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br Materials and methods br Results
2021-10-01
Materials and methods Results Discussion The glucose transporter GLUT1 can be acutely activated or inhibited in L929 fibroblast auda by a wide variety of reagents or nutrient conditions [[9], [10], [11], [12],36,50]. This abrupt change in the activity of GLUT1 occurs within minutes and wit
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br FAAH regulation of ECB signaling ECBs are
2021-09-30
FAAH regulation of ECB signaling ECBs are fatty regorafenib side effects amides and monoacylglyerols functioning as neuromodulator lipids that exhibit rapid (within seconds) on-demand biosynthesis in response to neuronal activation, and are subsequently degraded by specialized catabolic enzymes.
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br Transportation from TGN toward plasma membrane
2021-09-30
Transportation from TGN toward plasma membrane The insulin molecules are packaged along with other molecules such as C-peptides, amylin, Zn2+, ATP and GABA in synaptic-like macrovesicles (SLMVs, with the diameters of 50–100 nm) and large dense core vesicles (LDCVs, with the diameters of 200–500 n
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GSK dimethylpiperidin yl butoxy phenyl piperidine carbonyl n
2021-09-30
GSK-835726 (3-[4-[4-[4-[4-(3,3-dimethylpiperidin-1-yl)butoxy]phenyl]piperidine-1-carbonyl]naphthalen-1-yl]propanoic acid) is a dual H1/H3 receptor antagonist with the potential to be used in allergic rhinitis. Likewise GSK-1004723, the drug-likeness criteria have not been passed by this drug candida
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Arena Pharmaceutical introduced a biaryl
2021-09-30
Arena Pharmaceutical introduced a biaryl sulfone derivative with antagonistic activity at H3Rs known as APD-916, ((R)-1-(2-(4'-(3-methoxypropylsulfonyl)biphenyl-4-yl)ethyl)-2-methylpyrrolidine), which was rationally designed from corresponding sulfonamides in order to yield compounds with short dura
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Given the role that activation of GC C has
2021-09-30
Given the role that activation of GC-C has in stimulating fluid secretion in the intestine, attempts have been made to exploit this pathway to relieve symptoms of chronic constipation. Currently, an orally administered synthetic ST mimic, linaclotide [29], has been successfully shown to alleviate co
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On the basis of the structure of the
2021-09-30
On the basis of the structure of the Rab35/ACAP2 complex, the authors identified Thr76 in switch II of Rab35 as one key specificity determinant (Lin et al., 2019). The crystal structure shows that the hydroxyl group of Thr76 forms a Tetrazole with Asp756 in ACAP2, while the methyl group is a part of
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Various inhibitors have been developed to
2021-09-30
Various inhibitors have been developed to target molecules present in these pathways. They include both man-made monoclonal NHS-SS-Biotin as well as small molecule membrane permeable inhibitors that often target kinases or phosphatases [5], [338], [348], [364]. In summary, these pathways are freque
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br Conclusion and future perspectives The
2021-09-30
Conclusion and future perspectives The nicotinic Cy3 hydrazide receptor GPR109A and its close relatives GPR109B and GPR81 are primarily expressed in adipocytes and are coupled to Gi-type G proteins. Recently, the ketone body β-hydroxy-butyrate, the β-oxidation intermediate 3-hydroxy octanoic aci
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It is interesting to note that the
2021-09-30
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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SAR around amino derivative revealed a number of
2021-09-30
SAR around amino-derivative revealed a number of interesting trends related to the serum shift and in vitro activity (). A comparison of derivative , and its epimer , showed that the stereochemistry had little effect on the serum shift and the intrinsic affinity for the receptor. In contrast, re-po
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The life cycle of T cruzi
2021-09-30
The life cycle of T. cruzi requires both vertebrate and invertebrate hosts. In the insect (invertebrate) vector, the protozoan undergoes extracellular replication, whereas in the mammalian (vertebrate) host it replicates by obligate intracellular multiplication (Rodrigues et al., 2014). Hence, the p
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EAATs can transport glutamate aspartate
2021-09-30
EAATs can transport glutamate, aspartate, cysteic acid, and serine-o-sulfate (Bjorn-Yoshimoto and Underhill, 2016). All EAATs work as symporters co-transporting 2 or 3 molecules of Na+ and a proton with each molecule of glutamate (or aspartate). In addition, a K+ ion is counter-transported ending in
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In conclusion atorvastatin but not pravastatin impaired gluc
2021-09-30
In conclusion, atorvastatin but not pravastatin impaired glucose utilization in C2C12 cells and glucose tolerance in HFD mice, which may be partly due to the inhibition of GLUT4 translocation in muscle cells. The decrease in the cholesterol level induced by atorvastatin may partly account for the in
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The HH signaling has also been
2021-09-30
The HH signaling has also been implicated in the regulation of cancer stem KPT-9274 receptor (CSC) by promoting their self-renewal [53]. Activated HH signaling has been identified in CSCs of many solid tumors, such as glioblastoma, breast, colon, pancreatic cancer, melanoma, and hematological malig
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