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Recently several groups reported that four orphan receptors
2022-10-04

Recently, several groups reported that four orphan receptors, GPR40, GPR41, GPR43, and GPR120, can be activated by free fatty acids. Short-chain fatty acids are specific agonists for GPR41 and GPR43 . Medium and long-chain fatty acids can activate GPR40 and GPR120 . Our previous report showed that
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The study of TcMYH protein is a step
2022-10-04

The study of TcMYH protein is a step forward for the characterization of a GO system in T. cruzi. The complete system appears to be present and our findings demonstrate that is important to maintain DNA stability of the nuclear and mitochondrial genomes, particularly in the presence of oxidative str
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Although we showed that RBL H
2022-10-04

Although we showed that RBL-2H3 Sc98 TAK-901 australia took up histamine from the microenvironment, it was unclear which transporter mediated its passage across the plasma membrane. Other biogenic amines have selective transporters that belong to the neurotransmitter sodium symporter family, includi
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In this study for the
2022-10-04

In this study, for the first time: 1) the electrochemical glutamate oxidase-based biosensor was optimized for the determination of low micromolar glutamate concentrations; 2) the algorithm of the analysis of exocytotic and transporter–mediated glutamate release was developed; 3) the comparative anal
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br Conclusion In summary a series of novel GPR
2022-10-04

Conclusion In summary, a series of novel GPR40 agonists bearing phenylpropiolic S63845 receptor motif with favorable metabolic stability were prepared and evaluated for their activities as GPR40 agonists. Among them, compound 9 was identified as a structurally distinct GPR40 agonist possessing p
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In this study we present the synthesis and structure activit
2022-10-04

In this study, we present the synthesis and structure–activity studies of a structurally distinct series possessing high potency and selectivity in HEK cell lines together with a potentially promising overall biopharmacological profile. Focusing on creating sufficient structural dissimilarity with g
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For many plasma membrane receptors including GPCRs their
2022-10-03

For many plasma membrane receptors including GPCRs, their density on the cell-surface is finely controlled by various transcriptional, post-transcriptional and post-translational mechanisms, and is often a determinant of overall receptor function in a cell. To date, the transcriptional regulation an
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The sexual dimorphism in dlGALR a and dlGALR b receptors
2022-10-02

The sexual dimorphism in dlGALR1a and dlGALR1b receptors found in the gonads of adult fish led us to hypothesize that the gene expression difference between female and males might be attributed to the differences in steroid production between female and male gonads. Interestingly we have found that
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N Alkylated quinolinium dyes are the common fluorescence
2022-10-02

N-Alkylated quinolinium dyes are the common fluorescence molecules used in fluorescence sensing and cell imaging because of their attractive optical properties as well as high DNA binding affinities.13, 14, 15, 16, 17, 18, 19, 20 Moreover, the quinolinium moiety usually plays the role of donor in va
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Recently some researchers working in China Pharmaceutical Un
2022-10-02

Recently, some researchers working in China Pharmaceutical University developed novel FFA1 agonists some of which were found to be efficacious in the management of type 2 diabetes and with low toxicity. For instance, Zheng et al. [48] in their in vivo study using experimental animals, reported that
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With the identification of small nonpolar substituents
2022-10-02

With the identification of small nonpolar substituents at R3 of the phenylpropanoic acid ring providing improved activity at FFA4, exploration of the benzyl SAR was undertaken (). Small substituents were well tolerated at both the and positions (–) with the 2-bromo- (), 2-isopropoxy- (), and 3-methy
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FPR ligands comprise structurally very diverse classes of co
2022-10-02

FPR ligands comprise structurally very diverse protoporphyrin ix of compounds, ranging from naturally occurring peptides/proteins or “danger signals” such as PAMPs and DAMPs (see 1.1), respectively, to endogenous lipids and even various synthetic non-peptides, such as benzimidazoles, pyrazolones, p
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Paxilline Recently considerable effort has been
2022-10-02

Recently, considerable effort has been invested in developing FDPS inhibitors based on alternative scaffolds (including nonbisphosphonates) that allow other tissue types and parasite-derived forms of FDPS , to be targeted. There are several limits in analyzing inhibitors of FDPS activity: the most
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Consistent with our result Camacho
2022-10-02

Consistent with our result, Camacho-Barquero and coworkers showed that curcumin reduced phospho-P38 MAPK. P-38 MAPK is a key effector of several downstream factors that eventually modulate the homing of monocytic cells during the onset of intestine inflammation (Camacho-Barquero et al., 2007). Along
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Similar to in vitro data in vivo studies have also
2022-10-02

Similar to in vitro data, in vivo studies have also revealed modulation of TLR4-induced inflammatory responses by AEA. The proposed AEA reuptake inhibitor AM404 has been shown to attenuate TLR4-induced increases in plasma levels of IL-6 and IL-1β, the latter effect mediated by CB1 receptor activatio
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