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Among the various delivery strategies in the field of nano
2021-11-17
Among the various delivery strategies in the field of nano-DDS, developing smart targeted nanocarriers has long been a research focus for pharmaceutical scientists11., 12.. The ideal drug delivery outcome must be precisely delivering the therapeutic agents to their sites of action, especially for an
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In conclusion we demonstrated that extrasynaptic glutamate c
2021-11-17
In conclusion, we demonstrated that extrasynaptic glutamate could in situ affect the AA metabolism via brain CYPs. CYP1B1 and CYP2U1 genes in the astrocytes are the downstream genes of CREB, and the up-regulation of CYP1B1 and CYP2U1 expression by glutamate was due to the increases in phosphorylated
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To further investigate if GPR
2021-11-17
To further investigate if GPR40 was the functional target of these phenylpropiolic CX-6258 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 [15]. HEK293-GPR40 c
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br Acknowledgements The authors are grateful for funding
2021-11-17
Acknowledgements The authors are grateful for funding provided by the Health Research Council of New Zealand. Introduction Glucose is the most important energy carrier of the brain. Glucose transporter type 1 (Glut1) is located at the blood–brain barrier and assures the energy-independent, fa
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As many of the above
2021-11-17
As many of the above studies highlight, several decades of research on Cx43 has revealed that many of these functional roles are attributed to the C-terminal domain (CT) of this protein which cannot be explained by the formation and existence of intercellular channels. Recent findings on the existen
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When we compared the effects in FST induced by
2021-11-17
When we compared the effects in FST induced by GAL and GAL(1–15), we observed that the increase in the immobility induced by GAL(1–15) was significantly higher than the one induced by GAL (Millon et al., 2015). Moreover, in climbing behaviour, GAL(1–15) also induced a stronger decrease in climbing r
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Corresponding to the different insulinotropic signaling
2021-11-17
Corresponding to the different insulinotropic signaling, the competitive radioligand-binding studies demonstrated at least 3 distinct Ketoconazole receptor on GPR40: orthosteric binding site for endogenous ligands, allosteric binding site for partial agonists and another allosteric binding site for
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Sperm exocytosis or acrosome reaction AR
2021-11-17
Sperm exocytosis or acrosome reaction (AR) is a regulated secretion with special characteristics essential for fertilization. The AR relies on the same highly conserved molecules that drive intracellular membrane fusion and exocytosis in all other mtor inhibitors (see [59] for a recent review). Two
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In conclusion three heat stable cyclic peptides guanylin
2021-11-17
In conclusion, three heat-stable cyclic peptides, guanylin, uroguanylin and renoguanylin are expressed in the intestine and kidney of the European eel, Anguilla anguilla. Their physiological functions are likely to be mediated, at least in part, by two isoforms of the guanylate cyclase type C recept
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Activity of compound in rat brain tissue highlights the
2021-11-17
Activity of compound 10 in rat Isorhamnetin tissue highlights the potential to use this new class of allosteric sGC inhibitors to study the role of the NO—sGC—cGMP signalling pathway in the brain. Reducing amounts of cGMP in cells would have implications in downstream signalling proteins, such as c
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Main Text There are over small GTPases that
2021-11-17
Main Text There are over 200 small GTPases that play critical roles in diverse fundamental cellular processes such as signal transduction, Hordenine receptor dynamics, and intracellular trafficking. Most of the GTPases act as switch-like molecules by cycling between the guanosine triphosphate (GTP)
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Despite the rapid development of synthetic ligands
2021-11-16
Despite the rapid development of synthetic ligands, the endogenous ligands of GPR109A, GPR109B and GPR81 remained elusive until recently. This is probably the result of their relatively low potencies and their metabolite character (Table 1). Traditionally, agonists of GPCRs were believed to belong t
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To further implicate the role of EAAT in morphine induced
2021-11-16
To further implicate the role of EAAT3 in morphine-induced place preference, the effects of morphine on EAAT3 NESS 0327 synthesis was determined. Interestingly, morphine increased EAAT3 protein expression in the plasma membrane of mPFC, nucleus accumbens and VTA but not in the hippocampus of wild-ty
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Ghrelin receptors in non mammals
2021-11-16
Ghrelin receptors in non-mammals are reportedly more “complicated/complex and diverse” than in mammals, having additional paralogs and splice variants (Kaiya et al., 2014). Several teleost fish GHS-Rs have been identified; however, functional characterization has been conducted in only a few (see, K
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Deoxycholic acid Further we examined the degradation of
2021-11-16
Further, we examined the degradation of Cx43. Autophagy and the proteasome system have previously been implicated in Cx43 degradation (Falk et al., 2014). DEX inhibited communication between Deoxycholic acid by promoting the degradation of Cx43 through autophagy in osteocytes (Gao et al., 2016). In
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