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PBI is an agonist of GPR
2022-06-17
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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Peptone To help resolve the question
2022-06-17
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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br Experimental br Results br Discussion The use of Dex
2022-06-17
Experimental Results Discussion The use of Dex-BSA asa membrane-limited glucocorticoid has been met with some skepticism, mainly for its assumed instability. Here we provide conclusive evidence that Dex-BSA is stable in solution over an extended period of time and at high temperature (i.e.,
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C steroids and their glycosylation products distribute widel
2022-06-17
C21 steroids and their glycosylation products distribute widely in Asclepiadaceae plants. Their anticancer activities have been shown in different human cell lines and in vivo animal experiments [[27], [28], [29], [30], [31], [32]]. However, the mechanisms of their anticancer activities are still un
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br Some Gardos channel perplexities While much is known abou
2022-06-17
Some Gardos channel perplexities While much is known about the Gardos channel (inside Ca2+-activated K+ channel) and it's characteristics in human red blood nucleoside analogs (e.g. [18,19]), there are a number of intriguing and unexplained phenomena that are in much need of study. One is that ac
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br Acknowledgments The authors gratefully
2022-06-17
Acknowledgments The authors gratefully acknowledge the support provide by National Natural Science Foundation of China (Number 31301415). Introduction β-Galactosidases (EC 3.2.1.23), frequently known as lactases, are widely used in lactose hydrolysis. This disaccharide is present in mammalian
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The synthesis of compounds and
2022-06-17
The synthesis of compounds and were achieved according to standard procedures. As shown in , The compound 4-methyl-1-(4-sulfobutyl)quinolonium () was prepared by alkylation reaction. Compounds and were synthesized by substitution reactions between 4-fluorobenzaldehyde and , , '-trimethylethanedi
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GLP is released in response to
2022-06-17
GLP-1 is released in response to ingestion of nutrients including carbohydrates, protein, and fat. Recent studies aimed at identifying the receptors involved in nutrient stimulated GLP-1 secretion have identified free fatty Varenicline Tartrate receptor 4 (FFA4/GPR120) as a potential 7TM receptor in
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In the light of the above
2022-06-17
In the light of the above-mentioned considerations, it is interesting to note that the FPR-related research with regards to bias agonism did not prosper during considerably during the last decade (possible exceptions are [[8], [9], [10], [11]]. However, with new insights in receptor chemistry and fu
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This review is an overview on the ongoing trials
2022-06-17
This review is an overview on the ongoing trials involving anti-FGF-FGFR therapies (Wu et al., 2013). Pathway FGFR in cancer A recent study comparing more than 4800 tumor tissue samples has shown that 7.1% of all tumor types have genetic alterations in the FGF-FGFR axis. The aberrations perce
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G-1 australia The pharmacokinetic properties of were
2022-06-17
The pharmacokinetic properties of 12 were amenable to oral dosing allowing in vivo comparison to 6. Compared to a maximum efficacious dose of 6 (60mg/kg), 12 demonstrated improved glycemic control during OGTT in high-fat fed/STZ treated (HF/STZ) and BDF/diet-induced obesity (DIO) mouse models of typ
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br Acknowledgements This work was in
2022-06-17
Acknowledgements This work was in part supported by the FöFoLe program by Ludwig-Maximilians-Universität München (to T.S.), the Deutsche Forschungsgemeinschaft (DFG) CO 291/5-2, the Human Frontier Science Program (HFSP) RGP0013, the Helmholtz Validation Funds (Helmholtz Association of German Rese
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br Introduction The term autophagy was coined by Christian
2022-06-17
Introduction The term “autophagy” was coined by Christian de Duve in 1963 to describe the process of removing and degrading intracellular components such as unused proteins and damaged organelles through lysosomes [1,2]. Autophagy has been divided into three main types, namely, macroautophagy, mi
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At the heart of ferroptosis
2022-06-17
At the heart of ferroptosis is a process of lethal lipid peroxidation, which is the oxidative addition of molecular oxygen (O2) to lipids, such as polyunsaturated fatty acyl tails in phospholipids. The first descriptions of such enzymatic reactions were in 1955 by Peterson and colleagues [50] and Ro
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The release of FBPase and aldolase from
2022-06-17
The release of FBPase and aldolase from subcellular structures of muscle was dependent on the presence of the crowding agent imitating the physiological conditions – PEG 8000 (Table 1). The amount of both enzymes associated with structures of muscle Fmoc-Glu(OtBu)-OPfp was about 6–7 times higher in
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