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melatonin receptor agonists It appears that not all GPR agon
2022-05-31
It appears that not all GPR119 agonists require a high dose to elicit acceptable melatonin receptor agonists control. According to preclinical data presented at the GTCbio Diabetes Summit, a 3mg/kg dose of AR-7947 was enough to induce similar blood glucose-lowering effects compared to those achieved
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br Perspectives br Contributors BP study concept design
2022-05-31
Perspectives Contributors BP: study concept & design, literature review, data analysis & synthesis & presentation, primary draft of the manuscript; JDR: data analysis, Fig. 1 illustration, manuscript review & revision; ZP: study concept & design, manuscript review & edit; MI: manuscript review
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br Discussion The present study showed that the factors of
2022-05-31
Discussion The present study showed that lomitapide the factors of pre-exposure and glutamate drug injections might affect the total latency time. However, the factor of sex did not affect the total latency time. The results indicate that the glutamate system and pre-exposure, but not sex, influe
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br Conflicts of interest br Funding This work was
2022-05-31
Conflicts of interest Funding This work was supported by the National Natural Science Foundation of China (No.81670558; 81800542), and the Science & Technology Development Fund of Tianjin Education Commission for Higher Education (No.2017KJ221). Acknowledgements Introduction Free fatty
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br Materials and methods br Results br
2022-05-31
Materials and methods Results Discussion Our study demonstrates that human GIP(3-30)NH2 is a selective GIPR antagonist that inhibits both GIP-mediated cAMP signaling, β-arrestin recruitment, and GIPR internalization. Furthermore, we demonstrate that human GIP(3-30)NH2 binds with high affini
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Seizures in turn selectively modulate
2022-05-31
Seizures, in turn, selectively modulate the crizotinib synthesis of GalR in the hippocampus. Thus, pilocarpine-induced SE led to a 30% downregulation of GalR2 without affecting GalR1 (personal communication with T. Bartfai, Scripps Research Institute). Therefore, despite the fact that GalR2 could ha
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We next determined the selectivity profile of the
2022-05-31
We next determined the selectivity profile of the most potent GPR40 agonists (4k–n) against other free fatty Imeglimin receptors (FFA3/GPR41, FFA2/GPR43 and FFA4/GPR120). FFA2 and FFA3 agonists have a preference in binding short-chain fatty acids while FFA1 and FFA4 have a higher affinity to medium
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STA-21 Natural product based drug discovery can be enhanced
2022-05-30
Natural-product-based drug discovery can be enhanced with computational methods [205]. Because most of the reported small-molecule natural inhibitors of fMLF-induced functional responses were not evaluated in STA-21 binding assays, we used molecular modeling to predict how well these compounds fit t
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br Introduction In addition to glucose
2022-05-30
Introduction In addition to glucose, which is the foremost stimulator of insulin secretion in beta-cells, other nutrients such as free fatty acids (also called non-esterified fatty acids, NEFA) contribute to glucose-stimulated insulin secretion (GSIS). Glucose triggers the processes leading to in
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Consistent with our result Camacho Barquero and coworkers sh
2022-05-30
Consistent with our result, Camacho-Barquero and coworkers showed that curcumin reduced phospho-P38 MAPK. P-38 MAPK is a key effector of several downstream factors that eventually modulate the homing of monocytic cells during the onset of intestine inflammation (Camacho-Barquero et al., 2007). Along
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The third group also included samples belonging
2022-05-30
The third group also included samples belonging to subjects with undetectable viraemia, for which the negative or persistence of the indeterminate WB result in subsequent samples indicated a non-HIV infection. In this subgroup, the VITROS HIV Combo test (as well as the other two tests) was negative
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Estradiol Cypionate It is important to mention that the IC o
2022-05-30
It is important to mention that the IC50 of cetirizine needed to achieve histamine H2 receptor desensitization was 0.43 µM or 170 ng/ml (Fig. 1B), becoming clinically relevant since pharmacokinetic studies after oral administration of the clinically used dose (10 mg/day) reported a maximal plasma co
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Nowadays it is accepted that
2022-05-30
Nowadays, it is accepted that ligands which have been classically described as inverse agonists, due to their negative efficacy at modulating the G protein pathway, could also display some positive efficacy regarding receptor desensitization, internalization, or even signaling though another pathway
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Myocardial growth and maturation is regulated in
2022-05-30
Myocardial growth and maturation is regulated in part by signals from the underlying endocardium (Brutsaert, 2003, de la Pompa and Epstein, 2012, Rentschler et al., 2010). More generally, endothelial SM-406 australia play an increasingly appreciated role in instructing organogenesis by providing in
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br Hippo pathway signalling The Hippo
2022-05-30
Hippo pathway signalling The Hippo pathway is an evolutionarily conserved signal transduction pathway regulated by cell-cell contact, cell polarity, mechanical cues, ligands of G-protein coupled receptors, and cellular sphingosine 1 phosphate receptor status [10]. This pathway is linked to devel
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