• We first investigated the influence

  2021-09-29

  

  We first investigated the influence of the -acyl group of the glycine amide side chain and found that shorter linkers lead to better activities (–); simple -benzoyl substituents were always superior to the 3-arylpropanoyl group present in the high-throughput hit (). Electron withdrawing substituents

• The aim of this study is to explore new Glo

  2021-09-29

  

  The aim of this study is to explore new Glo-I inhibitors using the structure-based pharmacophore approach. Eighteen Glo-I co-crystallized structures have been explored to investigate their pharmacophoric features. Ninety two pharmacophoric models were generated. QSAR analysis followed by Ligand Prof

• br Membrane transporters as a novel therapeutic target

  2021-09-29

  

  Membrane transporters as a novel therapeutic target in pediatric TBI The concept of targeting membrane transporters began with identifying a neuroprotective drug and a corresponding transporter inhibitor. Somewhat serendipitously, we discovered that N-acetylcysteine (NAC), a cysteine donor for GS

• Channeling of SFA away from generation of toxic lipid metabo

  2021-09-28

  

  Channeling of SFA away from generation of toxic lipid metabolites such as ceramide, towards inert TG accumulation in response to cosupplementation with increased levels of MUFAs has previously been shown in many cell types including the pancreatic β-cells [37]. Our studies indicate that similar mech

• The results show that pimarane and

  2021-09-28

  

  The results show that -pimarane and -strobane diterpenoids exert inhibitory effects on FXa suggesting that they may have potential as FXa inhibitor. However, it should be noted that some compounds such as compounds , , , and are poorly bioavailable. Thus, the current study indicates that the number

• br Role of funding source

  2021-09-28

  

  Role of funding source Conflict of interest Acknowledgements We thank F. Blaskovits and P. Kesner for technical assistance. This project was supported by operating grants from the Canadian Institutes of Health Research (CIHR) to X. Zhang (MOP123249) and the National Natural Science Foundati

• br Materials and methods br Results and discussion To analyz

  2021-09-28

  

  Materials and methods Results and discussion To analyze the dependence of lysosomal exocytosis on Cu we exposed HeLa Heparin to fresh buffer containing normal levels of free Ca (1mM) and measured β-hex levels in the extracellular medium, followed by measuring β-hex content in the total cellul

• br Heme oxygenase inhibitors Historically

  2021-09-28

  

  Heme oxygenase-1 inhibitors Historically, the first class of competitive HO-1 inhibitors was represented by MPs, heme analogs in which the central iron Firefly Luciferase australia of heme is exchanged by another element, such as zinc, cobalt, tin, or chromium. These molecules compete with heme

• br Discussion The present study explored that the effect

  2021-09-28

  

  Discussion The present study explored that the effect of the MTP gene −493G/T polymorphism on the risk of hepatic steatosis in Turkish patients with chronic HCV genotype 1 infection. Some researchers revealed that the MTP gene −493G/T polymorphism was associated with hepatic steatosis in CHC infe

• While phosphorylation site motifs are

  2021-09-28

  

  While nampt inhibitor site motifs are typically described in terms of residues that promote phosphorylation, negatively selected residues can also be an important component of substrate recognition. Such ‘forbidden’ resides can act as a filter to prevent phosphorylation of a site by the ‘wrong’ kin

• Of special interest is that riociguat and NO donors

  2021-09-28

  

  Of special interest is that riociguat and NO donors decreased the phosphorylation of many proteins in human platelets. This aspect is presently under further investigation but a few comments can be made already here. Of the extensive spectrum and diversity of human protein kinases and protein phosph

• br Conclusion In this report we describe the synthesis

  2021-09-28

  

  Conclusion In this report, we describe the synthesis and evaluation of oxadiazole-based GSK3 inhibitors. Occupation of the ATP-binding pocket in its entirety led to the identification of several potent and selective compounds. These compounds are characterized by IC50 values in the low nanomolar

• En el caso de la foliculitis

  2021-09-28

  

  En el caso de la foliculitis decalvante (FD), se ha publicado un estudio multicéntrico español de 82 pacientes en el que se concluye que el tratamiento que consigue una mayor efectividad (mejora en 15/15 pacientes tratados) y un mayor periodo de remisión postratamiento (7,2 meses) es la combinación

• Biochemical assays have provided evidence that prolonged

  2021-09-28

  

  Biochemical assays have provided evidence that prolonged exposure to GPR35 agonists can induce GPR35 internalization [2], [4], [11], [13]. Our finding that neuronal excitability decreased regardless of whether the slices were superfused for a few minutes or incubated for a few hours with GPR35 agoni

• Compounds and were tested for pharmacodynamic effects in

  2021-09-28

  

  Compounds , and were tested for pharmacodynamic effects in a mouse oral glucose tolerance test (oGTT) in wild-type and GPR120 deficient mice, and each compound demonstrated GPR120 mechanism-based effects. Data for compound is shown in , indicating mechanism-based reduction in glucose excursion at b

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