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Compounds and were tested for
2022-06-16
Compounds , and were tested for pharmacodynamic effects in a mouse oral glucose tolerance test (oGTT) in wild-type and GPR120 deficient mice, and each compound demonstrated GPR120 mechanism-based effects. Data for compound is shown in , indicating mechanism-based reduction in glucose excursion a
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With this goal in mind we proceeded
2022-06-16
With this goal in mind, we proceeded to explore the C5-heteroaryl class of pyrazole-acids. Initial efforts, focused on a thiophene replacement, demonstrated little improvement. The 2-thiophene derivative (0.25μM and 0.24μM), a surrogate to the phenyl moiety, demonstrated only a modest boost in activ
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Limited efforts were made to
2022-06-16
Limited efforts were made to exploit the naturally-occurring antigen-specific Treg for ex vivo expansion. This study sets up a reproducible protocol for the expansion of insulin-specific Treg isolated from NOD mice. These NU 1025 exhibited higher suppressive capacity compared to the polyclonal Treg
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There was a statistical significant
2022-06-16
There was a statistical significant correlation between CD39 expression on CD4+ T cells and CD38 and ZAP-70 (Table 3). Del 6q was detected in 19 patients (63.3%) with a range of 2–75% and a mean of 32.97 ± 14.85. As regards to the staging system, del 6q was significantly higher in high risk group o
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During pain signal transmission glutamate
2022-06-16
During pain signal transmission, glutamate is released into the synaptic cleft, which, in turn, causes activation of N-methyl-d-aspartate (NMDA) receptors and hence neurotransmission across the synapse occurs. The synaptic concentration and resultant activity of glutamate are controlled by excitator
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Fmoc-Thr(tBu)-OH australia To help resolve the question of s
2022-06-16
To help resolve the question of simple binding versus transport, we reasoned that if quercetin is transported by GLUT1, we should be able to block its uptake by other GLUT1 inhibitors. We initially investigated the effects of two newly identified GLUT1 inhibitors, BAY-876 and WZB-117. WZB-117 was fi
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Up to now the research about the effect
2022-06-16
Up to now, the research about the effect of PAs on inhibiting carbohydrase activity in vitro or reducing blood sugar level in vivo was mainly reported in PAs from grape seeds, Lepisanthes alata (Malay cherry) leaves, sorghum, pomegranate, cranberry and persimmon (Banerji and Banerjee, 2016, Barrett
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Sequences of hexokinases were initially deduced and predicte
2022-06-16
Sequences of hexokinases were initially deduced and predicted based on cDNA clones (Andreone et al., 1989, Schwab and Wilson, 1989, Schwab and Wilson, 1991, Griffin et al., 1991, Thelen and Wilson, 1991). Analysis of genome sequence data identified, in PF-562271 to the 4 expected known hexokinase e
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br Acknowledgements br Introduction Glucagon a amino acid pe
2022-06-15
Acknowledgements Introduction Glucagon, a 29-amino SBE 13 HCl synthesis peptide, is released from the pancreatic islets, intestine and stomach. Glucagon is released under hypoglycemic conditions and then elevates blood glucose levels, serving as a major counter hormone [1]. The regulation of
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Neither GIP nor GIPR SNPs
2022-06-15
Neither GIP nor GIPR SNPs were associated with occurrence of fractures in the OPRA cohort (Table 4). Discussion The basis for this study lies in the role of glucose-insulinotropic peptide (GIP) hormone in the regulation of insulin secretion as well as its anabolic effect on osteoblasts and inhib
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Iodination of commercially available with excess ICl
2022-06-15
Iodination of commercially available with excess ICl in AcOH gave a quantitative yield of , which was cyclized with benzyl thioamides to give the 2-benzyl-9,10-dihydro-4-1-thia-3,4-diaza-benzo[]azulenes . Coupling of the iodides with heterocycles including imidazoles, triazoles, or zinc cyanide usi
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Canine ANGPTL7 / Angiopoietin-like 7 Protein (Fc Tag) br Su
2022-06-15
Summary The presented results of the analysis of the unfolding of G-quadruplex and i-motif, which may appear within the telomeric DNA region, led to several important conclusions. Namely, determination of the work necessary to unfold of these structures, in biased molecular dynamics involving ste
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The extensive worldwide research efforts in the decade follo
2022-06-15
The extensive worldwide research efforts in the decade following FFA1 de-orphaning aimed at developing clinically useful FFA1 agonists were nearly halted after Takeda’s first-in-class agent fasiglifam (TAK-875) was discontinued in phase III of human trials. On the date of submission of this manuscri
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LDN 209929 dihydrochloride Regarding IAV types of hemagglut
2022-06-15
Regarding IAV, 18 types of hemagglutinin and 11 types of neuraminidase were described and none of the commercialized antiviral drugs are susceptible to protect against all strains that will emerge from the animal reservoir (Webby and Webster, 2003). The strong dependencies of influenza viruses on we
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As a part of our continuing efforts towards discovery of
2022-06-15
As a part of our continuing efforts towards discovery of new class of compounds against different therapeutic areas and based on the literature reports, we designed a dual pharmacophore which possess a long aliphatic chain of free fatty acids and a phenyl propanoid part of known GPR40 agonists. Here
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