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In addition to the four classical FGFRs there is an
2022-06-06
In addition to the four classical FGFRs there is an additional receptor, FGFR like-1 (FGFRL1, also known as FGFR5) (Ornitz and Itoh, 2015, Trueb et al., 2003). FGFRL1 gene was discovered in a cartilage specific cDNA library in 2000 (Trueb, 2011, Trueb et al., 2003) and thereafter it has been found i
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Electrochemical techniques have attracted broad attention fo
2022-06-06
Electrochemical techniques have attracted broad attention for their outstanding advantages, such as satisfactory sensitivity and convenient operation. Nowadays, nucleic Bestatin hydrochloride nanostructures such as DNA tetrahedron structure, nucleic acid-mimicking structure, exhibit noticeable appl
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In summary we have designed and explored
2022-06-05
In summary, we have designed and explored synthetic routes towards novel acylsulfamoyl benzoxaborole-based HCV NS3 protease inhibitors. Interestingly, the resulting, unoptimized P1–P3 and P2–P4 macrocyclic inhibitors were equipotent in an enzyme assay and somewhat less potent in replicon assays, com
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br GPR is a class A GPCR expressed
2022-06-05
GPR119 is a class A GPCR expressed on pancreatic β-cells and certain enteroendocrine MK 571 which upon activation with an agonist, increases insulin secretion in response to rising glucose levels. Mechanistically, this insulinotropic effect is bifurcated involving both GPR119-mediated β-cell signa
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br Acknowledgement This work was supported in part by grants
2022-06-05
Acknowledgement This work was supported in part by grants from the Ministerio de Economía y Competitividad from Spain (BFU2011-23034). Introduction The glutamate hypothesis of schizophrenia emerged from observations in the 1960s that phencyclidine and similar psychotomimetic agents produce s
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We confirmed a decrease in extracellular glutamate uptake an
2022-06-05
We confirmed a decrease in extracellular glutamate uptake and the presence of efflux in an endothelial cell model of oxygen-glucose deprivation (OGD), which effectively simulates the inefficient energy supply after brain injury [15], and analysed the function of endothelial EAATs and explored the ro
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Here we studied the effects of
2022-06-05
Here we studied the effects of BZ flurazepam (FZ) at high doses in acute and chronic settings of tolerance and dependence in GluR-A−/− mice (Zamanillo et al., 1999). We used measurements in which the phenomenon of “learning while intoxicated” should play only a minor role in order to find out the si
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The novel Ghsr IRES Cre
2022-06-05
The novel Ghsr-IRES-Cre knock-in mouse line allowed us to deconstruct the involvement of MBH GHSR-expressing neurons in mediating food intake responses using chemogenetic modulation of their neuronal activity. In our studies, hM4Di DREADD virus injections to inhibit GHSR neurons targeted several nuc
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br Discussion br Concluding remarks There are
2022-06-05
Discussion Concluding remarks There are potentially hundreds or thousands of G-quadruplexes which form within promoters, telomeres, RNA transcripts, and even LINEs and SINES [9,11,121,122]. As articulated previously [27], G-quadruplexes are easily targetable with heterocyclic aromatic compound
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br Introduction Fructose bisphosphatase FBPase
2022-06-02
Introduction Fructose 1,6-bisphosphatase (FBPase; EC 3.1.3.11) catalyses the irreversible reaction of hydrolysis of fructose 1,6-bisphosphate to fructose 6-phosphate and inorganic phosphate [1]. Genetic and kinetic studies so far have demonstrated that at least two distinct isoenzymes of FBPase e
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br Experimental procedures br Results br Discussion
2022-06-02
Experimental procedures Results Discussion This study demonstrates that the genetic disruption or pharmacological inhibition of FAAH completely prevented all manifestations of pain symptoms in an NTG-induced migraine animal model. Thus, FAAH disruption or blockade abolished the activation o
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Despite a large amount of uptake for both
2022-06-02
Despite a large amount of uptake for both nanoparticles, only after transport across intestinal epithelia do the nanoparticles really contribute to improving absorption. Though the transport of nanorods across monolayer was a little bit more than nanospheres, the total transport was less than 2% (A1
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In the course of studies leading to the discovery
2022-06-02
In the course of studies leading to the discovery of , modifications at the P3-P4 interface of these tripeptide-based inhibitors were examined with the goal of improving potency while maintaining a PK profile similar to . In this report, we summarize those studies which led to the identification of
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br Reactive Dicarbonyls and Mitochondrial Dysfunction Althou
2022-06-02
Reactive Dicarbonyls and Mitochondrial Dysfunction Although mitochondrial dysfunction has been suggested to be one of the main pathogenic mechanisms in diabetic neuropathy, little is known about the nature and extent of mitochondrial damage resulting from chronic hyperglycemia. Mitochondria funct
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To further investigate if GPR was the functional target of
2022-06-01
To further investigate if GPR40 was the functional target of these phenylpropiolic Ponceau S Staining Solution analogs, GW-1100, a selective antagonist of GPR40-mediated Ca2+ elevations in HEK293 cells with an IC50 value equal to 1 μM, was used to inhibit agonist-induced intracellular calcium flux
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