Gyorgy Keri

Summary

Country: Hungary

Publications

  1. ncbi request reprint Drug discovery in the kinase inhibitory field using the Nested Chemical Library technology
    Gyorgy Keri
    Peptide Biochemistry Research Group of Hungarian Academy of Sciences in Department of Medicinal Chemistry and Pathobiochemistry and Rational Drug Design Laboratory Cooperative Research Center, Semmelweis University, Budapest, Hungary
    Assay Drug Dev Technol 3:543-51. 2005
  2. ncbi request reprint Multidrug transporter ABCG2 prevents tumor cell death induced by the epidermal growth factor receptor inhibitor Iressa (ZD1839, Gefitinib)
    N Barry Elkind
    National Medical Center, Institute of Haematology and Immunology, Membrane Research Group of the Hungarian Academy of Sciences, Budapest, Hungary
    Cancer Res 65:1770-7. 2005
  3. doi request reprint Synthesis and biological evaluation of novel pyrido[2,3-b]pyrazines inhibiting both erlotinib-sensitive and erlotinib-resistant cell lines
    László Kékesi
    Vichem Chemie Research Ltd, Herman Ottó u 15, H 1022 Budapest, Hungary Rational Drug Design Laboratory CRC, Semmelweis University, POB 131, H 1367 Budapest 5, Hungary
    Bioorg Med Chem Lett 23:6152-5. 2013
  4. doi request reprint Small-molecule inhibitors of NADPH oxidase 4
    Gabor Borbely
    Vichem Chemie Research Ltd, Budapest, Hungary
    J Med Chem 53:6758-62. 2010
  5. ncbi request reprint Synthesis and characterization of novel quinazoline type inhibitors for mutant and wild-type EGFR and RICK kinases
    Nora Breza
    Rational Drug Design Laboratory CRC, Semmelweis University, Budapest, Hungary
    J Recept Signal Transduct Res 28:361-73. 2008
  6. doi request reprint Design and synthesis of new imidazo[1,2-a]pyridine and imidazo[1,2-a]pyrazine derivatives with antiproliferative activity against melanoma cells
    Rita Garamvolgyi
    Department of Pharmaceutical Chemistry, Semmelweis University, Budapest, Hungary Vichem Chemie Research Ltd, Budapest, Hungary
    Eur J Med Chem 108:623-43. 2016
  7. ncbi request reprint Comparison of ELISA-based tyrosine kinase assays for screening EGFR inhibitors
    Edit Varkondi
    Rational Drug Design Laboratory CRC, Semmelweis University, Budapest, Hungary
    J Recept Signal Transduct Res 25:45-56. 2005
  8. ncbi request reprint Synthesis of selective SRPK-1 inhibitors: novel tricyclic quinoxaline derivatives
    Zsolt Székelyhidi
    Peptide Biochemistry Res Group of Hung Acad Sci and Cooperative Research Centre, Semmelweis University, Rippl Rónai u 37, Budapest 1062, Hungary
    Bioorg Med Chem Lett 15:3241-6. 2005
  9. doi request reprint Novel compounds reducing IRS-1 serine phosphorylation for treatment of diabetes
    Laura Simon-Szabó
    MTA SE Pathobiochemistry Research Group, Department of Medical Chemistry, Molecular Biology and Pathobiochemistry, Semmelweis University, 1444 Budapest, Hungary
    Bioorg Med Chem Lett 26:424-8. 2016
  10. ncbi request reprint Tyrosine kinase inhibitors - small molecular weight compounds inhibiting EGFR
    Bálint Hegymegi-Barakonyi
    Vichem Chemie Research Ltd, Budapest, Hungary
    Curr Opin Mol Ther 11:308-21. 2009

Collaborators

Detail Information

Publications31

  1. ncbi request reprint Drug discovery in the kinase inhibitory field using the Nested Chemical Library technology
    Gyorgy Keri
    Peptide Biochemistry Research Group of Hungarian Academy of Sciences in Department of Medicinal Chemistry and Pathobiochemistry and Rational Drug Design Laboratory Cooperative Research Center, Semmelweis University, Budapest, Hungary
    Assay Drug Dev Technol 3:543-51. 2005
    ..Applying NCL technology we have developed lead compounds for several validated kinase targets...
  2. ncbi request reprint Multidrug transporter ABCG2 prevents tumor cell death induced by the epidermal growth factor receptor inhibitor Iressa (ZD1839, Gefitinib)
    N Barry Elkind
    National Medical Center, Institute of Haematology and Immunology, Membrane Research Group of the Hungarian Academy of Sciences, Budapest, Hungary
    Cancer Res 65:1770-7. 2005
    ..Therefore, variable expression and polymorphisms of ABCG2 may significantly modify the antitumor effect as well as the absorption and tissue distribution of Iressa...
  3. doi request reprint Synthesis and biological evaluation of novel pyrido[2,3-b]pyrazines inhibiting both erlotinib-sensitive and erlotinib-resistant cell lines
    László Kékesi
    Vichem Chemie Research Ltd, Herman Ottó u 15, H 1022 Budapest, Hungary Rational Drug Design Laboratory CRC, Semmelweis University, POB 131, H 1367 Budapest 5, Hungary
    Bioorg Med Chem Lett 23:6152-5. 2013
    ..The signaling network(s) involved in the mechanism(s) of action of these novel compounds in overcoming erlotinib resistance remain to be elucidated...
  4. doi request reprint Small-molecule inhibitors of NADPH oxidase 4
    Gabor Borbely
    Vichem Chemie Research Ltd, Budapest, Hungary
    J Med Chem 53:6758-62. 2010
    ..Twenty-four compounds inhibited Nox4 activity with low-micromolar IC(50) values of which three were selected for further drug development...
  5. ncbi request reprint Synthesis and characterization of novel quinazoline type inhibitors for mutant and wild-type EGFR and RICK kinases
    Nora Breza
    Rational Drug Design Laboratory CRC, Semmelweis University, Budapest, Hungary
    J Recept Signal Transduct Res 28:361-73. 2008
    ..Selected compounds were tested on wild-type and mutant forms of EGFR, RICK, and pUL97 kinases; their logP and logS values for assessing suitability as drugs were calculated and hit or lead compounds identified...
  6. doi request reprint Design and synthesis of new imidazo[1,2-a]pyridine and imidazo[1,2-a]pyrazine derivatives with antiproliferative activity against melanoma cells
    Rita Garamvolgyi
    Department of Pharmaceutical Chemistry, Semmelweis University, Budapest, Hungary Vichem Chemie Research Ltd, Budapest, Hungary
    Eur J Med Chem 108:623-43. 2016
    ..We found several compounds expressing submicromolar IC50 values against the A375P cells, from which 15d, 17e, 18c, 18h, 18i demonstrated the highest potencies with IC50 below 0.06 μM. ..
  7. ncbi request reprint Comparison of ELISA-based tyrosine kinase assays for screening EGFR inhibitors
    Edit Varkondi
    Rational Drug Design Laboratory CRC, Semmelweis University, Budapest, Hungary
    J Recept Signal Transduct Res 25:45-56. 2005
    ..In conclusion, normalization of the EGFR activity used for inhibitor screening and standardization of detection methods enable safe comparison of data...
  8. ncbi request reprint Synthesis of selective SRPK-1 inhibitors: novel tricyclic quinoxaline derivatives
    Zsolt Székelyhidi
    Peptide Biochemistry Res Group of Hung Acad Sci and Cooperative Research Centre, Semmelweis University, Rippl Rónai u 37, Budapest 1062, Hungary
    Bioorg Med Chem Lett 15:3241-6. 2005
    ..Most of these novel compounds have drug-like properties according to experimentally determined LogP and LogS values...
  9. doi request reprint Novel compounds reducing IRS-1 serine phosphorylation for treatment of diabetes
    Laura Simon-Szabó
    MTA SE Pathobiochemistry Research Group, Department of Medical Chemistry, Molecular Biology and Pathobiochemistry, Semmelweis University, 1444 Budapest, Hungary
    Bioorg Med Chem Lett 26:424-8. 2016
    ..A series of novel pyrido[2,3-d]pyrimidin-7-one derivatives were synthesized as potential antidiabetic agents, preventing IRS-1 phosphorylation at serine 307 in a cellular model of lipotoxicity and type 2 diabetes...
  10. ncbi request reprint Tyrosine kinase inhibitors - small molecular weight compounds inhibiting EGFR
    Bálint Hegymegi-Barakonyi
    Vichem Chemie Research Ltd, Budapest, Hungary
    Curr Opin Mol Ther 11:308-21. 2009
    ..In addition, the use of target fishing for selectivity profiling, off-target identification and quantitative structure-activity relationship modeling for the prediction of EGFR inhibition is discussed...
  11. ncbi request reprint High-affinity interaction of tyrosine kinase inhibitors with the ABCG2 multidrug transporter
    Csilla Ozvegy-Laczka
    National Medical Center, Institute of Hematology and Immunology, Membrane Research Group of the Hungarian Academy of Sciences, Budapest, Hungary
    Mol Pharmacol 65:1485-95. 2004
    ..These data also raise the possibility that an extrusion of TKIs by multidrug transporters, e.g., ABCG2, may be involved in tumor cell TKI resistance...
  12. ncbi request reprint Optimization of important early ADME(T) parameters of NADPH oxidase-4 inhibitor molecules
    Gabor Borbely
    Pathobiochemistry Research Group of Hungarian Academy of Sciences, Department of Medical Chemistry, Semmelweis University, Budapest, Hungary
    Med Chem 8:174-81. 2012
    ....
  13. doi request reprint Synthesis, characterization and systematic comparison of FITC-labelled GnRH-I, -II and -III analogues on various tumour cells
    József Murányi
    MTA SE Pathobiochemistry Research Group, Tuzolto St 37 47, H1094, Budapest, Hungary
    J Pept Sci 22:552-60. 2016
    ..Copyright © 2016 European Peptide Society and John Wiley & Sons, Ltd. ..
  14. pmc Targeting vascular endothelial growth factor receptor 2 and protein kinase D1 related pathways by a multiple kinase inhibitor in angiogenesis and inflammation related processes in vitro
    Attila Varga
    Pathobiochemistry Research Group, Hungarian Academy of Sciences Semmelweis University, Budapest, Hungary
    PLoS ONE 10:e0124234. 2015
    ..In summary, we described a novel function of a multiple kinase inhibitor which strongly inhibits the VEGFR2-PKD1 signaling and might be a novel inhibitor of pathological inflammatory pathways...
  15. ncbi request reprint Comparison of predictive ability of water solubility QSPR models generated by MLR, PLS and ANN methods
    Dániel Eros
    Semmelweis University, Department of Medicinal Chemistry, Biopeptide Research Group of the Hungaian Academy of Sciences, Budapest, Hungary
    Mini Rev Med Chem 4:167-77. 2004
    ..85. These values give a good chance for successful pre-selection of screening compounds from virtual libraries, based on the predicted water solubility...
  16. doi request reprint A novel drug discovery concept for tuberculosis: inhibition of bacterial and host cell signalling
    Rita Székely
    Vichem Chemie Research Ltd, Herman Ottó 15, H 1022 Budapest, Hungary
    Immunol Lett 116:225-31. 2008
    ..In the course of our future work, we will increase the potency of the next generation of PknB inhibitors in order to improve their antibacterial activity...
  17. doi request reprint Interaction of the EGFR inhibitors gefitinib, vandetanib, pelitinib and neratinib with the ABCG2 multidrug transporter: implications for the emergence and reversal of cancer drug resistance
    Csilla Hegedus
    Membrane Research Group of the Hungarian Academy of Sciences, Department of Biophysics, Semmelweis University and National Blood Center, Budapest, Hungary
    Biochem Pharmacol 84:260-7. 2012
    ..In addition, the finding that these EGFR inhibitors efficiently block ABCG2 function may help to design novel drug-combination therapeutic strategies...
  18. doi request reprint Protein kinase inhibitor-induced endothelial cell cytotoxicity and its prediction based on calculated molecular descriptors
    Eszter Herczenik
    Research Group of Inflammation Biology and Immunogenomics, Hungarian Academy of Sciences Semmelweis University, Budapest, Hungary
    J Recept Signal Transduct Res 29:75-83. 2009
    ..Our results show that the cytotoxic effects of PKIs should be taken into account for optimal drug development to overcome endothelial cell-related side effects...
  19. ncbi request reprint A novel plasmin-inhibitor inhibits the growth of human tumor xenografts and decreases metastasis number
    Bela Szende
    1st Institute of Pathology and Experimental Cancer Research, Semmelweis University, Molecular Pathology Research Group of Hungarian Academy of Sciences, Budapest, Hungary
    In Vivo 16:281-6. 2002
    ....
  20. ncbi request reprint Biochemical assay-based selectivity profiling of clinically relevant kinase inhibitors on mutant forms of EGF receptor
    Edit Varkondi
    Rational Drug Design Laboratory CRC, Semmelweis University, Budapest, Hungary
    J Recept Signal Transduct Res 28:295-306. 2008
    ....
  21. ncbi request reprint Improved, high yield synthesis of 3H-quinazolin-4-ones, the key intermediates of recently developed drugs
    Laszlo Orfi
    Department of Pharmaceutical Chemistry, Semmelweis University, Hogyes E u 9, Budapest, Hungary
    Curr Med Chem 11:2549-53. 2004
    ..There was no considerable effect of microwave-, or traditional thermal activation on the yield and compound purity...
  22. pmc NADPH oxidase 4 is expressed in pulmonary artery adventitia and contributes to hypertensive vascular remodeling
    Scott A Barman
    From the Department of Forensic Medicine, Nanjing Medical University, Jiangsu, China F C Department of Pharmacology and Toxicology S A B, Y S, w h, D J R F and Vascular Biology Center F C, C D, Y W, J D S, N B, O R, R R, S M B, D W S, G R, D J R F, Georgia Regents University, Augusta Vichem Chemie, Ltd, Budapest, Hungary L O, C S K, G K, I S Institute for Organic Chemistry, University of Leipzig, Leipzig, Germany A G Institute for Pathology, Hannover Medical School, Hannover, Germany D J Departments of Clinical Laboratories and Biochemistry, University of Texas Health Science Center at San Antonio R A and Pathobiochemical Research Group of Hungarian Academy of Sciences G K and Department of Pharmaceutical Chemistry L O, Semmelweis University, Budapest, Hungary
    Arterioscler Thromb Vasc Biol 34:1704-15. 2014
    ..Therefore, we sought to identify the vascular cells expressing Nox4 in PAs and determine the functional relevance of Nox4 in PH...
  23. ncbi request reprint Determination of human serum alpha1-acid glycoprotein and albumin binding of various marketed and preclinical kinase inhibitors
    Ferenc Zsila
    Department of Molecular Pharmacology, Institute of Biomolecular Chemistry, Chemical Research Center, H 1525, Budapest, P O Box 17, Hungary
    Curr Med Chem 16:1964-77. 2009
    ..Structural, biological and drug binding properties of AAG as well as the applicability of the CD method in studying drug-protein binding interactions are also briefly reviewed...
  24. ncbi request reprint Inhibition of c-Met with the specific small molecule tyrosine kinase inhibitor SU11274 decreases growth and metastasis formation of experimental human melanoma
    Istvan Kenessey
    2nd Institute of Pathology, Semmelweis University, Budapest, Hungary
    Curr Cancer Drug Targets 10:332-42. 2010
    ..Consequently, SU11274 treatment might represent a useful strategy for controlling melanoma progression and metastasis in patients with MM...
  25. ncbi request reprint Comparison of the cytotoxic effects of receptor tyrosine kinase inhibitors on macrophage functions; possible side effects in the immune defense
    András Hrabák
    Department of Medical Chemistry, Molecular Biology and Pathobiochemistry, Semmelweis University, Budapest, Hungary
    Immunol Lett 107:169-75. 2006
    ..However, these side effects may be important when RTK inhibitors are selected against tumor growth, indicating that certain inhibitors may impair the immune defense during therapeutical application...
  26. pmc Metformin attenuates palmitate-induced endoplasmic reticulum stress, serine phosphorylation of IRS-1 and apoptosis in rat insulinoma cells
    Laura Simon-Szabó
    Department of Medical Chemistry, Molecular Biology and Pathobiochemistry, Semmelweis University, Budapest, Hungary MTA SE Pathobiochemistry Research Group, Department of Medical Chemistry, Molecular Biology and Pathobiochemistry, Semmelweis University, Budapest, Hungary
    PLoS ONE 9:e97868. 2014
    ..Our results indicate that the β-cell protective activity of metformin in lipotoxicity can be at least partly attributed to suppression of ER stress. ..
  27. doi request reprint TP53 mutation-correlated genes predict the risk of tumor relapse and identify MPS1 as a potential therapeutic kinase in TP53-mutated breast cancers
    Balazs Gyorffy
    Research Laboratory of Pediatrics and Nephrology, Hungarian Academy of Sciences, Budapest, Hungary Oncogenomic Research Group, 2nd Department of Pediatrics, Semmelweis University, Budapest, Hungary
    Mol Oncol 8:508-19. 2014
    ..Our results collectively demonstrate that TP53-correlated kinase MPS1, is a potential therapeutic target in BC patients with TP53 mutated tumors, and that SP600125 warrant further development in future clinical trials. ..
  28. ncbi request reprint Micellar proportion: a parameter to compare the hydrophobicity of the pseudostationary phases or that of the analytes in micellar electrokinetic chromatography
    Zsófia Dobos
    Peptide Biochemistry Research Group of Hungarian Academy of Sciences and Semmelweis University, Semmelweis University Budapest, Department of Medical Chemistry, Molecular Biology and Pathobiochemistry, Budapest, Hungary
    Electrophoresis 26:849-57. 2005
    ..Z + B, where Z is the number of carbon atoms of the alkyl chain in the alkyl benzene homologous series...
  29. ncbi request reprint Validation subset selections for extrapolation oriented QSPAR models
    Csaba Szántai-Kis
    Cooperative Research Center, Semmelweis University, Pf 131, Budapest 5, Hungary, 1367
    Mol Divers 7:37-43. 2003
    ..e., when the model had to make a lot of extrapolations. We also compared the top final models obtained from external validation set selection methods in three independent and different sizes of 'chemical universe sets'...
  30. doi request reprint Detection of hydrogen peroxide by lactoperoxidase-mediated dityrosine formation
    Agnes Donkó
    Department of Physiology, Semmelweis University, Faculty of Medicine, Budapest, Hungary
    Free Radic Res 43:440-5. 2009
    ..These experiments successfully measured the activity of NADPH oxidase 4 (Nox4) by this method. It was concluded that LPO-mediated dityrosine formation offers a simple way for H2O2 measurement...
  31. pmc Epidermal growth factor receptor (EGFR) high gene copy number and activating mutations in lung adenocarcinomas are not consistently accompanied by positivity for EGFR protein by standard immunohistochemistry
    Ferenc Pinter
    KPS Medical Biotechnology and Healthcare Services, Budapest, Hungary
    J Mol Diagn 10:160-8. 2008
    ..These results indicate that molecular diagnostic methods appear to be most important for the identification of lung adenocarcinoma patients who may benefit from EGFR inhibitor treatments...