. Alexacou, M.-D. Charavgi, G.N. Oikonomakos, S. E. Zographos; D.D. Leonidas, N.G. Oikonomakos, and L. Somsák (2009) Tetrahedron Asymm. 20, 733-740.

  6. Influence of Naturally-occurring 5′-Pyrophosphate-linked Substituents on the Binding of Adenylic Inhibitors to Ribonuclease A: an X-Ray Crystallographic Study. Holloway, D.E., Chavali, G.B., Leonidas, D.D., Baker, M.D., and Acharya, K.R. (2009).  Biopolymers 91, 995-1008.

  7. Morpholino, piperidino, and pyrrolidino derivatives of pyrimidine nucleosides as inhibitors of Ribonuclease A: synthesis, biochemical and crystallographic evaluation. Samanta, A., Leonidas, D.D., Dasgupta, S., Pathak, T., Zographos, S.E., and Oikonomakos, N.G. (2009). J. Med. Chem. 52, 932-942

  8. The structure of phosphorylase kinase holoenzyme at 9.9 Ċ resolution and location of the catalytic subunit and the substrate glycogen phosphorylase. Venien-Bryan, C., Jonic, S. Skamnaki, V., Brown, N., Bischler, N., Oikonomakos, N.G., Boisset, N., and Johnson, L.N. (2009). Structure 17, 117-127.

  9. New inhibitors of Glycogen Phosphorylase as potential Antidiabetic Agents. Somsak, L., Czifrak, K., Toth, M., Bokor, E., Chrysina, E.D., Alexacou, K.-M., Hayes, J.M., Tiraidis, C., Lazoura, E., Leonidas, D.D., Zographos, S.E., and Oikonomakos, N.G. (2008). Curr. Med. Chem. 15, 2933-2983.

  10. Pentacyclic triterpenes, inhibitors of glycogen phosphorylase, as potential drugs for type 2 diabetes: X-ray crystallographic studies. Zographos, S.E., Leonidas, D.D., Alexacou, K.M., Gimisis, T., Hayes, J.M., Oikonomakos, N.G, Wen, X., Sun, H., Liu, J., Cheng, K., Zhang, P.,  Zhang, L.,  Hao, J.,  Zhang, L., and  Ni, P. (2008).Planta Medica 74, 1146-1147. 

  11. Naturally Occurring Pentacyclic Triterpenes as Inhibitors of Glycogen Phosphorylase: Synthesis, Structure-Activity Relationships and X-ray Crystallographic Studies. X. Wen, H. Sun, J. Liu, K. Cheng, P. Zhang, L. Zhang, J. Hao, L. Zhang, P. Ni, S.E. Zographos, D. D. Leonidas,K.-M. Alexacou, T. Gimisis, J.M. Hayes, and N.G. Oikonomakos (2008). J. Med. Chem. 51, 3540-3554

  12. X ray sequence ambiguities of Sclerotium rolfsii lectin resolved by mass spectrometry. G.J. Sathisha, Y.K. Subrahmanya Prakash, V.B. Chachadi, N.N. Nagaraja, S.R.Inamdar, D.D. Leonidas, H.S. Savithri, and B.M. Swamy (2008). Amino Acids 5, 309-320

  13. Advances in glycogen phosphorylase inhibitor design. Oikonomakos, N.G, Somsák, L. (2008) Curr Opin Investig Drugs. 4, 379-395

  14. New Synthetic Seven-Membered 1-Azasugars Displaying potent inhibition towards glycosidases and glucosylceramide transferase. Li, H, Liu T, Zhang, Y, Favre, S, Bello, C, Vogel, P, Butters, T.D., Oikonomakos, N.G, Marrot, J., Blériot, Y. (2008) Chembiochem. 9, 253-260

  15. Crystallographic and Computational studies on 4-phenyl-N-(β-D-glucopyranosyl)-1H-1,2,3-triazole-1-acetamide, an inhibitor of glycogen phosphorylase: comparison with a-D-glucose, N-acetyl-b-D-glucopyranosylamine and N-benzoyl-N´-b-D-glucopyranosyl urea binding. K.-M. Alexacou, J.M. Hayes, C. Tiraidis, S.E. Zographos, D.D. Leonidas, E.D. Chrysina, G. Archontis,  N.G. Oikonomakos, J.V. Paul, B. Varghese, and D. Loganathan (2008). Proteins 71, 1307-1323.

  16. FR25900, a potential anti-hyperglycemic drug, binds at the allosteric site of glycogen phosphorylase. C. Tiraidis, K.-M. Alexacou, S.E. Zogrpahos, D.D. Leonidas, T. Gimisis, and N.G. Oikonomakos (2007). Protein Sci 16, 1773-1782.

  17. Differential expression of molecular motors in the motor cortex of sporadic ALS. M. Pantelidou, S.E. Zographos, C.W. Lederer, T. Kyriakides, M.W. Pfaffl, and N. Santama (2007). Neurobiol. Dis. 26, 577-589

  18. Structural basis of the carbohydrate recognition of the Sclerotium rolfsii lectin. D.D. Leonidas, B.M. Swamy, G.N. Hatzopoulos, S.J. Gonchigar, V.B. Chachadi, S.R. Inamdar, S.E. Zographos, and N.G. Oikonomakos (2007). J. Mol. Biol. 368, 1145-1161

  19. In the Search of Glycogen Phosphorylase Inhibitors: Synthesis of C-D-Glycopyranosyl-benzo(hydro) quinones. Inhibition of and binding to glycogen phosphorylase in the crystal. L. He, Y.Z. Zang, M. Tanoh, G.-R. Chen, J.-P. Praly, E.D. Chrysina, M.N. Kosmopoulou, D.D. Leonidas, and N.G. Oikonomakos (2007). Eur. J. Org. Chem. 596-606.

  20. Recognition of Ribonuclease A by 3 '-5'-Pyrophosphate-linked Dinucleotide Inhibitors: a Molecular Dynamics/Continuum Electrostatics Analysis. S. Polydoridis, D.D. Leonidas, N.G. Oikonomakos, and G. Archontis. (2007). Biophys. J.  92, 1659-1672

  21. Regulation of hepatic glycogen metabolism by purine nucleoside site inhibitors of glycogen phosphorylase. Hampson, L.J., Arden, C., Agius, L., Ganotidis, M., Kosmopoulou, M.N., Tiraidis, C., Elemes, Y., Sakarellos, C., Leonidas, D.D., and Oikonomakos, N.G. (2006).  Bioorg. Med. Chem. 14, 7835-7845

  22. Development of potent, orally active 1-substituted-3,4-dihydro-2-quinolone glycogen phosphorylase inhibitors. Birch, A.M., Kenny, P.W., Oikonomakos, N.G., Otterbein, L.R., Schofield, P., Whittamore, P.R.O., and Whalley, D.P. (2006).  Bioorg. Med. Chem. Lett., 17, 394-399..

  23. Iminosugars as potential inhibitors of glycogenolysis: structural insights into the molecular basis of glycogen phosphorylase inhibition. Oikonomakos, N.G., Tiraidis, C., Leonidas, D.D., Zographos, S.E., Kristiansen, M., Jessen, C.U., Nørskov-Lauritsen, L., and Agius, L. (2006). J. Med. Chem. 49, 5687-5701.

  24. Novel thienopyrrole glycogen phosphorylase inhibitors: synthesis, in vitro SAR and crystallographic studies. Whittamore, P.R.O., Addie, M.S., Bennett, S.N.L., 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., and Whitehouse, J. (2006). . Bioorg. Med. Chem. Lett. 16, 5567-5571.

  25. The binding of 3´-N-piperidine-4-carboxyl-3´-deoxy-ara-uridine to Ribonuclease A in the crystal. D.D. Leonidas, T.K. Maiti, A. Samanta, S. Dasgupta, T. Pathak, S.E. Zographos, and N.G. Oikonomakos (2006). Bioorg. Med. Chem. 14, 6055-6064.

  26.  Indirubin and indigo analogues as potential inhibitors of glycogenolysis: structural basis of glycogen phosphorylase inhibition. N. G. Oikonomakos, M. N. Kosmopoulou, D. D. Leonidas, E. D. Chrysina, C. Tiraidis, N. Bischler, K. E. Tsitsanou, S. E. Zographos, I. D. Kostas, and G. Eisenbrand (2006). Indirubin, the red shade of indigo (Meijer L., Guyard N., Skaltsounis L. & Eisenbrand G., eds) 18, 177-189.

  27. Crystallographic studies on N-azidoacetyl-beta-D-glucopyranosylamine, an inhibitor of glycogen phosphorylase: comparison with N-acetyl-beta-D-glucopyranosylamine. E.I. Petsalakis, E.D. Chrysina, C. Tiraidis, T. Hadjiloi, D.D. Leonidas, N.G. Oikonomakos, U. Aich, B. Varghese, and D. Loganathan (2006). Bioorg. Med. Chem. 14, 5316-5324.

  28.  Binding of oxalyl derivatives of beta-d-glucopyranosylamine to muscle glycogen phosphorylase b. T. Hadjiloi, C. Tiraidis, E.D. Chrysina, D.D. Leonidas, N.G. Oikonomakos, P. Tsipos, and T. Gimisis. (2006) Biorg. Med. Chem. 14, 3872-3882. Cover Story

  29. Crystallographic studies on two bioisosteric analogues, N-acetyl-beta-d-glucopyranosylamine and N-trifluoroacetyl-beta-d-glucopyranosylamine, potent inhibitors of muscle glycogen phosphorylase. E. Anagnostou, M.N. Kosmopoulou, E.D. Chrysina, D.D. Leonidas, T. Hatdjiloi, C. Tiraidis, S.E. Zographos, Z. Gyorgydeak, L. Somsak, T. Dosca, P. Gergely, F.N. Kolisis, and N.G. Oikonomakos (2006). Bioorg. Med. Chem. 14, 181-189. Cover Story

  30.  Indirubin-3'-Aminooxy-Acetate inhibits glycogen phosphorylase by binding at the inhibitor and the allosteric site. Broad specificities of the two sites. M.N. Kosmopoulou, D.D. Leonidas, E.D. Chrysina, G. Eisenbrand, and N.G. Oikonomakos (2005). Lett. Drug Des. Disc. 2, 377-390  Cover story

  31. The binding of IMP to Ribonuclease A. G.N. Hatzopoulos, D.D. Leonidas, R. Kardakaris, J. Kobe, and N.G. Oikonomakos (2005). FEBS J 272, 3988-4001

  32. Crystallographic studies on acyl ureas, a new class of glycogen phosphorylase inhibitors, as potential antidiabetic drugs. N.G. Oikonomakos, M.N. Kosmopoulou, E.D. Chrysina, D.D. Leonidas, I.D. Kostas, K.U. Wendt, T. Klabunde, and E. Defossa (2005). Protein Sci. 14, 1760-1771

  33. Kinetic and crystallographic studies on 2-((-D-glucopyranosyl)-5-methyl-1,3,4-oxadiazole,-benothiazole, and -benzimidazole, inhibitors of muscle glycogen phosphorylase b. Evidence for a new binding site. E.D. Chrysina, M.N. Kosmopoulou, C. Tiraidis, R. Kardakaris, N. Bischler, D.D. Leonidas, Z. Hadady, L. Somsak, T. Docsa, P. Gergely, and N.G. Oikonomakos. (2005).  Protein Sci. 14, 873-888.

  34. Binding of beta-D-glucopyranosyl bismethoxyphosphoramidate to glycogen phosphorylase b: Kinetic and crystallographic studies. E.D. Chrysina, M.N. Kosmopoulou, R. Kardakaris, N. Bischler, D.D. Leonidas, T. Kannan, D. Loganathan, and N.G. Oikonomakos (2005). Bioorg. Med. Chem. 13, 765-772

  35. Binding of the potential antitumour agent indirubin-5-sulphonate at the inhibitor site of rabbit muscle glycogen phosphorylase b. M.N. Kosmopoulou, D.D. Leonidas, E.D. Chrysina, N. Bischler, G. Eisenbrand, C.E. Sakarellos, R. Pauptit, and N.G. Oikonomakos. (2004) Eur. J. Biochem.271, 2280-2290.

  36.  High resolution crystal structures of Ribonuclease A complexed with adenylic and uridylic nucleotide inhibitors. Implications for structure-based design of ribonucleolytic inhibitors. D.D. Leonidas, G.B. Chavali, N.G. Oikonomakos, E.D. Chrysina, M.N. Kosmopoulou, M.Vlassi, C. Frankling, and K.R. Acharya  (2003) Protein Sci. 12, 2559-2574. Cover Story

  37. Crystallographic studies on alpha- and beta-D-glucopyranosyl formamide analogues, inhibitors of glycogen phosphorylase. E.D. Chrysina, N.G. Oikonomakos, S.E. Zographos, M.N. Kosmopoulou, N. Bischler, D.D. Leonidas, L. Kovács, T. Docsa, P. Gergely, and L. Somsák (2003) Biocatal. & Biotransfor. 21, 233-242.

  38. The binding of beta- and gamma-cyclodextrins to glycogen phosphorylase b: kinetic and crystallographic studies. N. Pinotsis, D.D. Leonidas, E.D. Chrysina, N.G. Oikonomakos, and I.M. Mavridis (2003) Protein Sci. 12, 1914-1924.  Cover Story

  39. Crystal structure of rabbit muscle glycogen phosphorylase a in complex with a potential hypoglycaemic drug at 2.0 Å resolution. N.G. Oikonomakos, E.D. Chrysina, M.N. Kosmopoulou, and D.D. Leonidas (2003) Biochim. Biophys. Acta 1647, 325-332.

  40. Crystallization and preliminary X-ray crystallographic analysis of Sclerotium rolfssii lectin. D.D. Leonidas, B.M. Swamy, A.G. Bhat, S.R. Inamdar, M.N. Kosmopoulou, E.D. Chrysina, and N.G. Oikonomakos (2003) Acta Cryst. D59, 363-365.

  41. Guest-host crosstalk in angiogenin/RNase A chimeric protein. D.E. Holloway, R. Shapiro, M.C. Hares, D.D. Leonidas and K.R. Acharya (2002) Biochemistry 41, 10482-10489.

  42. Oikonomakos, N.G., Skamnaki, V.T., Osz, E., Szilagyi, L., Somsak, L., Docsa, T., Toth, B. and Gergely, P. (2002). Kinetic and crystallographic studies of glucopyranosylidene spirothiohydantoin binding to glycogen phosphorylase b. Bioorg. Med. Chem. 10, 261-268. {PDB code: 1HLF}

  43. Cook, A., Lowe, E.D., Chrysina, E.D., Skamnaki, V.T. Oikonomakos, N.G. and Johnson, L.N. (2002). Structural studies of Phospho-CDK2/Cyclin A bound to nitrate, a transition state analogue: Implications for the protein kinase mechanism. Biochemistry 41, 7301-7311. {PDB code: 1GY3}

  44. Oikonomakos, N.G. (2002). Glycogen phosphorylase as a molecular target for type 2 diabetes therapy. Curr Protein Pept Sci. 3, 561-586. Cover Story

  45. The 1.76 A resolution crystal structure of glycogen phosphorylase b complexed with glucose, and CP320626, a potential antidiabetic drug. N.G. Oikonomakos, S.E. Zographos, V.T. Skamnaki, and G. Archontis (2002).  Bioorg. Med. Chem. 10, 1313-1319. {PDB code: 1H5U}

  46. Charcot-Leyden Crystal protein (galectin-10) is not a dual-function galectin with lysophospholipase activity, but binds a lysophospholipase inhibitor in a novel structural function. S.J. Ackerman, L. Liu, M.A. Kwatia, M.P. Savage, D.D. Leonidas, G.J. Swaminathan, and K.R. Acharya (2002) J. Biol. Chem. 277, 14859-14868.

  47.  The binding of N-acetyl- and N-benzoyl-N' -beta-D-glucopyranosyl urea to glycogen phosphorylase b: Kinetic and crystallographic studies. N.G. Oikonomakos, M. Kosmopoulou, S.E. Zographos, D.D. Leonidas, L. Somsak, V. Nagy, J.-P. Praly, T. Docsa, B. Toth, & P. Gergely (2002) Eur. J. Biochem. 269, 1684-1696.  Cover Story 

  48. Crystallographic Studies on the Role of the C-terminal Segment of Human Angiogenin in Defining Enzymatic Potency. D.D. Leonidas, R. Shapiro, G.V. Subbarao, A. Russo & K.R. Acharya (2002) Biochemistry 41, 2552-2562.

  49. Cleavage of 3',5'-pyrophosphate-linked dinucleotides by Ribonuclease A and Angiogenin. A.M. Jardine, D.D. Leonidas, J.L. Jenkins, C. Park, R.T. Raines, K.R. Acharya & R. Shapiro (2001) Biochemistry 40, 10262-10272.

  50. Binding of phosphate and pyrophosphate ions at the active site of human angiogenin as revealed by X-ray crystallography. D.D. Leonidas, G.B. Chavali, A.M. Jardine, S. Li, R. Shapiro & K.R. Acharya (2001) Protein Sci. 10, 1669-1676.

  51. Crystal structure of the Eosinophil Major Basic Protein at 1.8Å: An atypical lectin with a paradigm shift in specificity. G.J. Swaminathan, A.J. Weaver, D.A. Loegering, J.L. Checkel , D.D. Leonidas, G.J. Gleich & K.R. Acharya (2001) J. Biol. Chem. 276, 26197-26203

  52. Crystallization and preliminary investigations on a telomeric repeat sequence C4 A2C4A2.G. Savitha, D. Leonidas, K.R. Acharya & M.A. Viswamitra (2001) Acta Cryst. D57, 873-875.

  53. Mapping the ribonucleolytic active site of eosinophil-derived neurotoxin (EDN): High resolution crystal structures of EDN complexes with adenylic nucleotide inhibitors. D.D. Leonidas, E. Boix, R. Prill, M. Suzuki, R. Turton, K. Minson, G.J. Swaminathan, R.J. Youle, & K.R. Acharya (2001). J. Biol. Chem. 276, 15009-15017

  54. Poulas K, Eliopoulos E., Vatzaki E., Navaza J., Kontou M., Oikonomakos N., Acharya K.R., Tzartos S.J. (2001). Crystal structure of Fab198, an efficient protector of the acetylcholine receptor against myasthenogenic antibodies. Eur. J. Biochem., 268, 3685-93. {PDB code: 1FN4}

  55. The crystal structure of Human Placenta Growth Factor-1 (PlGF-1), an angiogenic protein at 2.0 Å resolution S. Iyer, D.D. Leonidas, G.J. Swaminathan, D. Maglione, M. Battisti, M. Tucci, M. G. Persico, & K.R. Acharya  (2001). J. Biol. Chem., 276, 12153-12161

  56. Tsitsanou, K.E., Skamnaki, V.T., and  Oikonomakos, N.G. (2000). Structural basis of the synergistic inhibition of glycogen phosphorylase a by caffeine and a potential antidiabetic drug. Arch. Biochem. Biophys. 384, 245-254. {PDB code: 1C8L}

  57. Skamnaki, V.T., Oikonomakos, N.G. (2000). Kinetic characterization of the double mutant R148A/E182S of glycogen phosphorylase kinase catalytic subunit: the role of the activation loop. J. Protein Chem. 19, 499-505.

  58. Oikonomakos, N.G., Schnier, J.B., Zographos, S.E., Skamnaki, V.T., Tsitsanou, K.E., and Johnson, L.N. (2000). Flavopiridol inhibits glycogen phosphorylase by binding at the inhibitor site. J. Biol. Chem. 275, 34566-34573. {PDB code: 1C8K}

  59. Oikonomakos, N.G., Skamnaki, V.T., Tsitsanou, K.E., Gavalas, N.G., and Johnson, L.N. (2000). A new allosteric site in glycogen phosphorylase b as a target for drug interactions. Structure 8, 575-584. {PDB code: 1C50}

  60. The crystal structure of the Fab fragment of a rat monoclonal antibody against the main immunogenic region of the human muscle acetylcholine receptor. M. Kontou, D.D. Leonidas, E.H. Vatzaki, P. Tsantili, A. Mamalaki, N.G. Oikonomakos, K.R. Acharya & S.J. Tzartos (2000). Eur. J. Biochem., 267, 2389-2397.

  61. Oikonomakos, N.G., Tsitsanou, K.E., Zographos, S.E., Skamnaki, V.T., Goldmann, S., and Bischoff, H. (1999). Allosteric inhibition of glycogen phosphorylase a by the potential antidiabetic drug 3-isopropyl-(2-chlorophenyl)-1,4-dihydro-1-ethyl-2-methyl-pyridine-3,5,6-tricarboxylate. Protein Sci 8, 1930-1945. {PDB code: 2GPA, 3AMV}

  62. Skamnaki, V.T., Owen, D.J., Noble, M.E.M., Lowe, D., Oikonomakos, N.G., and Johnson, L.N. (1999). Catalytic mechanism of phosphorylase kinase probed by mutational studies. Biochemistry 38, 14718-14730.

  63. Tsitsanou, K.E., Oikonomakos, N.G., Zographos, S.E., Skamnaki, V.T., Gregoriou, M., Watson, K.A., Johnson, L.N., and Fleet, G.W.J. (1999). Effects of commonly used cryoprotectants on glycogen phosphorylase activity and structure. Protein Sci. 8, 741-749. {PDB codes: 1BX3, 1B4D} Cover Story

  64. Crystal structure of eosinophil cationic protein at 2.4 Å resolution.E. Boix, D.D. Leonidas, Z. Nikolovski, M.V. Nogués, C.M. Cuchillo, & K.R. Acharya (1999). Biochemistry 38, 16794-16801.

  65. Selective recognition of Mannose by the Human Eosinophil Charcot-Leyden Crystal Protein (Galectin-10): A crystallographic study at 1.8 Å resolution. G.J. Swaminathan, D.D. Leonidas, M.P. Savage, S.J. Ackerman, & K.R. Acharya (1999). Biochemistry 38, 13837-13843 .

  66. Toward rational design of Ribonuclease inhibitors: high-resolution crystal structure of a Ribonuclease A complex with a potent 3',5'-pyrophosphate-linked dinucleotide inhibitor. D.D. Leonidas, R. Shapiro, L.I. Irons, N. Russo, & K.R. Acharya (1999). Biochemistry 38, 10287-1029.

  67. Crystal structure of a hybrid between Ribonuclease A and Bovine Seminal Ribonuclease: The Basic surface, at 2.0 Å resolution. E.H. Vatzaki, S.C. Allen, D.D. Leonidas, K. Trautwein-Frirz, S. A. Benner, & K.R. Acharya (1999). Eur. J. Biochem. 260, 176-182

  68. Refined crystal structures of native human Angiogenin and two active site variants:Implications for the unique functional properties of an enzyme involved in neovascularisation during tumour growth. D.D. Leonidas, R. Shapiro, S.C. Allen, G.V. Subbarao, K. Veluraja, & K.R. Acharya (1999). J. Mol. Biol. 283, 1209-1233 .

  69. Fleet, G.W.J., Estevez, J.C., Smith, M.D., Bleriot, Y., Carmen de la Fuente, Krulle, T.M., Besra, G.S., Brennan, P.J., Nash, R.J., Johnson, L.N., Oikonomakos, N.G., and Stalmans, W. (1998).Sugar mimics from sugar lactones. Pure and Applied Chemistry 70, 279-284.

  70. Gregoriou, M., Noble, M.E.M., Watson, K.A., Garman, E.F., Krulle, T.M., Fuente, C., Fleet, G.W.J., Oikonomakos, N.G., and Johnson, L.N. (1998). The structure of a glycogen phosphorylase glucopyranose spirohydantoin complex at 1.8   resolution and 100 K: the role of the water structure and its contribution to binding. Protein Sci. 7, 915-927. {PDB code: 1A8I, 2GPN}

  71. Heightman, T.D., Vasella, A., Tsitsanou, K.E., Zographos, S.E., Skamnaki, V.T., and Oikonomakos, N.G. (1998). Cooperative interactions of the catalytic nucleophile and the catalytic acid in the inhibition of alpha-glycosidases. Calculations and their validation by comparative kinetic and structural studies of the inhibition of glycogen phosphorylase b. Helv. Chem. Acta 81, 853-864. {PDB code: 1AXR}

  72. Structural studies on Angiogenin, a protein implicated in neovascularization during tumour growth. K.R. Acharya, D.D. Leonidas, A.C. Papageorgiou, N. Russo, & R. Shapiro (1998). In Angiogenesis:Models, Modulators, and Clinical Applications (M.Maragoudakis ed.) Plenum Press, New York, pp. 165-178.

  73. Structural basis for the recognition of carbohydrates by human galectin-7. D.D. Leonidas, E.H. Vatzaki, H. Vorum, J.E. Celis, P. Madsen, & K.R. Acharya (1998). Biochemistry 37, 13930-18.

  74. The structure of glycogen phosphorylase b with an alkyl-dicarboxylic acid compound, novel and potent inhibitor. S.E. Zographos, N.G. Oikonomakos, K.E. Tsitsanou, D.D. Leonidas, E.D. Chrysina, V.T. Skamnaki, H. Bischoff, S. Goldmann, M. Schramm, K.A. Watson, & L.N. Johnson, (1997). Structure 5, 1413-1425.

  75. Crystal structures of ribonuclease A complexes with 5'- diphosphoadenosine 3'-phosphate and 5'-diphosphoadenosine 2'- phosphate at 1.7 Å resolution. D.D. Leonidas, R. Shapiro, L.I. Irons, N. Russo, & K.R. Acharya (1997). Biochemistry 36, 5578-5588.

  76. Lowe, E.D., Noble, M.E.M., Skamnaki, V.T., Oikonomakos, N.G., Owen, D.J., and Johnson, L.N. (1997). The crystal structure of a phosphorylase kinase peptide substrate complex: kinase substrate recognition. EMBO J. 16, 6646-6658. {PDB code: 2PHK}

  77. Krulle, T.M., Fuente, C., Watson, K.A., Gregoriou, M., Johnson, L.N., Tsitsanou, K.E., Zographos, S.E., Oikonomakos, N.G., and Fleet, G.W.J. (1997). Stereospecific synthesis of spirohydantoins of beta-glucopyranose: Inhibitors of glycogen phosphorylase. Synlett. 1997, 211-213.

  78. Zographos, S.E., Oikonomakos, N.G., Tsitsanou, K.E., Leonidas, D.D., Chrysina, E.D., Skamnaki, V.T., Bischoff, H., Goldman, S., Schram, M., Watson, K.A. and Johnson, L.N. (1997). The structure of glycogen phosphorylase b with an alkyl-dihydropyridine-dicarboxylic acid compound, a novel and potent inhibitor. Structure 5, 1413-1425. {PDB code: 2AMV}

  79. Fuente, C., Krulle, T.M., Watson, K.A., Gregoriou, M., Johnson, L.N., Tsitsanou, K.E., Zographos, S.E., Oikonomakos, N.G., and Fleet, G.W.J. (1997). Glucopyranose Spirohydantoins: Specific inhibitors of glycogen phosphorylase. Synlett. 1997, 485-487.

  80. The refined crystal structure of Toxic Shock Syndrome Toxin at 2.07 Å resolution. A.C. Papageorgiou, R.D. Brehm, D.D. Leonidas, H.S. Tranter, & K.R. Acharya (1996). J. Mol. Biol. 260, 553-569 .

  81. Oikonomakos, N.G., Zographos, S.E., Tsitsanou, K.E., Johnson, L.N. and Acharya, K.R. (1996). Activator anion site in pyridoxal phosphorylase b : The binding of phosphite, phosphate and fluorophosphate anions in the crystal. Protein Sci. 5, 2416-2428. {PDB codes: 2SKC, 2SKD, 2SKE}

  82. Kontou, M., Vatzaki, E.H., Kokla, A., Acharya, K.R., Oikonomakos, N.G., and Tzartos, S.J. (1996). Characterisation, crystallisation and preliminary X-ray diffraction analysis of a Fab fragment of a rat monoclonal antibody with very high affinity for the human muscle acetylcholine receptor. FEBS Lett. 389, 195-198.

  83. Mitchell, E.P., Withers, S.G., Emert, P., Vasella, A.T., Garman, E.F., Oikonomakos, N.G. and Johnson, L.N. (1996).Ternary complex crystal structures of glycogen phosphorylase with a transition state analogue nojirimycin tetrazole and phosphate in the T and R states. Biochemistry 35, 7341-7355. {PDB codes: 1NOI, 1NOJ, 1NOK}

  84.  Crystal structure of human Charcot-Leyden crystal protein, an eosinophil lysophospholipase, identifies it as a new member of the carbohydrate-binding family of galectins. D.D. Leonidas, B.L. Elbert, Z. Zhou, H. Leffler, S.J. Ackerman, & K.R. Acharya (1995). Structure 3, 1379-1393 Cover Story

  85. Sulphate-activated phosphorylase b : the pH-dependence of catalytic activity. S.E. Zographos,  N.G. Oikonomakos, H.B.F. Dixon, W.G. Griffin, L.N. Johnson, & D.D. Leonidas (1995). Biochem. J.  310, 565-570.

  86. Oikonomakos, N.G., Zographos, S.E., Johnson, L.N., Papageorgiou, A.C., and Acharya, K.R. (1995). The binding of 2-deoxy-glucose-6-phosphate to glycogen phosphorylase b: kinetic and crystallographic studies. J. Mol. Biol. 253, 114-131. {PDB code: 2PRI}

  87. Watson, K.A., Mitchell, E.P., Johnson, L.N., Cruciani, G., Son, J.C., Bichard, C.J.F., Fleet, G.W.J., Oikonomakos, N.G., Kontou, M., and Zographos, S.E. (1995). Glucose analogue inhibitors of glycogen phosphorylase: from crystallographic analysis to drug prediction using GRID force-field and GOLPE variable selection. Acta Crystallogr. D51, 458-472.

  88. Oikonomakos, N.G., Kontou, M., Zographos, S.E., Watson, K.A., Johnson, L.N., Bichard, C.J.F., Fleet, G.W.J., and Acharya, K.R. (1995). N-acetyl-beta-D-glucopyranosylamine: a potent T state inhibitor of glycogen phosphorylase. A comparison with alpha-D-glucose. Protein Sci. 4, 2469-2477. {PDB code: 2PRJ}

  89. Bichard, C.J.F., Mitchell, E.P., Wormald, M.R., Watson, K.A., Johnson, L.N., Zographos, S.E., Koutra, D.D., Oikonomakos, N.G. and Fleet, G.W.J. (1995). Potent inhibition of glycogen phosphorylase by a spirohydantoin of glucopyranose: first pyranose analogues of hydantocidin. Tetrahedron Lett. 36, 2145-2148.

  90. The design of potential antidiabetic drugs - experimental investigation of a number of beta-D-glucose analog inhibitors of glycogen phosphorylase. N.G. Oikonomakos, M. Kontou, S.E. Zographos, H.S. Tsitoura, L.N. Johnson, K.A. Watson, E.P. Mitchell, G.W.J. Fleet, J.C. Son, C.J.F. Bitchard, D.D. Leonidas, & K.R. Acharya (1994). Eur. J. Drug Metab. Pharmacokinet. 19, 185-192.

  91. Design of inhibitors of glycogen phosphorylase: A study of  alpha- and beta-C- glucosides and 1-thio-beta-D-glucose compounds. K.A. Watson, E.P. Mitchell, L.N. Johnson, J.C. Son, C.J.F. Bitchard, M.G. Orchard, G.W.J. Fleet, N.G. Oikonomakos, D.D. Leonidas, M. Kontou, & A.C. Papageorgiou, (1994). Biochemistry 33, 5745-5758.

  92. Vatzaki, E.H., Acharya, K.R., Oikonomakos, N.G., and Tzartos, S.J. (1993). Crystallization and preliminary crystallographic study of an Fab fragment of a pathogenic rat monoclonal antibody against the nicotinic acetylcholine receptor. Protein Sci. 2, 1770-1772.

  93. Johnson, L.N., Snape, P., Martin, J.L., Acharya, K.R., Barford, D., and Oikonomakos, N.G. (1993). Crystallographic binding studies on the allosteric inhibitor glucose-6-phosphate to T state glycogen phosphorylase b. J. Mol. Biol. 232, 253-267. {PDB code: 1GPY}

  94. Watson, K.A., Mitchell, E.P., Johnson, L.N., Son, J.C., Bichard, C.J.F., Fleet, G.W.J., Ford, P., Watkin, D.J., and Oikonomakos, N.G. (1993). X-ray crystallographic analysis of 2,6-anhydro-N-methyl-D-glycero-D-ido-heptonamide: the first example of a simple glucose analogue with a skew boat structure. J. Chem. Soc. Chem. Commun. 654-656.

  95. Control of phosphorylase b by a modified cofactor : Crystallographic studies on R-state Glycogen Phosphorylase reconstituted with Pyridoxal 5'-diphosphate. D.D. Leonidas, N.G. Oikonomakos, A.C. Papageorgiou, K.R. Acharya, D. Barford, & L.N. Johnson, (1992). Protein Sci. 1, 1112-1122.

  96. Kinetic Properties of tetrameric glycogen phosphorylase b in solution and in the crystalline state. D.D. Leonidas, N.G. Oikonomakos, A.C. Papageorgiou, & T.G. Sotiroudis, (1992) Protein Sci. 1, 1123-1132.

  97. Glucose analogue inhibitors of glycogen phosphorylase : the design of potential drugs for diabetes. J.L. Martin, K. Velouraja, K. Ross, L.N. Johnson, G.W.J. Fleet, N.G. Ramsden, I. Bruce, M.G. Orchard, N.G. Oikonomakos, A.C. Papageorgiou, D.D. Leonidas, & H.S. Tsitoura, (1991). Biochemistry 30, 10101-10116.

  98. Sulphate activates phosphorylase b by binding to the Ser (P) site. D.D. Leonidas, N.G. Oikonomakos, & A.C. Papageorgiou, (1991). Biochim. Biophys. Acta 1076, 305-307.

  99. The binding of D-gluconhydroximo-1,5-lactone to glycogen phosphorylase: Kinetic, ultracentrifugation, and crystallographic studies. A.C. Papageorgiou, N.G. Oikonomakos, D.D. Leonidas, D. Barford, J.L. Martin, K.R. Acharya, L.N. Johnson, B. Bernet, D. Beer, & A. Vasella, (1991). Biochem. J. 274, 329-338.

  100. The ammonium sulfate activation of phosphorylase b. D.D. Leonidas, N.G. Oikonomakos, A.C. Papageorgiou, A. Xenakis, C.T. Cazianis, & F. Bem, (1990). FEBS Lett. 261, 23-27.

  101. Inhibition of rabbit muscle glycogen phosphorylase by D-Gluconhydroximo-1,5 lactone-N-phenylurethane. A.C. Papageorgiou, N.G. Oikonomakos, & D.D. Leonidas (1989). Arch. Biochem. Biophys. 272, 376-385.

 

 


 
 

 

 

 

Research Interests:

Control of glycogen metabolism

Phosphoenolpyruvate carboxykinase

Pancreatic glucokinase

Ribonucleases

Carbohydrate recognition
Human TAFs9 proteins
Xylanases and feruloyl esterases

Olfactory Binding Proteins
 

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