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The mammalian AMPA receptor protein
2021-10-16
The mammalian AMPA receptor protein family comprises four subunits, termed GluR-A through GluR-D (or GluR1 through GluR4), which form hetero-tetrameric receptor complexes Dingledine et al. 1999, Rosenmund et al. 1998. These subunits possess distinctive intracellular C-terminal domains that can be gr
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Genetic disruption or pharmacologic inhibition
2021-10-16
Genetic disruption or pharmacologic inhibition of the hepatic glucagon pathway has invariably been shown to increase pancreatic α cell mass. This has been observed in glucagon receptor (GCGR) knockout (Gcgr−/−) mice (Gelling et al., 2003), glucagon knockout mice (Hayashi et al., 2009), prohormone co
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Inflammatory pain is very common in the clinic A study
2021-10-15
Inflammatory pain is very common in the clinic. A study demonstrated that galanin was upregulated after nerve injury or inflammation (Ma and Bisby, 1997). It has been reported that galanin plays an important role in the transmission of nociceptive information in the spinal cord of rats with inflamma
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Knock out mice of FXR showed enhancing cholesterol
2021-10-15
Knock-out mice of FXR showed enhancing cholesterol metabolism in vivo and reducing serum levels of total cholesterol. Additionally, the results of FXR-deficiency mice revealed potential effects on the improvement of obesity and diabetes.19, 20 As a natural FXR ligand, guggulsterone possesses antagon
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With the identification of small nonpolar substituents
2021-10-15
With the identification of small nonpolar substituents at R3 of the phenylpropanoic acid ring providing improved activity at FFA4, exploration of the benzyl SAR was undertaken (). Small substituents were well tolerated at both the and positions (–) with the 2-bromo- (), 2-isopropoxy- (), and 3-methy
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a br Materials and methods br Results br Discussion The deve
2021-10-15
Materials and methods Results Discussion The development of HCC is a multistep process involving the accumulation of multiple genetic and epigenetic alterations that lead to the activation of oncogenes and inactivation of tumor suppressor genes [20]. Frequent intrahepatic or pulmonary metas
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Mapping PPI networks is challenging
2021-10-15
Mapping PPI networks is challenging, as it is difficult to express and purify large variaties of nor-Binaltorphimine dihydrochloride in sufficient quantities to allow the study of interactions between them. Membrane-bound proteins are particularly difficult to purify in functional form due to their
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Multiple studies from our laboratory and others which
2021-10-15
Multiple studies from our laboratory and others, which have used stoichiometric kinetic analyses of ANP/NPRA, have provided strong evidence that bound ligand-receptor complexes are internalized and processed intracellularly, and that degraded products are released into the culture medium of various
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br Modulators of the GUCY
2021-10-15
Modulators of the GUCY2C/cGMP/PDEs signaling pathways for CRC prevention and therapy (pre-clinical and clinical development) Several modulators of the GUCY2C/cGMP/PDEs signaling pathways, including GUCY2C agonists and PDEs inhibitors, have been developed and explored as chemopreventive agents for
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GSTP c C T SNP was genotyped in
2021-10-15
GSTP1 c.341C > T SNP was genotyped in 90 patients tumor and 180 normal healthy individuals. The profile of GSTP1 c.341C > T Anisomycin and genotypes is shown in Table 2. The profile of the genotypes was in agreement with Hardy-Weinberg equilibrium (χ2 = 2.11). Minor allele frequency (341T) among OS
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Introduction Glycogen synthase kinase GSK is an enzyme playi
2021-10-15
Introduction Glycogen synthase kinase-3 (GSK-3) is an enzyme playing multiple roles in animal tissues and organs, and STO-609 acetate is not an exception. Apart from involvement in regulation of apoptosis and survival GSK-3 influences neuronal morphology, synapse formation, memory reconsolidation
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In addition during the preparation
2021-10-15
In addition, during the preparation of this manuscript, Oka et al. [7] demonstrated that LPA acts as receptor ligand for GPR35 and that LPA is more potent than KYNA in eliciting a calcium mobilization (EC50: 30nM vs. 39μM for LPA and KYNA, respectively). Other endogenous GPR35 ligands, therefore, mi
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Overall this study provides compelling evidence that
2021-10-15
Overall, this study provides compelling evidence that overexpression of catalase coupled with an enriched diet of OM3 fatty acids are metabolically beneficial. This combination was shown to increase adipose tissue expression of the GPR120/FFAR4, which by interacting with the Nrf2 pathway, resulted i
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Strengths The primary feature of
2021-10-15
Strengths The primary feature of GPR119 agonists resides in their dual mechanism of action in regulating blood glucose 1, 2, 3, 15. GPR119 agonists stimulate GLP-1 release from intestinal L JP 1302 dihydrochloride as well as glucose-dependent insulin secretion and insulin promoter activity enhance
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In three independent groups identified
2021-10-15
In 2003, three independent groups identified GPR109A (HM74A) and GPR109B (HM74), two GPCRs, as the receptors for niacin., , GPR109A, which is present in all species, is a high affinity receptor for niacin., GPR109B, which is only present in human and chimpanzee, is a low affinity receptor for niac
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