• Over the last few years experimental evidence

  2022-02-25

  

  Over the last few years, experimental evidence for the involvement of Epac1 in cancer progression is beginning to emerge (Almahariq et al., 2015, Banerjee and Cheng, 2015, Parnell et al., 2015, Parnell et al., 2015, Schmidt et al., 2013). For example in melanoma cells, silencing of Epac1 attenuates

• br Materials and methods br Results br Discussion In

  2022-02-25

  

  Materials and methods Results Discussion In this study, we demonstrated that zaprinast (a cGMP-PDE inhibitor) induced the intracellular calcium mobilization in the sulconazole receptor coexpressing GPR35 and Gqi5, Gqo5, or Gα16. Induction of intracellular calcium mobilization by zaprinast

• Because of its excellent GPR potency good hERG selectivity a

  2022-02-25

  

  Because of its excellent GPR119 potency, good hERG selectivity and favorable rat t, Seratrodast australia was scaled-up and further profiled. The synthetic protocols described in , were both suitable for a multi-gram scale synthesis of compound . An off-target screen was performed against an exte

• To characterize the binding receptor for HIV gp in autophagy

  2022-02-25

  

  To characterize the binding receptor for HIV-1 gp120 in autophagy, we used the CXCR4 inhibitor AMD3100 and NMDA receptor inhibitor MK801 along with gp120 to treat the cardiomyocytes. Our data demonstrated that inhibition of the NMDA receptor significantly blocked the increase of gp120 induced autoph

• 873 This study does have important limitations to consider T

  2022-02-25

  

  This study does have important limitations to consider. The utilization of a recombinant gp120 monomer (at a single concentration of 100 ng/ml) instead of live virus particles may limit the validity of our results. Moreover, extrapolation of an in vitro cell culture model to animals or humans cannot

• An alternative approach to improving

  2022-02-25

  

  An alternative approach to improving pharmacokinetic profile while retaining high GlyT1 potency was also pursued. Libraries were prepared in which potency enhancing piperidine C4 substituents were combined with clearance lowering truncated alkyl sulfonamides. The result was the discovery of (). Unl

• The inhibition of NSAIDs towards GLOI

  2022-02-25

  

  The inhibition of NSAIDs towards GLOI provides a direction for the development of novel effective GLOI inhibitors. Although the inhibitory activity of indomethacin was determined and the interactions between it urat1 inhibitor and GLOI were probed by NMR titration experiments, no detailed inhibitor

• The standard model of stress postulates the activation of bo

  2022-02-25

  

  The standard model of stress postulates the activation of both the sympathoadrenomedullary axis and the hypothalamo-pituitary-adrenocortical axis. Long-term activation of either neuroendocrine axes has been shown to be harmful [12]. Short-term activation of the sympathoadrenomedullary axis is used t

• Pirarubicin br Introduction Depression is a prevalent and

  2022-02-25

  

  Introduction Depression is a prevalent and disabling psychiatric illness that affects millions of individuals worldwide, resulting in enormous personal suffering and public health costs [1]. Traditional antidepressants such as monoamine oxidase inhibitors (MAOIs) and selective serotonin reuptake

• Interestingly when glucose is deleted in

  2022-02-25

  

  Interestingly, when glucose is deleted in PCa cells, GLUT1 is increased. Also, AR is almost entirely located in the nucleus, correlating with the increment in GLUT1 levels. These results are in agreement with those reported by Vaz et al. [16], They described an increase in GLUT1 after DHT stimulatio

• br Dysregulation of glutamate transporter expression and

  2022-02-25

  

  Dysregulation of glutamate transporter expression and function Aberrant glutamate transporter function and expression are associated with various neurological disorders. Therefore, understanding the underlying mechanisms of EAAT1/2 expression may provide therapeutic targets for treating neurologi

• Such responses have led to the idea that elasmobranchs may

  2022-02-25

  

  Such responses have led to the idea that elasmobranchs may be glucose intolerant. However, certain species, such as the North Pacific spiny dogfish (Squalus suckleyi; note that the species used in this study was previously referred to as Squalus acanthias but a study by Ebert et al. (2010) provided

• In conclusion we provided the

  2022-02-25

  

  In conclusion, we provided the first evidence of a modification and regulation of GCK by O-GlcNAc modification that until now was not explored. This discovery provides important clues in the prevention of hyperglycemia and development of novel therapeutic drugs to treat type 2 diabetes. Acknowled

• Herein in consider of the high similarity between GR HBP

  2022-02-25

  

  Herein, in consider of the high similarity between GR HBP site and AR HBP site, we applied rational drug design strategy to develop AR/GR antagonists based on the chemical structures of antiandrogens and crystal structure of GR. The following bioassay identified Z19 as a dual AR/GR antagonist. Z19 i

• The identification of distinct expression domains in

  2022-02-25

  

  The identification of distinct expression domains in the limb suggested that these domains might have specific biological functions. We explored this possibility by determining enriched biological processes for each category using GO ontology term analysis (WebGestalt) (Zhang et al., 2005). Category

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