• After initial optimization of the distances we obtained the

  2022-04-01

  

  After initial optimization of the distances we obtained the structure iG shown schematically in Fig. 1. This is the telomeric fragment of chromosome with the noncanonical structures of i-motif and G-quadruplex placed symmetrically in the middle of the duplex. Obviously, we consider the situation whe

• RN 1734 Since our new compound Fex could be a new FXR

  2022-04-01

  

  Since our new compound Fex-3 could be a new FXR ligand, we try to demonstrate that Fex-3 was an intestinal-restricted FXR agonist which only activated FXR in the intestine not in the liver or other organs. Initially, we investigated this in Caco-2 RN 1734 with transwell experiments. From and , we

• FXR agonists represent an attractive class of drugs

  2022-04-01

  

  FXR agonists represent an attractive class of drugs for patients with PFIC. Synthetic and semi-synthetic FXR agonists, with higher affinity and potency to activate FXR, have been successfully tested in animal models of cholestasis. In these murine models, the semi-synthetic steroidal FXR ligand obet

• With the identification of small nonpolar

  2022-04-01

  

  With the identification of small nonpolar substituents at R3 of the phenylpropanoic acid ring providing improved activity at FFA4, exploration of the benzyl SAR was undertaken (). Small substituents were well tolerated at both the and positions (–) with the 2-bromo- (), 2-isopropoxy- (), and 3-methy

• ionomycin The knowledge that piroxicam competes with ligands

  2022-04-01

  

  The knowledge that piroxicam competes with ligands that bind to FPR may be of importance for a deeper understanding of the anti-inflammatory effects possessed by this NSAIDs. It has recently been reported that not only phagocytes but also platelets express FPR on their cell surface and that these re

• Compounds were tested for GPR activity in

  2022-04-01

  

  Compounds , were tested for GPR40 activity in a functional assay monitoring calcium flux in CHO 5-lipoxygenase transiently transfected with human GPR40 gene. As shown in , compound was found to be a nanomolar GPR40 agonist, while compound was much less potent than . To explore the structure activ

• The possibility of having false positives even

  2022-04-01

  

  The possibility of having false positives, even if minimized, is always present and requires that a reactive result should be followed by a confirmation test. Traditionally, Western blot (WB) has been used, but various types of immunoblotting that use recombinant CA-074 Me or synthetic peptides are

• There are several limitations in our study

  2022-03-31

  

  There are several limitations in our study. First, only the naturally occurring resistance-associated mutations in patients coinfected with HIV/HCV Cy5 Firefly Luciferase mRNA receptor 1b were analyzed. The result was only applicable to HCV genotype 1b, but not the HCV genotype 1a patients. We did n

• Egypt has the highest prevalence of

  2022-03-31

  

  Egypt has the highest prevalence of HCV worldwide with almost 20% of the population being infected. The HCV subtype 4a belonging to genotype 4 (HCV-4) is the most common genotype in Egypt [25], [26], [27], [28]. The sequence of the NS5A/NS5B junction for the Egyptian genotype 4 is Glu-Asp-Val-Val-Cy

• We found that activator drugs decrease NOsGC

  2022-03-31

  

  We found that activator drugs decrease NOsGC protein levels in Sf9 cells. This decrease in protein levels is more pronounced for BAY 60–2770 compared to cinaciguat, and more obvious for α1/β1 compared to α2/β1 (see Fig. 2). This led us to hypothesize that the reduction in protein level correlates wi

• Under most circumstances NO is a potent

  2022-03-31

  

  Under most circumstances, NO is a potent endogenous vasodilator. Therefore, its involvement in an endothelium-dependent contraction seems paradoxical, to say the least. Soluble guanylyl cyclase (sGC) is the major downstream target of NO; its inhibition results in the lack of vasoconstrictor response

• Introduction Epigenetic alterations play an important role

  2022-03-31

  

  Introduction Epigenetic alterations play an important role in carcinogenesis. Aberrant promoter CpG island hypermethylation causes transcriptional gene silencing [1], and has been documented for a number of genes in prostate cancer (PCA) [2]. Histone modifications are also important regulators of t

• LPCs have been previously described as potential anti

  2022-03-31

  

  LPCs have been previously described as potential anti-diabetic factors due to stimulation of secretory activity from the isolated rodent pancreas, L-type cells, ands insulin-producing cell lines, with LPC 18:1 as the main structure of interest (Soga et al., 2005, Sakamoto et al., 2006, Overton et al

• Compound was synthesized in a racemic fashion with this

  2022-03-31

  

  Compound was synthesized in a racemic fashion with this study and plans for an enantioselective synthesis could be developed based on the activity of racemic . Synthesis of compound followed a slightly different synthetic route due to the ineffectuality of the S2 reaction on the secondary position (

• Adenosine triphosphatase ATP is a signaling molecule in acut

  2022-03-31

  

  Adenosine triphosphatase (ATP) is a signaling molecule in acute pain and chronic pain(Burnstock, 2009, Burnstock, 2013, Burnstock, 2014, Chizh and Illes, 2001). It is also known that presynaptic A1 receptors are involved in the inhibition of transmitter release (Vizi and Knoll, 1976). Extracellular

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