• It is apparent from the data

  2022-06-15

  

  It is apparent from the data in that none of the ligands exhibits significant toxicity as determined by the viability of human embryonic kidney (HEK 293) cells at a concentration of 100 μM. It is also apparent from the data in and that a number of the ligands inhibit the HIV-1 IN enzyme. However,

• individuals with variants in the codon region had

  2022-06-15

  

  13 individuals with variants in the codon 1031–1159 region had global developmental delay and apparent ID, ranging from speech delay and learning difficulties to markedly impaired basic life functions (Table 2 and Table S3). The last available occipitofrontal-circumference measurements revealed micr

• Based on the aforementioned findings variations

  2022-06-15

  

  Based on the aforementioned findings, variations of the imidazole heterocycle present in the endogenous ligand histamine (1) led to 2-(thiazol-2-yl)ethanamine (2-TEA, 2) and later to 2-(3-bromophenyl)histamine or 2-(3-(trifluoromethyl)phenyl)histamine (3) (Fig. 3). Interestingly, 2-TEA demonstrated

• br cAMP cGMP effector systems in human platelets PKA

  2022-06-15

  

  cAMP/cGMP effector systems in human platelets (PKA, PKG, PDEs) In eukaryotic cells, the effects of intracellular cAMP are mediated by two types of cAMP-dependent protein kinases (PKA type I and II) and cAMP-regulated guanine nucleotide exchange factors (EPAC/cAMP-GEF) which activate the RAS GTPas

• However a direct effect of ROS on GSNOR has also

  2022-06-15

  

  However, a direct effect of ROS on GSNOR has also been described. Inhibition of GSNOR by ROS has been demonstrated for yeast [44], Arabidopsis[36], and Baccaurea ramiflora (Burmese grape) [45] suggesting that this could be a general mechanism of crosstalk between ROS and ·No signaling. Interestingly

• The intracellular signaling that mediates the

  2022-06-14

  

  The intracellular signaling that mediates the adipogenesis induced by GPR120 still remains largely unknown. In the present study we showed that TUG-891 induced the activation of [Ca2+]i and ERK1/2 signaling in 3T3-L1 cells. Moreover, incubation of TUG-891 combined with BAPTA-AM or U0126 abolished TU

• Recently a G protein coupled receptor GPR a was

  2022-06-14

  

  Recently, a G-protein-coupled receptor, GPR109a, was identified as a molecular target for niacin. Following this breakthrough, our group initiated a drug discovery program focused on the development of a high affinity ‘flush-free’ niacin-like agonist. Previously, we reported on the identification of

• This study was approved by our institutional ethics committe

  2022-06-14

  

  This study was approved by our institutional ethics committee, and informed consent was obtained from each participant or legal guardian. We performed whole-genome SNP genotyping in the one unaffected and two affected siblings by using the Illumina Human 610 Genotyping BeadChip panel, which interrog

• The in vivo biological activity of the four novel analogues

  2022-06-14

  

  The in vivo biological activity of the four novel analogues was then systematically assessed in three animal models including normal control, high fat fed and ob/ob mice. As expected from earlier in vitro studies, all four glucagon receptor antagonists had minor effects on glucose or insulin concent

• br The actions of GLP on the vasculature endothelium

  2022-06-14

  

  The actions of GLP-1 (9–36) on the vasculature/endothelium The previous sections have ascribed the vascular and/or endothelial actions of GLP-1/GLP-1R agonists to potential direct actions through a canonical GLP-1R, but as mentioned previously, whether VSMCs and ECs express a full-length GLP-1R r

• Although GLP has greater insulin releasing effects at pharma

  2022-06-14

  

  Although GLP-1 has greater insulin-releasing effects at pharmacological concentrations [10], it is apparent that the higher circulating concentrations of GIP combined with more pronounced increase in secretion following feeding make GIP the major physiological incretin [7], [11]. The peptide exerts

• br Discussion RBCs possess a much simpler composition and

  2022-06-14

  

  Discussion RBCs possess a much simpler composition and structure than other eukaryotic 7ACC1 and can therefore serve as a convenient system on which to study how cell functioning relates to the molecular and supramolecular properties of its constituents. The model developed in this work is aimed

• Cx has been shown to be

  2022-06-14

  

  Cx45 has been shown to be serine phosphorylated by CaMKII, CK1, PKA, and MAPK in HeLa umi 2 [77], [78]. Phosphorylation by PKA and MAPK were associated with decreased junctional conductance [78], suggesting that phosphorylation of Cx45 may influence conduction properties. Overall, the roles of both

• Cx mimetic peptides short synthetic peptides corresponding

  2022-06-14

  

  Cx mimetic peptides, short synthetic peptides corresponding to intracellular amino LDC1267 sequences of diverse Cx have better specificity compared to traditional GJ blockers and openers. In particular, it was reported that Cx mimetic peptides reversibly inhibited GJ channel function in a concentrat

• Based on the above considerations the

  2022-06-14

  

  Based on the above considerations, the β-galactosidase gene from Exiguobacterium acetylicum MF03 (not previously reported) was cloned, expressed and purified with the aim of assessing the potential of this novel enzyme for catalyzing reactions of synthesis and hydrolysis of glycosides. Because of E.

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