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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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Gene expression of both GPR A
2021-10-15

Gene expression of both GPR109A and GPR81 in adipocytes has been linked to PPARγ activation [22]. Treatment with the thiazolidinedione (TZD) PPARγ agonist, rosiglitazone, increases GPR109A and GPR81 expression, and knockdown of PPARγ suppresses receptor expression in fully differentiated human multi
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Migratory properties of Treg are extremely
2021-10-15

Migratory properties of Treg are extremely important for the potential in vivo application. Therefore, the observed expression of CXCR3 on almost all obtained insulin-specific Treg is crucial for directing Pertussis Toxin receptor into the inflamed tissue (in this case pancreatic islets). CXCR3 res
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br Results and discussion br Conclusions br Introduction The
2021-10-15

Results and discussion Conclusions Introduction There is no effective treatment for HIV-associated neurocognitive disorder (HAND) which affects about half of the over 36 million people infected (Saylor et al., 2016). HIV can remain in the ap1 during combination antiretroviral therapy (Elli
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Glutamate aspartate transporters or excitatory amino
2021-10-15

Glutamate-aspartate transporters or excitatory amino SCH 727965 transporters (EAATs) are essential for the maintenance of glutamate homeostasis. EAATs are widely distributed in central neurons and glial cells (Danbolt, 2001, Martinez-Lozada et al., 2011). They are driven by Na + and K+ gradients (J
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br Materials and methods br Conflicts of interest Some
2021-10-15

Materials and methods Conflicts of interest Some of the peptidomimetic compounds in this work are the subject of the patent application “Peptidomimetics for Imaging the Ghrelin Receptor”, WO/2016/191865 A1, December 8th, 2016. Acknowledgements Special thanks go to Rebecca McGirr (Lawson He
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By using pharmacological treatment with CBX
2021-10-15

By using pharmacological treatment with CBX or transgenic animals lacking the two major astroglial Cxs, the Double KO mouse, we demonstrated that the gap-FRAP technique was able to detect the total inhibition of GJC with a reduction of about 39% and 38% compared to control, respectively. The residua
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Recent studies have elucidated a profound role for FFA in
2021-10-14

Recent studies have elucidated a profound role for FFA4 in modulation of metabolism and energy utilization as well as endocrine and immune function, and as a consequence, have thrust FFA4 to the forefront of drug discovery efforts. For example, activation of FFA4 by fatty corticosterone or syntheti
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To further investigate if GPR was the functional
2021-10-14

To further investigate if GPR40 was the functional target of these phenylpropiolic CHC analogs, GW-1100, a selective antagonist of GPR40-mediated Ca2+ elevations in HEK293 cells with an IC50 value equal to 1 μM, was used to inhibit agonist-induced intracellular calcium flux [15]. HEK293-GPR40 cells
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