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cantharidin Glutamate activates cationic glutamate gated cha
2022-06-23
Glutamate activates cationic glutamate-gated channels (i.e. ionotropic glutamate receptors) that mediate the fast excitatory actions of glutamate. It also activate G protein-coupled receptors, named metabotropic glutamate receptors (mGluRs) (Pin and Bettler, 2016). The eight subtypes of mGluRs are k
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Through the analysis of various synthetic GPR agonists
2022-06-23
Through the analysis of various synthetic GPR40 agonists as reported in literature, we found that a number of these compounds contained a phenylpropanoic NVP-LAQ824 mg motif which was inspired from naturally occurring medium to long chain fatty acids. For instance, in the early period of discovering
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Expression and translocation of GLUT are
2022-06-23
Expression and translocation of GLUT4 are regulated by various mechanisms including protein kinase C isoforms (PKCs) and mitogen-activated protein kinase (MAPK) signals [22], [23], but the real mechanism that statins alter expression and function of GLUT4 has not been fully identified. It is general
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In the present study compared to diabetic
2022-06-23
In the present study, compared to diabetic control rats, hepatic glucose-6-phosphatase activity was significantly decreased in both SE and METF treated diabetic animals, with the latter producing greater reduction in glucose-6-phosphatase activity. This observation is consistent with the claim of Ta
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Nuclear export of GK has been reported to be dependent
2022-06-23
Nuclear export of GK has been reported to be dependent on a GK nuclear export signal (NES), mapped to residues 300–310 (Shiota et al., 1999). The assignment of a nuclear export signal common to both the liver and pancreatic GK isoform sequence suggests a possible reversible translocation of GK acros
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br Discussion According to the generally accepted notion whi
2022-06-22
Discussion According to the generally accepted notion which originated from the study of ATP-depleted NAD/NADH Quantitation Colorimetric Kit the changes in Ca2+ homeostasis induced by ATP depletion and leading to the activation of the Gárdos effect are due to the inhibition of Ca2+ pumping, and t
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LXRs are physiological regulators of cholesterol and
2022-06-22
LXRs are physiological regulators of cholesterol and lipid metabolism and influence glucose metabolism. In addition, they have been shown to repress transcription of certain pro-inflammatory genes (Jakobsson et al., 2012; Ogawa et al., 2005; Terasaka et al., 2005). Thus, LXRs can either activate or
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GLP is released in response to ingestion
2022-06-22
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 sodium butyrate receptor 4 (FFA4/GPR120) as a potential 7TM receptor involv
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In addition to the four classical FGFRs
2022-06-22
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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The precise mechanism by which erastin inhibits
2022-06-22
The precise mechanism by which erastin inhibits SLC7A11-mediated cystine import it still unknown. The initially proposed mechanism, by which erastin binds a related transport protein, SLC7A5, and inhibits SLC7A11 in trans [25], was revised soon after, and it was suggested that erastin inhibits SLC7A
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Introduction High mobility group box HMGB
2022-06-22
Introduction High mobility group box 1 (HMGB1) is a nuclear protein that plays a fundamental role in the regulation of DNA-associated events such as DNA repair, transcription, and replication. HMGB1 can be translocated to the cytosol, plasma membrane, and extracellular space in response to various
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Fas ligand FasL the natural ligand of Fas
2022-06-22
Fas ligand (FasL), the natural ligand of Fas, can interact with Fas and thus induce cell apoptosis through the cascade of death signal in various cell types [8]. Additionally, Fas, which is a member of the tumor necrosis factor (TNF) receptor superfamily and death receptor family, is one kind of tra
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Compounds and were evaluated for their pharmacokinetic prope
2022-06-22
Compounds and were evaluated for their pharmacokinetic properties in rats and the results are summarized in . Following intravenous (IV) administration, both compounds displayed low clearance (CL), short half-lives (t) and low volumes of distribution (V). When dosed orally as a solution, exposure
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br Conflict of interest br
2022-06-22
Conflict of interest Author contributions Introduction 2-Quinolones [quinoline-2(1H)-ones], while less prominent than the isomeric 4-quinolones, nevertheless enjoy significant attention as scaffolds in compounds exhibiting a variety of biological activities. These include: 4-aryl-6-chloroqu
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Histamine which was used as the agonist had low potencies
2022-06-22
Histamine, which was used as the agonist, had low potencies in our functional experiments when compared to its affinity from binding studies (e.g. Lim et al., 2005). This phenomenon is related to the fact that the coupling of the presynaptic receptor to the transduction machinery and the final funct
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