• br Fragment based drug discovery FBDD is a powerful method

  2020-10-08

  

  Fragment-based drug discovery (FBDD) is a powerful method to discover drug leads and has been widely adopted in both academia and industry. FBDD can be used to explore chemical dihydrofolate reductase inhibitor antibacterial space with libraries which are smaller in size, producing drug leads with

• Supported by the Austrian Science Fund FWF grant

  2020-10-08

  

  Supported by the Austrian Science Fund FWF (grant P22521-B18 to A.H.) and the Austrian National Bank (grant 14263 to A.H.). K.J. was funded by the PhD Program DK-MOLIN (FWF-W1241). Acknowledgements Introduction Acute lung injury (ALI) and acute respiratory distress syndrome (ARDS), a more sev

• Under optimized assay conditions very low concentrations pM

  2020-10-08

  

  Under optimized assay conditions, very low concentrations (20pM) of [125I]YP20 bound to hCRF1-CHO fdps membranes with high specificity (>95% inhibited by 1μM astressin) and in a membrane protein-dependent manner. Specific binding was selective vs. the hCRF2α subtype because little specific binding

• br Conclusion In this study we have shown the construction

  2020-10-08

  

  Conclusion In this study, we have shown the construction, expression and purification of CPG2 fused to the HIV-1 TAT peptide (TAT–CPG2). We have demonstrated for the first time that TAT-CPG2 in both native and denatured forms could be efficiently transduced into the HepG2 cells. Also, we have pro

• The four other mutations S T V I T

  2020-10-08

  

  The four other mutations (S281T, V317I, T328A and A329S) were not detected in the absence of the A286S. This could suggest that when all of them are present, there would be a tri-dimensional structural modification that would interfere with the binding of the insecticide and produce different levels

• The modes of action of insecticides are

  2020-10-08

  

  The modes of action of insecticides are classified by the Insecticide Resistance Action Committee (IRAC) [6]. In this classification, a large proportion of insecticides are categorized as nerve- and muscle-targeting insecticides, which encompass GABACl antagonists (Group 2) and GluCl allosteric modu

• The N B method has the overall

  2020-10-08

  

  The N&B method has the overall advantage that it is not restricted to certain dyes specific for energy transfer [55], and is also able to detect higher order receptor Tariquidar on the focal point in living cells. Conclusion The N&B method has shown to be a powerful tool to locate and quantify t

• The glycolytic pathway is a catabolic route that ends

  2020-10-06

  

  The glycolytic pathway is a catabolic route that ends with the synthesis of pyruvate (Pyr). In Arabidopsis embryos, the conversion of phosphoenolpyruvate (PEP) to Pyr, catalyzed by pyruvate kinase (PK), is mainly located in the plastids [10], [11]. The preceding reaction is catalyzed by enolase (ENO

• br Effects of culture conditions on drug

  2020-10-06

  

  Effects of culture conditions on drug-induced gene GSK2126458 in primary human hepatocytes Past progress in elucidating the optimal conditions for the long-term cultivation of rodent hepatocytes has helped define some of the key components in the matrix and medium environment that are most critic

• Two parameters were extracted from these experiments

  2020-10-05

  

  Two parameters were extracted from these experiments to compare the interactions of the three compounds with ct-DNA. The association constant K for the binding of the naphthalimide derivatives to ct-DNA was calculated by fitting the evolution of the fluorescence spectra with a 1:1 binding model usin

• Our comparison of all ER iso forms with ER

  2020-10-01

  

  Our comparison of all ERα (iso)forms with ERβ immunostaining suggests that overall ERβ expression is lower than that of ERα isoforms. This contrasts the so far reported data for ERs in the lung, but is not a paradox; in pathology routine, ER positivity is defined stricto senso by nuclear WT ERs. As

• Imatinib STI is a first line

  2020-09-30

  

  Imatinib (STI-571) is a first-line tyrosine kinase inhibitor (TKI) targeted at breakpoint cluster region-Abelson kinase (ABL) for the treatment of chronic myeloid leukemia (CML) [26]. As a type II inhibitor, imatinib achieves significant selectivity by binding to an inactive DFG-out conformation (DF

• The expression of EBI has been found to be dysregulated

  2020-09-30

  

  The expression of EBI2 has been found to be dysregulated in several types of B cell malignancies and is thus reduced in e.g. diffuse large B-cell lymphomas [12] and chronic lymphocytic leukemia [13] and increased in post-transplantation lymphoproliferative disorders (PTLDs) [14]. EBI2 is also highly

• br Acknowledgements The research leading to these results ha

  2020-09-30

  

  Acknowledgements The research leading to these results has received funding from the European Union Seventh Framework Programme (FP7-PEOPLE-2013-COFUND) under grant agreement no 609020 − Scientia Fellows (JB) and the Research Council of Norway (NFR-grant 221444) (JB, JPM, OB). Introduction Hu

• br Results br Discussion Taking advantage of the highly

  2020-09-30

  

  Results Discussion Taking advantage of the highly specific protein–protein interactions among cognate VKGILS-NH2 that mediate SUMO conjugation to substrates, we have developed a novel strategy for achieving inhibition of SUMO conjugation in vivo based on disruption of SUMO E1–E2 interactions.

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