• br Conclusion In conclusion we showed that

  2022-04-02

  

  Conclusion In conclusion, we showed that apoptosis is involved in etoposide-induced pancreatic β-cell cytotoxicity. More importantly, as shown in Fig. 6, the results of this study demonstrated that etoposide induces pancreatic β-cell death via the JNK/ERK activation-mediated GSK-3 downstream-trig

• While the specific set of challenges associated

  2022-04-02

  

  While the specific set of challenges associated with deorphanization and transforming each poorly characterized GPCR into a useful drug target will be unique, much can be learned by considering how these issues have been addressed for other receptors. One group of poorly characterized GPCRs that hav

• Approximately mammalian genes encoding family A or

  2022-04-02

  

  Approximately 250 mammalian genes encoding family A (or rhodopsin-like) GPCRs have been cloned (Lee et al., 2001a). As yet, the total number of cloned GPCRs reported in the literature including the secretin and metabotropic glutamate-like families of GPCRs falls short of the projected 616 GPCR-encod

• Conjugated BAs via S PR also activate ERK and AKT

  2022-04-02

  

  Conjugated BAs via S1PR2 also activate ERK1/2- and AKT-signaling pathways leading to the growth and invasion of cholangiocarcinoma cells. The role of conjugated BAs via S1PR2 to regulate apoptosis or cancer progression remains to be dissected. Nevertheless, there is no doubt that the composition of

• br AUTHOR CONTRIBUTIONS br ACKNOWLEDGMENTS br Introduction C

  2022-04-02

  

  AUTHOR CONTRIBUTIONS ACKNOWLEDGMENTS Introduction Chronic neuropathic pain is a common symptom in patients with human immunodeficiency virus (HIV)-1 infection. Glycoprotein 120 (gp120) is an HIV-1 protein that can cause pain behaviors in animal models (Hao, 2013, Nasirinezhad et al., 2015,

• m1 receptor Lamina II SG spinal cord neurons play an importa

  2022-04-01

  

  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

• br Methods br Results and discussion

  2022-04-01

  

  Methods Results and discussion Conclusions A third example of a hexokinase using polyphosphate exclusively as a phosphoryl donor has been identified, this time in mammalian tissues. This is the first polyphosphate utilizing enzyme activity demonstrated in mammalian MK 886 synthesis as far a

• To directly address whether pharmacological

  2022-04-01

  

  To directly address whether pharmacological attenuation of physiological GIP provides therapeutic benefits in obese mice, we pursued a selective long-acting antagonist to complement the work we report on GIPR agonism. We report a GIP analog of sufficient aqueous solubility that employs a shortened N

• In summary the SAR of

  2022-04-01

  

  In summary, the SAR of a series of phenylpropanoic acid-free fatty vomitoxin receptor agonists is described which resulted in the identification of potent FFA4 agonists. The superior pharmacokinetic properties of compound led to its selection as an in vivo tool compound which afforded robust effic

• br Results and discussion CATALYST software allows automatic

  2022-04-01

  

  Results and discussion CATALYST software allows automatic pharmacophore construction by using a collection of molecules with activities ranging over a number of orders of magnitude. In addition, CATALYST pharmacophores (hypotheses) explain the variability of bioactivity with respect to the geomet

• br Acknowledgements Funding for this study is gratefully ack

  2022-04-01

  

  Acknowledgements Funding for this study is gratefully acknowledged from the Department of Employment and Learning (QC) and the Northern Ireland Chest Heart and Stroke Association (2008107). Introduction Preeclampsia is a major human pregnancy-specific disorder that occurs in at least 5–10% of

• Cy3 NHS ester (non-sulfonated) LMWHs are currently recommend

  2022-04-01

  

  LMWHs are currently recommended for the treatment of VTE in patients with cancer. Compared to vitamin K antagonists, LMWHs are more effective in reducing the risk of recurrent VTE without increasing the risk of bleeding [13]. However, a post hoc analysis of this Cy3 NHS ester (non-sulfonated) previ

• To enhance the impact of GD

  2022-04-01

  

  To enhance the impact of GD2 as an immune target in this cancer, we investigated a novel strategy to upregulate expression on the cell surface of EwS cells by an epigenetic agent, based on the following rationale. Biosynthesis of GD2 and other gangliosides during organ development is driven by stage

• This connection is supported by studies in the SIV macaque

  2022-04-01

  

  This connection is supported by studies in the SIV macaque model of HIV, where treatment with methamphetamine, which greatly enhances CNS dopamine levels (Truong, 2005); increased SB 216763 viral load. Methamphetamine also increased expression of the HIV co-receptor CCR5 in CNS macrophages, thereby

• Introduction Histamine Imidazolyl ethylamine is an important

  2022-03-31

  

  Introduction Histamine [2-(4-Imidazolyl)-ethylamine] is an important mediator of many physiological and pathological processes including inflammation, gastric Arecaidine but-2-ynyl ester tosylate secretion, neuromodulation, regulation of immune function, cell proliferation and differentiation, amo

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