• br Patients and Methods Patients who had been initiated

  2021-05-13

  

  Patients and Methods Patients who had been initiated on a DPP-4 inhibitor (see in the online version at doi:10.1016/j.clinthera.2018.06.002) between April 2012 and June 2017, when the common threshold for dose adjustment for all non-linagliptin DPP-4 inhibitors was a creatinine clearance (CrCl) l

• Of the acidic hydroxyazoles involved hydroxypyrazole had the

  2021-05-13

  

  Of the acidic hydroxyazoles involved, hydroxypyrazole had the weakest acidic profile (pKa in the range of 6–7), although highly deprotonated at physiological pH. During hit optimization, the two pyrazole ring positions available for substitution provide an opportunity for a better exploration of the

• Significantly less is known about regulation

  2021-05-13

  

  Significantly less is known about regulation of phytocystatin gene expression. A genomic clone corresponding to the barley cystatin Icy gene has been characterized (Gaddour et al., 2001) and the function of its promoter region has been analysed by Martínez et al. (2005b). Bioinformatic analysis of t

• Quercetin competitively inhibited BFC activity

  2021-05-13

  

  Quercetin competitively inhibited BFC activity in human recombinant cDNA-expressed CYP3A4 with Ki=15.4±1.52μM, and myricetin noncompetitively with Ki=74.6±7.99μM (Fig. 4). The degree of inhibition by quercetin was not affected by a pre-incubation step and was similar in the microsomes from both gend

• Acidic substituents showed moderate biochemical activity

  2021-05-13

  

  Acidic substituents () showed moderate biochemical activity, but these compounds showed reduced cellular potency. Additional compounds bearing a carboxylic Ki16198 were also prepared and tested (data not shown). All of acidic compounds showed low cellular potency regardless of their biochemical acti

• From the general synthetic route

  2021-05-13

  

  From the general synthetic route, we first synthesized a directed set of analogues of general formula , keeping the synthesis simple by using a symmetrical pyrazole (R=R=Me). The SAR of a set of 30 compounds in the GTPγS binding assay turned out to be quite tight: only 4 (13%) compounds showed moder

• We further examined our hypothesis that

  2021-05-13

  

  We further examined our hypothesis that the activation of CRF and CCK systems is responsible for the enhanced anxiety-like behavior induced by immobilization stress using two antagonists to block the expression of CRF1 and CCK2 receptors. It was found that CCK2 receptor antagonist CR2945 or CRF1 ant

• Carnitine acetyltransferase CrAT transesterifies short chain

  2021-05-13

  

  Carnitine acetyltransferase (CrAT) transesterifies short-chain acyl-CoAs, and is located both in mitochondria and peroxisomes. In yeasts and mammals this protein is the product of a single gene [20,21] and the sorting to different organelles is evolutionary conserved, although the mechanism of diffe

• br Experimental methods br Results and discussion

  2021-05-13

  

  Experimental methods Results and discussion Conclusions Here we describe the first reported method for high-yield HC 067047 synthesis of active and soluble mature CPG2 (in the absence of the leader peptide) and its individual catalytic and dimerization domains in E. coli. Such a method is o

• In the Cu bioassay notwithstanding the absence of significan

  2021-05-13

  

  In the Cu bioassay, notwithstanding the absence of significant Cu bioaccumulation in bulk tissues over the 96-h exposure period (less than 2-fold difference in tissue Cu between controls and the second-highest treatment), T-ChE activity increased with Cu concentration in gill and, to a lesser extent

• ACSF The use of the periplasmic fraction as starting materia

  2021-05-13

  

  The use of the periplasmic fraction as starting material and the presence of a unique purification step concurred in improving the purification yield to 25.3%, which is significantly higher than what obtained with the previous purification protocol (6.7%). In addition, the analysis of the kinetic co

• On the other hand the interaction of the

  2021-05-12

  

  On the other hand, the interaction of the Kaempferia parviflora extract with CYP3A was uncompetitive with a low Vmax value. In the in vivo study, the Kaempferia parviflora extract did not interfere with CYP3A activity throughout the entire duration of treatment. This is fortunate as CYP3A isoforms a

• br EBV Infection Epstein Barr virus EBV

  2021-05-12

  

  EBV Infection Epstein–Barr virus (EBV, human herpesvirus 4) was discovered 50 years ago, when Epstein, Achong, and Barr used electron microscopy to identify viral particles in Burkitt's lymphoma cells. It belongs to the lymphocryptovirus (LCV) genus of the gammaherpesvirus subfamily (Fig. 1A). Th

• Due to the high attractiveness of E and E

  2021-05-12

  

  Due to the high attractiveness of E2 and E3 ligases as drug targets, a number of drug discovery assays have been published, based on detection by fluorescence (Dudgeon et al., 2010, Krist et al., 2016, Zhang et al., 2004), Bromfenac Sodium (Davydov et al., 2004, Huang et al., 2005, Kenten et al., 2

• In the present study we used linagliptin one

  2021-05-12

  

  In the present study, we used linagliptin, one of the commercially available DPP-4 inhibitors, because it has more long-lasting inhibition of DPP-4 activity than other drugs of this class. We hypothesized that linagliptin may interact with intercellular components, not only with DPP-4 on the plasma

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