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In conclusion we demonstrated that the atypical
2021-10-29
In conclusion, we demonstrated that the atypical high-basal activity of the mGlu3 Pam3CSK4 Biotin results mostly from its activation by low ambient glutamate concentrations. This is due to a unique interaction network located in the extracellular domain of the mGlu3 receptor. This network acts as “
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In the present study we set
2021-10-29
In the present study we set out to discover new non-steroidal SEGRA and to analyse their mechanism of function. Towards this goal we initiated a virtual screening (VS) approach, utilizing structure-based pharmacophore modeling, in silico docking and molecular dynamics (MD) simulations. Our pharmacop
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dihydrofolate reductase Introduction Glucocorticoids are rel
2021-10-29
Introduction Glucocorticoids are released in response to stress and play an important role in inflammation, cellular growth, development, body fluid homeostasis, carbohydrate, lipid, and protein metabolism. However, circulating glucocorticoid excess has been associated with a classical phenotype of
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In Solloway and colleagues reported that
2021-10-29
In 2015, Solloway and colleagues reported that mice with alpha cell hyperplasia due to inactive hepatic glucagon receptor signaling may most likely be caused by amino cell adhesion molecules dependent mechanisms [11]. The authors then showed these adaptations are regulated by ‘mechanistic target of
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br Preclinical development of GIP agonists Since
2021-10-29
Preclinical development of GIP agonists Since the action of DPP IV is not limited to GIP, the most specific pharmacological approach for GIP would be modification at the N-terminus to disrupt DPP IV-mediated degradation. Indeed, it has been shown that GIP analogues with N-terminal modifications a
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nf-κb pathway The mechanism by which Piezo
2021-10-29
The mechanism by which Piezo1 acts in the regulation of RBC volume is not firmly established. Its curved structure implies that it is activated by an increase in membrane tension (11), a mechanism indicated by electrophysiological measurements (16). However, the RBC membrane mechanics at its physiol
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Rottlerin Many natural flavonoids have been identified as in
2021-10-29
Many natural flavonoids have been identified as influencing ionotropic GABA receptors through bioassay-guided fractionation of plant extracts (Fig. 4). HPLC-based activity profiling of extracts the traditional Chinese herbal drug Kushen (Sophora flavescens root) led to the identification of the 8-la
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Another small compound targeting IBAT has been evaluated in
2021-10-29
Another small compound targeting IBAT has been evaluated in Phase I clinical trial (EudraCT 2013-001175-21) [86]. The oral administration of A4250 to healthy subjects did not give rise to any serious adverse events, was well tolerated and had a similar safety profile as elobixibat; however, it cause
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In summary the SAR of a series of phenylpropanoic
2021-10-29
In summary, the SAR of a series of phenylpropanoic acid-free fatty GANT 58 receptor receptor agonists is described which resulted in the identification of potent FFA4 agonists. The superior pharmacokinetic properties of compound led to its selection as an in vivo tool compound which afforded robus
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This SAR work led to the identification
2021-10-29
This SAR work led to the identification of compound 10r ((±)-2-[3-fluoro-4-[3-(hexylcarbamoyloxy)phenyl]phenyl]propanoic acid, ARN2508) [51] as a potent in vivo active inhibitor of intracellular FAAH and COX activities, which exerts profound anti-inflammatory effects in mouse models of IBD without c
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Microglia after activation can show prominently pro inflamma
2021-10-29
Microglia after activation can show prominently pro-inflammatory but also anti-inflammatory characteristics [46]. Although the ageing process is not a pathological process, many of the age-associated changes resemble those observed under pathological conditions. An increase number of pro-inflammator
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br Conclusion In this report we describe the
2021-10-28
Conclusion In this report, we describe the synthesis and evaluation of oxadiazole-based GSK3 inhibitors. Occupation of the ATP-binding pocket in its entirety led to the identification of several potent and selective compounds. These compounds are characterized by IC50 values in the low nanomolar
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br Lysophosphatidylinositol LPI LPI is
2021-10-28
Lysophosphatidylinositol (LPI) LPI is a subspecies of lysophospholipid consisting of inositol as its head group, one glycerol molecule and one acyl chain (Piñeiro and Falasca, 2012). The biosynthesis of this lipid starts from Phosphatidylinositol (PI) and is catalysed by the enzymes phospholipase
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In addition analysis of the functional elements in the
2021-10-28
In addition, analysis of the functional elements in the GnRH promoter region also identified other transcription factor binding sites, such as those for GATA-1 and Oct-1. However, those sites were not further validated in this study. Nevertheless, it has been reported that transcription factors such
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To investigate if such an effect is observed
2021-10-28
To investigate if such an effect is observed in native GlyT1, we introduced S605D and S605A mutations into GlyT1 and transfected these DNA constructs into N2a cells. For an internal control of calpain cleavage, we also introduced the first 100 amino-acids of the rat GlyT2N terminus upstream of the m
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