• The combination of niacin with a selective PGD

  2022-01-19

  

  The combination of niacin with a selective PGD2 receptor antagonist laropiprant, designed to circumvent the flushing side effect of niacin, has been evaluated in the HPS2-THRIVE study and showed no clinically meaningful benefit when administered in patients on top of statin therapy [41]. Our data s

• This data is in accordance with

  2022-01-19

  

  This data is in accordance with our recent results on the influence of cholesterol-depleting agent methyl-β-cyclodextrin on platelets (Borisova et al., 2011a). Dissipation of the proton electrochemical gradient of secretory granules by methyl-β-cyclodextrin did not evoke the release of endogenous gl

• Fig A demonstrates the body weight gain of

  2022-01-19

  

  Fig. 2A demonstrates the body weight gain of the pregestational females. High-fat diet in wild-type mice increased body weight in 2 weeks and sustained this increase over 8 weeks. A similar effect was noted in glut3 mice in response to a high-fat diet. Fig. 2B depicts fat and muscle mass as assessed

• The first GSM was identified

  2022-01-19

  

  The first GSM was identified from the discovery of non-steroidal anti-inflammatory drugs (NSAIDs). An amyloid reducing GSM that also suppresses inflammation is desirable. Inflammatory response is an invariable characteristic of AD pathogenesis, in part triggered by Aβ. During AD onset and progressio

• BCTC One may ask whether induced loss through chemical or ge

  2022-01-19

  

  One may ask whether induced loss, through chemical or genetic perturbation for example, of an essential cellular factor represents regulated cell death or simple loss of the homeostasis needed for life. For example, deletion of the Mdm2 gene, or inhibition of the MDM2 protein, results in cell death

• Lastly haspin inhibitor was assessed against a panel of

  2022-01-18

  

  Lastly, haspin inhibitor was assessed against a panel of 292 kinases at 10μM. At this high concentration, the N1-Methylguanosine-5'-Triphosphate receptor inhibited thirteen kinases, in addition to haspin, ⩾90%., These kinases were CaMK2b, CaMK2d, CDK7-CycH-Mat1, cGK2, CK1d, CLK1, CLK2, DYRK1A, DY

• We observed that the Toc G domain

  2022-01-18

  

  We observed that the Toc159G domain recognizes the N-terminal portion of the transit peptide of pSSU with a dissociation constant of 70 μM (Fig. 2; Table 1), while a tenfold higher KD was obtained for the phosphorylated C-terminal region. In turn, the homodimer of Toc34G recognizes the phosphorylate

• br Concluding remarks Several orphan

  2022-01-18

  

  Concluding remarks Several orphan GPCRs have expression profiles that indicate they are worthy of consideration as therapeutic targets. This view can be supported via various transgenic techniques, and it would be interesting to have wide-ranging phenotypic information on GPR35 knockout mice. Bas

• Lamina II SG spinal cord neurons play an

  2022-01-18

  

  Lamina II (SG) spinal cord neurons play an important role in regulating nociceptive input from the periphery [20,21]. Moreover, lamina II neurons are concentrated with glycinergic or GABAergic inhibitory interneurons. Therefore, it is possible that β-alanine might modulate nociceptive transmission i

• Through the analysis of various synthetic

  2022-01-18

  

  Through the analysis of various synthetic GPR40 agonists as reported in literature, we found that a number of these compounds contained a phenylpropanoic ppar pathway motif which was inspired from naturally occurring medium to long chain fatty acids. For instance, in the early period of discovering

• Here we investigated on epigenetic regulatory mechanisms of

  2022-01-18

  

  Here, we investigated on epigenetic regulatory mechanisms of ALX/FPR2 expression. Epigenetic changes, that include phosphorylation, acetylation, methylation and ubiquitination of DNA and histone proteins, occur in a variety of diseases [21] and are being recognized as key targets for personalized me

• Natural product based drug discovery can be

  2022-01-18

  

  Natural-product-based drug discovery can be enhanced with computational methods [205]. Because most of the reported small-molecule natural inhibitors of fMLF-induced functional responses were not evaluated in ZM 447439 binding assays, we used molecular modeling to predict how well these compounds f

• Till date the first line treatment of

  2022-01-18

  

  Till date, the first line treatment of T2DM is oral metformin followed by oral sulfonylureas, dipeptidyl peptidase-IV-inhibitors, and TZDs. As the disease progresses, injectable glucagon-like peptide-I analogues or ultimately insulin become necessary to maintain glycaemic control. Despite the establ

• Irsogladine br Acknowledgments We thank Drs Yasuhiro Saito

  2022-01-17

  

  Acknowledgments We thank Drs. Yasuhiro Saito and Mitsuru Futakuchi for helpful discussion. We also thank Drs. Kohei Miyazono and Tadashi Matsuda for cells. This work was supported by Grant-in-Aids for Scientific Research on Innovative Area (16H06373; 16K15273) from MEXT, Japan (to M.H.) and by Pr

• The glycolytic activator phosphofructo kinase fructose bisph

  2022-01-17

  

  The glycolytic activator 6-phosphofructo-2-kinase/fructose 2,6-bisphosphatase 3 (PFKFB3) is well-known as a downstream substrate of hypoxia-inducible factor 1α (HIF-1α) signaling pathway [5,6]. Tumor hypoxia has long been associated with increased malignancy, poor prognosis and drug resistance. HIF-

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