• br Material and methods br Results

  2022-08-12

  

  Material and methods Results Discussion Neurosteroids capable of blocking the NMDAR channel attract a lot of attention as possible therapeutic agents for the treatment of neurodegenerative diseases. A large number of new HO-3867 with different structures have been synthesized in order to c

• Previous studies have demonstrated that cannabinoid potentia

  2022-08-12

  

  Previous studies have demonstrated that cannabinoid potentiation of GlyR α3 subunits contributes to cannabinoid-induced analgesia. For instance, Dehydroxylcannabidiol (DH-CBD), a chemically modified cannabinoid, can alleviate acute pain and chronic inflammatory pain by targeting spinal α3 GlyRs (Xio

• A oligomers increased ubiquitination of GLT in astrocytes

  2022-08-12

  

  Aβ1-42 oligomers increased ubiquitination of GLT-1 in astrocytes. Previous studies found that astrocytic GLT-1 is internalized from the cell surface by ubiquitination of lysines located in the cytoplasmic C-terminus of the transporter (Gonzalez-Gonzalez et al., 2008, Martinez-Villarreal et al., 2012

• Glucagon regulates the transition from hepatic glucose utili

  2022-08-12

  

  Glucagon regulates the transition from hepatic glucose utilisation in the absorptive state to glucagon production in the post-absorptive state by acute stimulation of glycogenolysis and inhibition of glycolysis [1]. An important component of this response is the phosphorylation of liver PFK2/FBPase2

• The potential therapeutic actions of

  2022-08-12

  

  The potential therapeutic actions of GHSR in the central nervous system has been in the limelight lately. Peripheral administration of GHSR agonists have been shown to inhibit oxidative stress, apoptosis, proinflammatory cytokine production, microglia activation, mitochondrial dysfunction, and excit

• Some clinical reports have suggested that galanin has a role

  2022-08-12

  

  Some clinical reports have suggested that galanin has a role in the neurobiology of mood disorders [[6], [7], [8], [9], [10]]. In behavioral studies, contradictory results have been reported [11,12]. For example, systemic administration of non-selective galanin receptor agonists, such as galmic [13]

• Psoriasis is an inflammatory skin

  2022-08-12

  

  Psoriasis is an inflammatory skin disease characterized by epidermal hyperplasia; micro-abscesses; neo-angiogenesis; a proinflammatory cytokine environment involving alterations of IL-17A, IL-23, and TNF-α; and activation of and infiltration by macrophages, mast cells, neutrophils, CD11c+ dendritic

• br Results and discussion br

  2022-08-12

  

  Results and discussion Conclusion In the continued SAR study of our previous heterocycle scaffolds represented by VX765 2, we focused especially on improving their drug-like physicochemical properties directed by lipophilicity, LE and LLE. After explored several heterocyclic scaffolds, the po

• It raises a question about origin

  2022-08-11

  

  It raises a question about origin of the sensitivity to Ca of both FBPase isozymes. Was the ancestral vertebrate FBPase inhibited by calcium similarly to the liver isozyme? And is the high sensitivity of FBP2 a new evolutionary feature of warm-blooded vertebrates? Additionally, since subcellular lo

• The exact mechanism by which N BPs inhibit FPPS remains

  2022-08-11

  

  The exact mechanism by which N-BPs inhibit FPPS remains unclear. Computer modeling [10] suggests that N-BPs mimic the structure of the enzyme’s natural isoprenoid pyrophosphate substrates, geranyl pyrophosphate (GPP)/dimethylallyl pyrophosphate (DMAPP) or act as carbocation transition state analogs

• Syt itself does not catalyze lipid mixing and membrane fusio

  2022-08-11

  

  Syt1 itself does not catalyze lipid mixing and membrane fusion. Rather, the pairing of vesicular and target membrane SNAREs into complexes serves to pull bilayers together to drive fusion; Ca•syt1 accelerates these fusion reactions so that they occur on rapid timescales in a manner that is precisely

• Histamine which was used as

  2022-08-11

  

  Histamine, which was used as the agonist, had low potencies in our functional experiments when compared to its affinity from binding studies (e.g. Lim et al., 2005). This phenomenon is related to the fact that the coupling of the presynaptic receptor to the transduction machinery and the final funct

• br Acknowledgements This work was supported by

  2022-08-11

  

  Acknowledgements This work was supported by grants from the Agencia Nacional de Promoción Científica y Tecnológica (PICT2013-0495, PICT2016-1821), and from CONICET (PIP 2013-562), as well as from Fundación René Barón and Fundación Williams. Introduction Histamine poisoning, also known as scom

• Most hexokinases are widely expressed but distinct hexokinas

  2022-08-11

  

  Most hexokinases are widely expressed but distinct hexokinases predominate specific tissues (Katzen and Schimke, 1965, Rogers et al., 1975). Hexokinase I is found in all mammalian tissues, but is most abundant in the blasticidin and kidney (griffin et al., 1992). Hexokinase II is the primary hexoki

• In an effort to further improve the

  2022-08-11

  

  In an effort to further improve the intrinsic potency, we evaluated the effect of the C4-substituent of the triazole (). Replacement of the phenyl group with a cyclohexyl or with a 2-pyridyl substituent led to losses in potency. Increasing the size of the substituent to a bi-phenyl or naphthyl gr

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