• NSC23766 Acknowledgments We would like to thank Dr Greg Morr

  2021-11-08

  

  Acknowledgments We would like to thank Dr. Greg Morriello, Mr. Lehua Chang, Mr. Chris Moyes and Mr. Nam Fung Kar for intermediate 3 syntheses. Cheng Zhu would like to thank Dr. Milana Maletic, Mr. Kake Zhao and Mrs. Wanying Sun for helpful discussions. Introduction Glucagon-like peptide-1 (GLP-

• br Introduction Over the past two decades the prevalence

  2021-11-08

  

  Introduction Over the past two decades, the prevalence of obesity and obesity-associated metabolic diseases, such as T2D, insulin resistance, atherosclerosis and stroke, have been dramatically increased globally [1], [2], and obesity has been suggested to be the leading cause of the reduced life

• br Material and methods br

  2021-11-08

  

  Material and methods Results Discussion The inhibitory action of a GABA agonist, muscimol, on the level of mRNA encoding GnRH in the POA-hypothalamus [25] of follicular-phase sheep has suggested that at the hypothalamic level GABA may exert a suppressive effect on subsequent steps of the Gn

• br Introduction Major depressive disorder

  2021-11-08

  

  Introduction Major depressive disorder (MDD) is a disease with poorly recognized etiology. Currently used antidepressant drugs, which mainly affect synaptic neurotransmitter levels, show full clinical efficacy in only one third of patients (Rush, 2007). Thus it is now generally accepted that the

• Recent studies suggest that the

  2021-11-08

  

  Recent studies suggest that the biological importance of endogenous ghrelin becomes accentuated during exposure to more metabolically-constrained and stressful environments. Indeed, mice lacking either ghrelin or GHSR demonstrate impaired ability to adapt metabolically and/or behaviorally to caloric

• br Therapeutic approaches exploiting Cx

  2021-11-08

  

  Therapeutic approaches exploiting Cx43 function Due to their potential role in cancer metastasis, attempts have been made to alter connexin function to inhibit cancer growth. Therapeutic approaches include Cx43 peptide mimetics, Cx43 inhibitors, chemical agents capable of enhancing Cx43 function,

• Through the analysis of various synthetic GPR agonists as re

  2021-11-08

  

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

• Dysregulation of the HPA axis

  2021-11-08

  

  Dysregulation of the HPA axis, resulting in alteration to both baseline and stress-induced glucocorticoid levels (e.g., cortisol and corticosterone), has been implicated in several diseases and psychopathologies, including anxiety (McEwen et al., 2015, 2016; Shin and Liberzon, 2010). For example, ba

• The main consequence of glucose catabolism is

  2021-11-08

  

  The main consequence of glucose catabolism is the elevation of ATP concentration, which in turn suppresses the ATP sensitive potassium (KATP) channels gating function. The KATP channels are octamers composed of the tetrameric inward-rectifying potassium channels (with Kir6.1 and Kir6.2 subunits), th

• In cancer cells HIF upregulates

  2021-11-08

  

  In cancer cells, HIF-1α upregulates HK-II expression by binding to the hypoxia-responsive element in the HK-II promoter region to adapt to hypoxic conditions [20]. In the present study, we observed that mangiferin transiently increased HIF-1α expression in endothelial cells, suggesting another possi

• br Conclusions Beta cell specific expression in human

  2021-11-06

  

  Conclusions Beta cell-specific expression in human islets of DGCR2, GBF1, GPR44 and SerpinB10 has not previously been described, although the proteins have partly been characterized in other contexts not related to beta Mometasone furoate or diabetes. DGCR2, GPR44 and SerpinB10 were negative in

• br The mode of binding of ligands

  2021-11-06

  

  The mode of binding of ligands to GPR35 As noted above, although kynurenic ornidazole is an agonist at GPR35, this is true for neither kynurenine [8] nor kynurenic acid ethyl ester [13]. This implicates a key role for the carboxylate group in binding and/or activation of GPR35. Importantly, in s

• The use of HIV peptide epitope based vaccines is safer

  2021-11-06

  

  The use of HIV-1 peptide epitope-based vaccines is safer and cheaper than live or inactivated vaccines [8]. However, peptide epitope vaccines could show poor immunogenicity and have poor uptake by APCs [9]. Nevertheless, nanocarrier-based delivery platforms have been demonstrated to enhance the pept

• Sumoylation is involved in regulating protein protein intera

  2021-11-06

  

  Sumoylation is involved in regulating protein-protein interactions, subcellular protein localization, protein stability, and transcriptional factor activity (reviewed in [29]). The small ubiquitin-like modifier (SUMO) protein is covalently attached to a lysine residue in a Ψ-K-X-D/E consensus sequen

• Following the discovery of diketo compounds S and L

  2021-11-06

  

  Following the discovery of β-diketo compounds S-1360 [31] and L-731988 [32] as anti-HIV integrase inhibitors, a group of researchers discovered a potent ccr5 antagonist based derivative (1) as the inhibitor of HIV integrase functioning at the 3′-processing and strand transfer steps of HIV integrase

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