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The typical pharmacophore for GPR agonists
2021-12-21

The typical pharmacophore for GPR40 agonists contains four parts: head (acid moiety), central (phenyl ring), linker and tail (aromatic carbocyclic or heterocyclic ring) [20]. On the other hand, the chemical features that are required for the PPARγ agonists include hydrogen bond donors and acceptors
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The rapid actions of glucocorticoids range from
2021-12-21

The rapid actions of glucocorticoids range from the production of endocannabinoid as a retrograde messenger [9], to regulation of ion channels [10], [11], to inhibitory effects on immune Plumbagin sale [12], [13], [14]. Many different kinase signaling pathways have been implicated in the rapid actio
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So far several methods have been used
2021-12-21

So far, several methods have been used to monitor the level of GJC and its regulation in astrocytes studied in acute Iloperidone australia slices (see Giaume et al., 2012). This mainly includes approaches based either on electrophysiological properties of gap junction channels or on “dye coupling” e
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The orientation of the immobilized enzyme may affect its
2021-12-21

The orientation of the immobilized enzyme may affect its activity and stability and therefore the final biocatalyst performance. Since proteins present areas more prone to unfolding in their surface or near to it [36], the immobilization through these areas may improve the final biocatalyst stabilit
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Further research should indeed focus on understanding the nu
2021-12-21

Further research should indeed focus on understanding the nutritional value of food and its effect on metabolism, overall activation of metabolic NRs network. Moreover, given the prominent role of microbiota in the modulation of the FXR signalling (Degirolamo et al., 2014), there is enough impetus t
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In addition to the robust intracellular calcium mobilisation
2021-12-21

In addition to the robust intracellular calcium mobilisation, DHA and TUG-891 also induced MMP-9 granules release and superoxide production, supporting a key role of calcium in bovine neutrophil defense responses (Burgos et al., 2011). Pisani et al. (Pisani et al., 2009) described a reduction of bas
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Growing evidence supporting the anti inflammatory
2021-12-21

Growing evidence supporting the anti-inflammatory and tissue-protective effects of FPR antagonists led to the screening of commercial libraries for novel small-molecule FPR antagonists. As result of these screening efforts and/or structure–activity relationship (SAR)-directed design and synthesis, a
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Ning et al showed that LPC appeared to increase
2021-12-21

Ning et al. showed that LPC 18:1 appeared to increase insulin release through both GPR119-dependent and -independent mechanisms (Ning et al., 2008). In our study, we have shown that not only GPR119 but also GPR40 and GPR55 participate in LPC-stimulated insulin secretion (Fig. 4, Fig. 5) and target p
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Fig summarizes the results for M concentration
2021-12-20

Fig. 1 summarizes the results for 500 μM concentration of the drugs. Action of histamine is presented for comparison. Both 1-methylhistamine and Nα-methylhistamine strongly potentiated ASIC1a responses. The concentration-dependence of action of Nα-methylhistamine was measured (Fig. 1B). Fitting by H
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According to previous methods several mobile
2021-12-20

According to previous methods, several mobile phase compositions and gradient programmes were assayed to get the best resolved peaks for HA and MHA [12], [13], [24]. Considering the slightly structural differences of the analytes, a mobile phase consisting in two eluents of different polarity and pH
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Hippo Signaling in Cancer Immunity The Hippo pathway has
2021-12-20

Hippo Signaling in Cancer Immunity The Hippo pathway has evolutionarily conserved roles in limiting the size of organs [1]. It is a kinase cascade regulating transcriptional complexes in response to various upstream signals (Box 1). At the cellular level, the Hippo pathway inhibits cell proliferati
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The Hedgehog signaling pathway HH pathway hereafter is vital
2021-12-20

The Hedgehog signaling pathway (HH pathway hereafter) is vital for development and tissue homeostasis. [4] In recent years, studying the role of the HH pathway in carcinogenesis and cancer stemness has highlighted the HH inhibitors as putative cancer therapeutics [5]. However, clinical application o
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2179 Cux is a cell cycle dependent transcription repressor
2021-12-20

Cux1 is a 2179 dependent transcription repressor that is aberrantly expressed in the Pkd1 null, Pkd1CD, and cpk mouse models of PKD, as well as in human ADPKD cells (Vanden Heuvel et al., 1996; Sharma et al., 2005; Paul et al., 2011; Alcalay et al., 2008). In Pkd1 null mice and in human ADPKD cells
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A series of P P
2021-12-20

A series of P3-P4 ureas were explored first and their anti-NS3 protease activity, antiviral properties in a HCV replicon cell-based assay and PK profiles examined. Installation of a methyl group on the P4 side nitrogen NECA of the urea yielded , a molecule which retained intrinsic potency against t
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The involvement of prostaglandins on
2021-12-20

The involvement of prostaglandins on the effects induced by 1-nitro-2-phenylethane is similarly unlikely because vasorelaxation was not changed by indomethacin [20]. The inhibition of adenylyl cyclase with MDL-12330A [21] or cAMP-dependent protein kinase A with KT-5720 [22] also did not interfere wi
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