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Acknowledgments This work was supported by the
2022-06-05

Acknowledgments This work was supported by the Natural Science Foundation of China (Nos. 21602254, 81603194), the Natural Science Foundation of Jiangsu province, China (BK20160767) and National Found for Fostering Talents of Basic Science (NFFTBS, J1310032). Introduction Glucocorticoids (GC) pl
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Some malignant human tumors cells
2022-06-02

Some malignant human tumors Kenpaullone also express FPRs and respond to bacterial or endogenous agonists by increased motility and growth. For instance, FPRs expressed by human gastric cancer cells, mediate epithelial–mesenchymal transition, cell proliferation, migration, and resistance to apoptosi
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Following the discovery of diketo compounds S and L
2022-06-02

Following the discovery of β-diketo compounds S-1360 [31] and L-731988 [32] as anti-HIV integrase inhibitors, a group of researchers discovered a potent RN 1734 based derivative (1) as the inhibitor of HIV integrase functioning at the 3′-processing and strand transfer steps of HIV integrase. Bioass
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br Methods br Results br Discussion Exercise
2022-06-02

Methods Results Discussion Exercise results in a remarkable redistribution of blood flow, which increases in active skeletal muscles but decreases in the splanchnic circulation. The regional blood flow in the kidney, spleen, stomach and intestine was measured by using the microsphere techni
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Based on our results we propose three possible mechanisms of
2022-06-02

Based on our results, we propose three possible mechanisms of HER2 loss after trastuzumab-based therapy (Fig. 3). The first possibility is a result of the differential effects of treatments on clonal subsets. In breast cancer, such selective pressure has been suggested to preferentially eradicate HE
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br Conclusion The addition of cellulose to
2022-06-02

Conclusion The addition of K-115 to natural substrate increases the number of H-bonds which indicates an increase in the stability of the docking systems. The investigated compounds are more stable than natural substrate in docking systems, where the natural substrate has two H-bonds while the i
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Radezolid br Introduction The discovery that the nitric oxid
2022-06-02

Introduction The discovery that the nitric oxide (NO), soluble guanylate cyclase (sGC), and cyclic guanosine monophosphate (cGMP) pathway mediates erection has led to the use of phosphodiesterase type 5 (PDE-5) inhibitors as the gold standard for treating erectile dysfunction (ED) through the inh
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br Introduction Atherosclerosis is a chronic
2022-06-02

Introduction Atherosclerosis is a chronic inflammatory disease characterized by lipid and leukocyte accumulation within the arterial wall. Homocysteine (Hcy) is a thiol-containing amino Vinblastine sulfate derivative derived from the metabolism of dietary methionine. Epidemiological studies have
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Likewise and considering the aforementioned biological actio
2022-06-02

Likewise, and considering the aforementioned biological actions of ketogenic diet-derived MCFA on neuronal excitability, it could be postulated that specific receptors for fatty acids could also be involved. For example, the GPCR for medium to long chain fatty acids, FFA1/GPR40, might also contribut
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In this study we explore different mathematical models for
2022-06-02

In this study, we explore different mathematical models for describing the IVIVC of a preclinical dataset of 12 different dual GPR109A/GPR81 agonists. The objective is to establish a predictive model of in vivo lipolysis suppression in the rat based on in vitro potency data. First, a nonlinear mixed
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Acute in vivo experiments were performed in normoglycemic
2022-06-02

Acute in vivo experiments were performed in normoglycemic 129SVE mice to confirm GPR119 activation and corresponding BI6727 control. GIP release was utilized as a biomarker for target receptor engagement and plasma GIP levels were measured 45min after oral dosing (). Both 3 and 10mg/kg produced an i
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Previously we have shown that the
2022-06-02

Previously, we have shown that the natural flavonoid compounds that possess C-4 ketone group and C-5 hydroxy group, such as baicalein, luteolin, myricetin and quercetin, effectively inhibit human GLO I. Considering our interest in inhibitors of GLO I and based on the rationale mentioned above, struc
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PBI is an agonist of GPR and acts
2022-06-01

PBI-4050 is an agonist of GPR40 and acts as an antagonist or inverse agonist of GPR84. It cannot be excluded that other targets besides GPR40 and GPR84 could be implicated in the mechanism of action of PBI-4050 and could be explored in future studies. However, the present study, and in particular th
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br Acknowledgements br Introduction Aminoacyl tRNA
2022-06-01

Acknowledgements Introduction Aminoacyl-tRNA synthetases catalyze the formation of an ester bond between an amino tenofovir alafenamide and the 3′ end of a tRNA in a two-step reaction. First, the amino acid is activated and an enzyme-bound adenylate intermediate is formed. Then, the amino acid
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br Acknowledgements This work was financed
2022-06-01

Acknowledgements This work was financed by the projects “Mejora Genética del Almendro” (MINECO-Spain, AGL2017-85042-R), “The molecular mechanisms to break flower bud dormancy in fruit trees” to RS-P within the Villum Young Investigator Program and by the VILLUM Research Center for Plant Plasticit
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