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To further investigate if GPR was the
2022-03-21

To further investigate if GPR40 was the functional target of these phenylpropiolic Clozapine 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
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ICH induced striatal lesion produced a
2022-03-21

ICH-induced striatal lesion produced a reduction of EAAT1 expression analogous to the decreased glutamate uptake at 6 h. The combined reduction of excitatory amino lysophospholipid receptor transporters and of glutamate uptake activity might explain the well-known glutamate excitotoxicity following
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jnk inhibitor Here we reported series of carbohydrate modifi
2022-03-21

Here, we reported series of carbohydrate-modified compounds containing a dibromo substituted benzene ring which was derived from the red alga (). The conformation flexibility of jnk inhibitor and their polyol structures give them many unique biological properties as we have described earlier. More i
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Semaxanib synthesis Rifampicin that is methyl piperazinyl im
2022-03-21

Rifampicin, that is 3-[[(4-methyl-1-piperazinyl) imino] methyl]-rifamycin (Fig. 1), is a semisynthetic antibiotic drug. It is one of the most potent and broad drug against bacterial pathogens and tuberculosis [9]. In recent years, rifampicin has also been reported to have inhibitory effects on Taq R
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Bedaquiline It is important to underline that although ghrel
2022-03-21

It is important to underline that Bedaquiline although ghrelin increases the motivation to eat even in fed state, its effects on food intake and reward are blunted in obese animal models (Zigman et al., 2016). This emphasizes also the interconnection between homeostatic regulation of food intake an
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One major issue has dominated studies of the nematode connec
2022-03-21

One major issue has dominated studies of the nematode connectome: its reproducibility. The difficulties that had to be surmounted just to assemble a complete wiring diagram precluded comparisons of the complete wiring from several different animals. Instead the earliest adult hermaphrodite wiring di
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FPR ligands comprise structurally very diverse classes of co
2022-03-21

FPR ligands comprise structurally very diverse Oltipraz 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, pyridazine
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All models used here rely
2022-03-21

All models used here rely on WT FGFR3, which is activated by exogenous FGF ligand to alter chondrocyte proliferation and differentiation. This approach toward modeling the aberrant FGFR signaling in cartilage differs from the actual situation in ACH or TD, where the chondrocytes are exposed to long-
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A large body of literature have reported that various cellul
2022-03-18

A large body of literature have reported that various cellular pathways are dysregulated in NPC [19]. Among these pathways, Akt is frequently hyperactivated in NPC and regulates diverse cellular processes including tumor cell growth, proliferation, metabolism, survival and invasion, as well as angio
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Tourette s syndrome TS is a
2022-03-18

Tourette's syndrome (TS) is a neurobehavioral disorder characterized by chronic motor and vocal tics. The histaminergic system appears to be implicated in the pathophysiology of TS because H3R up-regulation has been observed in the striatum of HDC knock-out animal models (Rapanelli et al., 2017; Rap
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VU 0155069 mg We demonstrated that bilirubin the product of
2022-03-18

We demonstrated that bilirubin, the product of heme metabolism by HO-1, exerted a potent suppression of NADPH oxidase activity (Fig. 2B). Different from the down-regulation of NADPH oxidase subunit by HO-1 induction in macrophages [24], the protein levels of the NADPH oxidase subunits in vascular en
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ICLs represent of all generated DNA
2022-03-18

ICLs represent ICL Inducers in Cancer Therapy Nitrogen mustards with aromatic substituents (chlorambucil, melphalan) or a bioactivatable phosphoramide group (cyclophosphamide) were one of the first identified DNA crosslinkers. These agents are still used in combined schemes for the therapy of chr
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br Substrate Interactions Outside of the Catalytic Cleft As
2022-03-18

Substrate Interactions Outside of the Catalytic Cleft As for other types of protein–protein interactions, kinase–substrate docking interactions can occur through large binding interfaces or through recognition of short linear sequence motifs. For kinases with a large number of substrates, the use
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Multiple studies from our laboratory and others which have u
2022-03-18

Multiple studies from our laboratory and others, which have used stoichiometric kinetic analyses of ANP/NPRA, have provided strong evidence that bound ligand-receptor complexes are internalized and processed intracellularly, and that degraded products are released into the culture medium of various
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br Acknowledgements br Funding This work
2022-03-18

Acknowledgements Funding: This work was supported by the Instituto Nacional de Biomedicina do Semiárido (INCT-IBISAB-CNPq), Edital MCT/CNPq N° 014/2010 - Universal and Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES). Introduction Guanylin and uroguanylin are small, heat-
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