Auflistung nach Autor "Kontopidis, G."
Anzeige der Dokumente 1-20 von 24
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4-Arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects
Kryštof, V.; Cankař, P.; Fryšová, I.; Slouka, J.; Kontopidis, G.; Džubák, P.; Hajdúch, M.; Srovnal, J.; De Azevedo Jr, W. F.; Orság, M.; Paprskářová, M.; Rolčík, J.; Látr, A.; Fischer, P. M.; Strnad, M. (2006)In a routine screening of our small-molecule compound collection we recently identified 4-arylazo-3,5-diamino-1H-pyrazoles as a novel group of ATP antagonists with moderate potency against CDK2-cyclin E. A preliminary SAR ... -
beta-Lactoglobulin improves liposome's encapsulation properties for vitamin E delivery
Rovoli, M.; Gortzi, O.; Lalas, S.; Kontopidis, G. (2014)Vitamin E (VE) or alpha-tocopherol is the major fat-soluble antioxidant in the human body. It is a sensitive, easily oxidized in the air, molecule, so it must be protected from pro-oxidant elements which could affect its ... -
Catch the kinase conformer
McInnes, C.; Mezna, M.; Kontopidis, G. (2006)Protein kinases exist in inactive and active states, but little attention has been paid to which state is or should be the target in drug discovery efforts. In this issue of Chemistry & Biology, Okram et al. [1] tackle ... -
Design, synthesis, and evaluation of 2-methyl- and 2-amino-N-aryl-4,5- dihydrothiazolo[4,5-h]quinazolin-8-amines as ring-constrained 2-anilino-4-(thiazol-5-yl)pyrimidine cyclin-dependent kinase inhibitors
McIntyre, N. A.; McInnes, C.; Griffiths, G.; Barnett, A. L.; Kontopidis, G.; Slawin, A. M. Z.; Jackson, W.; Thomas, M.; Zheleva, D. I.; Wang, S.; Blake, D. G.; Westwood, N. J.; Fischer, P. M. (2010)Following the recent discovery and development of 2-anilino-4-(thiazol-5- yl)pyrimidine cyclin dependent kinase (CDK) inhibitors, a program was initiated to evaluate related ring-constrained analogues, specifically, 2-methyl- ... -
Development and Evaluation of a Novel Membrane Mimic System (PC/CHOL Liposome-beta-Lg Formulation) for Vitamin E Delivery
Rovoli, M.; Gortzi, O.; Lalas, S.; Kontopidis, G. (2012) -
Development and Evaluation of a Phospholipid-sterol-protein Membrane Resembling System
Gortzi, O.; Rovoli, M.; Lalas, S.; Kontopidis, G. (2015)The development and evaluation of a phospholipid-sterol-protein membrane resembling system containing beta-lactoglobulin (beta-Lg) has been studied. Liposomes have been successfully employed for the protection, controlled ... -
Discovery and characterization of 2-anilino-4- (thiazol-5-yl)pyrimidine transcriptional CDK inhibitors as anticancer agents
Wang, S.; Griffiths, G.; Midgley, C. A.; Barnett, A. L.; Cooper, M.; Grabarek, J.; Ingram, L.; Jackson, W.; Kontopidis, G.; McClue, S. J.; McInnes, C.; McLachlan, J.; Meades, C.; Mezna, M.; Stuart, I.; Thomas, M. P.; Zheleva, D. I.; Lane, D. P.; Jackson, R. C.; Glover, D. M.; Blake, D. G.; Fischer, P. M. (2010)The main difficulty in the development of ATP antagonist kinase inhibitors is target specificity, since the ATP-binding motif is present in many proteins. We introduce a strategy that has allowed us to identify compounds ... -
Discovery of N-Phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors
Wang, S.; Midgley, C. A.; Scaërou, F.; Grabarek, J. B.; Griffiths, G.; Jackson, W.; Kontopidis, G.; McClue, S. J.; McInnes, C.; Meades, C.; Mezna, M.; Plater, A.; Stuart, I.; Thomas, M. P.; Wood, G.; Clarke, R. G.; Blake, D. G.; Zheleva, D. I.; Lane, D. P.; Jackson, R. C.; Glover, D. M.; Fischer, P. M. (2010)Through cell-based screening of our kinase-directed compound collection, we discovered that a subset of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amines were potent cytotoxic agents against cancer cell lines, suppressed mitotic ... -
Efficient soluble expression of active recombinant human cyclin A2 mediated by E. coli molecular chaperones
Grigoroudis, A. I.; McInnes, C.; Premnath, P. N.; Kontopidis, G. (2015)Bacterial expression of human proteins continues to present a critical challenge in protein crystallography and drug design. While human cyclin A constructs have been extensively characterized in complex with cyclin dependent ... -
Iterative Conversion of Cyclin Binding Groove Peptides into Drug like CDK Inhibitors with Antitumor Activity
Premnath, P. N.; Craig, S. N.; Liu, S.; Anderson, E. L.; Grigoroudis, A. I.; Kontopidis, G.; Perkins, T. L.; Wyatt, M. D.; Pittman, D. L.; McInnes, C. (2015)The cyclin groove is an important recognition site for substrates of the cell cycle cyclin dependent kinases and provides an opportunity for highly selective inhibition of kinase activity through a non-ATP competitive ... -
Leukocyte counts in bronchoalveolar lavage fluid obtained from normal and Maedi-Visna-infected sheep
Katsoulos, P. D.; Christodoulopoulos, G.; Kontopidis, G.; Minas, A.; Tzivara, A.; Kritas, S. K. (2009)Background Bronchoalveolar lavage has proven helpful for the diagnosis of certain ovine diseases of the lungs. There is insufficient data concerning the leukocyte profile of bronchoalveolar lavage fluid (BALF) from MaediVisna ... -
Optimization of Non-ATP Competitive CDK/Cyclin Groove Inhibitors through REPLACE-Mediated Fragment Assembly
Liu, S.; Premnath, P. N.; Bolger, J. K.; Perkins, T. L.; Kirkland, L. O.; Kontopidis, G.; McInnes, C. (2013)A major challenge in drug discovery is to develop and improve methods for targeting protein-protein interactions. Further exemplification of the REPLACE (REplacement with Partial Ligand Alternatives through Computational ... -
Ovine β-lactoglobulin at atomic resolution
Kontopidis, G.; Nordle Gilliver, A.; Sawyer, L. (2014)The crystal structure of the triclinic form of the milk protein β-lactoglobulin from sheep (Ovis aries) at 1.1Å resolution is described together with a comparison of the triclinic structures of the low-pH bovine and high-pH ... -
Performance and antioxidant status of broiler chickens supplemented with dried mushrooms (Agaricus bisporus) in their diet
Giannenas, I.; Pappas, I. S.; Mavridis, S.; Kontopidis, G.; Skoufos, J.; Kyriazakis, I. (2010)In this study, we evaluated the growth performance and antioxidant status of broiler chicken supplemented with the edible mushroom Agaricus bisporus. Ninety 1-d-old female broiler chickens randomly allotted to 3 dietary ... -
Quantification of the Effects of Ionic Strength, Viscosity, and Hydrophobicity on Protein-Ligand Binding Affinity
Papaneophytou, C. P.; Grigoroudis, A. I.; McInnes, C.; Kontopidis, G. (2014)In order to quantify the interactions between molecules of biological interest, the determination of the dissociation constant (K-d) is essential. Estimation of the binding affinity in this way is routinely performed in ... -
Rationally Designed Less Toxic SPD-304 Analogs and Preliminary Evaluation of Their TNF Inhibitory Effects
Alexiou, P.; Papakyriakou, A.; Ntougkos, E.; Papaneophytou, C. P.; Liepouri, F.; Mettou, A.; Katsoulis, I.; Maranti, A.; Tsiliouka, K.; Strongilos, A.; Chaitidou, S.; Douni, E.; Kontopidis, G.; Kollias, G.; Couladouros, E.; Eliopoulos, E. (2014)SPD-304 was discovered as a promising tumor necrosis factor alpha (TNF) antagonist that promotes dissociation of TNF trimers and therefore blocks the interaction of TNF and its receptor. However, SPD-304 contains a potentially ... -
REPLACE: A strategy for iterative design of cyclin-binding groove inhibitors
Andrews, M. J. I.; Kontopidis, G.; McInnes, C.; Plater, A.; Innes, L.; Cowan, A.; Jewsbury, P.; Fischer, P. M. (2006)We describe a drug-design strategy termed REPLACE (REplacement with Partial Ligand Alternatives through Computational Enrichment) in which nonpeptidic surrogates for specific determinants of known peptide ligands are ... -
A statistical approach for optimization of RANKL overexpression in Escherichia coli: Purification and characterization of the protein
Papaneophytou, C. P.; Rinotas, V.; Douni, E.; Kontopidis, G. (2013)Receptor activator of nuclear factor-kappa B (RANK) and its cognate ligand (RANICL) is a member of the TNF superfamily of cytokines which is essential in osteobiology and its overexpression has been implicated in the ... -
Statistical approaches to maximize recombinant protein expression in Escherichia coli: A general review
Papaneophytou, C. P.; Kontopidis, G. (2014)The supply of many valuable proteins that have potential clinical or industrial use is often limited by their low natural availability. With the modern advances in genomics, proteomics and bioinformatics, the number of ... -
Synthesis and biological evaluation of potential small molecule inhibitors of tumor necrosis factor
Papaneophytou, C.; Alexiou, P.; Papakyriakou, A.; Ntougkos, E.; Tsiliouka, K.; Maranti, A.; Liepouri, F.; Strongilos, A.; Mettou, A.; Couladouros, E.; Eliopoulos, E.; Douni, E.; Kollias, G.; Kontopidis, G. (2015)Inhibition of tumor necrosis factor (TNF) production or function by small molecules has become a major focus in the pharmaceutical industry for the treatment of rheumatoid arthritis. In this study, a series of 39 novel ...