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br The Farnesoid X receptor FXR identification and ligands
2022-08-08
The Farnesoid X receptor (FXR): identification and ligands The Farnesoid X receptor (FXR) belongs to a family of proteins called Nuclear Receptors (NRs). NRs are a class of ligand-activated transcription factors, which transactivate networks of target genes, thereby mediating a wide range of phys
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br Short Communication Free fatty acid receptors FFAR play s
2022-08-08
Short Communication Free fatty Alda 1 synthesis receptors (FFAR) play significant roles in energy metabolism (Brown et al., 2005; Ichimura et al., 2009). The receptor FFAR1 is involved in insulin secretion in humans (Meidute Abaraviciene et al., 2013). Activation of the receptor FFAR2 increases l
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Interestingly we have shown that
2022-08-08
Interestingly, we have shown that OA required FFAR4 to induce osteoblast gene expression in MC3T3-E1 pre-osteoblasts, but not to inhibit osteoclastogenesis in RAW264.7 murine macrophages. As previously suggested, FFAR1 may mediate the effects of OA in osteoclasts. However, FFAR1 has also been shown
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br Acknowledgments This study was
2022-08-08
Acknowledgments This study was supported by a Conquer Cancer Foundation (American Society for Clinical Oncology) Drug Development Research Professorship Grant (AAA). Introduction Gastric cancer (GC) is one of difficult cancers to treat in terms of its poor prognosis and limited applicability
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Receptor activator of NF B ligand RANKL and
2022-08-08
Receptor activator of NF-κB ligand (RANKL) and macrophage colony-stimulating factor (M-CSF) stimulate the generation of osteoclast PF 04418948 [10], [11], [12], [13]. In response to sphingosine 1-phosphate (S1P) signaling, osteoclasts then attach to regions of bone undergoing resorption [14]. In RA
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Our observation of LPS induced increase in
2022-08-08
Our observation of LPS-induced increase in the sensitivity of cultured endothelium-intact coronary Tubastatin A HCl towards stimulation with selective ETB receptor agonist (S6c) could be explained by activation of TLRs receptors located on the endothelium of rat coronary arteries. However, the poss
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FoxM a downstream target of Gli has been
2022-08-05
FoxM1, a downstream target of Gli, has been mainly related to E6 Berbamine regulation and cellular proliferation in tumor (Alvarez-Fernandez and Medema, 2013, Halasi and Gartel, 2013, Teh et al., 2002). Especially, FoxM1 is a regulator of G1/S and G2/M transitions and M-phase progression (Wonsey & F
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As comparators compounds and were made using
2022-08-05
As comparators, compounds and were made using the pyrazolopyridine core with the CF triazole attached. The 2-fluorophenyl group was replaced with the methylpyrimidine in compound . The potency of these compounds were very good and compound looks attractive from a physicochemical perspective as it
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Here we used Drosophila and mouse models to address
2022-08-05
Here, we used Drosophila and mouse models to address the biological function of RALs in the adult intestine. Our results demonstrate a conserved in vivo role for RALs in ISC function during tissue homeostasis and regeneration. ISCs lacking RALs were at a disadvantage compared to wild-type neighbors.
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α-mangostin br Introduction Initial studies of cancer metabo
2022-08-05
Introduction Initial studies of cancer metabolism in the early 1920s showed that the cancer phenotype for glucose metabolism is unique, with increased abilities to take up glucose and produce lactate, even under aerobic conditions [1]. This pathway, called aerobic glycolysis or the Warburg effect
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Further our study provides the first
2022-08-05
Further, our study provides the first evidence that zaprinast and kynurenic Reboxetine mesylate mg administration not only prevented the development of thermal and mechanical hypersensitivity but also enhanced morphine antinociceptive properties. Morphine is considered to be one of the most effectiv
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6780 sale It is interesting to note that the
2022-08-05
It is interesting to note that the long and short forms of GPR120 exist at different basal levels of phosphorylation, with the short form demonstrating a greater degree of constitutive activity [12]. Importantly, Burns and Moniri [12] showed that, upon activation, the long and short isoforms of GPR1
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Herein we report the discovery of AM AM maintains
2022-08-05
Herein, we report the discovery of AM-3189 (). AM-3189 maintains the in vivo efficacy of AMG 837 while displaying a superior pharmacokinetic profile and minimal CNS exposure. As we reported previously, activity on the GPR40 receptor varies significantly with substitution at the β-carbon relative to
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Although most of the incretin effects on glucose metabolism
2022-08-05
Although most of the incretin effects on SU5416 metabolism can be secondary to their action on insulin/glucagon secretion, some evidence strongly suggests that they could also act directly on liver glucose utilization and production [4], [13], [22], [27], [34], [44]. Supporting this concept, Ayala
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While CART increased circulating levels of GIP and GLP
2022-08-05
While CART increased circulating levels of GIP and GLP-1 in vivo, we were unable to detect any effect of exogenous CART on GIP and GLP-1 mRNA expression or GLP-1 secretion in vitro. There is no ready explanation for this discrepancy. The CART doses used (both in vivo and in vitro) have been shown to
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