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Apart from the different assays used biased agonism could al
2021-11-06
Apart from the different assays used, biased agonism could also explain the inconsistent pharmacology of GPR55. Indeed, one study compared the effect of LPIs and Virodhamine in HEK293 ID-8 stably transfected with human GPR55. They found that the effect of both ligands on intracellular Ca2+ was bloc
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br Results br Discussion Cell contact
2021-11-06
Results Discussion Cell-contact-mediated spread of HIV-1 has been estimated to be at least an order of magnitude more efficient compared to passive dissemination of particles through the extracellular milieu. Thus, this form of viral transmission can have significant effects on the pathogenesi
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br Introduction The generic antifibrinolytic
2021-11-06
Introduction The generic antifibrinolytic drug tranexamic bupropion hydrochloride (TXA) inhibits the protein-protein interaction between plasminogen and fibrin [9]. TXA is frequently used to reduce bleeding in various hemorrhagic conditions, such as during surgical procedures in the heart [19].
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GPR can signal through not
2021-11-06
GPR40 can signal through not only IP3 but also cAMP depending upon the type of agonist ligand used. A full agonist engages both signaling mechanisms in contrast to the endogenous long-chain fatty PKC412 (LCFA) ligands and partial agonists. Thus, stimulation of GPR40 by endogenous LCFAs or by the sy
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Isochlorogenic acid A receptor In a previous study M ykkynen
2021-11-06
In a previous study (Möykkynen et al., 2003), we reported that ethanol lengthens the time needed for the AMPA receptors to recovery from desensitization in isolated hippocampal neurons. Here, we did not observe any effect of ethanol on recovery from desensitization in recombinant homomeric GluR-D re
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Here we examined whether complete ablation of
2021-11-06
Here, we examined whether complete ablation of GIP production could reduce weight gain in the absence of the adipocyte hormone leptin, a condition that results in extreme hyperphagia, obesity, hyperinsulinemia, and insulin resistance, in both mice [24] and humans [25]. We found that Lepob/ob mice be
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Until now various reports have demonstrated the
2021-11-06
Until now, various reports have demonstrated the therapeutic potential of enzyme-resistant forms of GIP in experimental diabetic animal models , , . In essence, structural modifications performed at the Tyr residue in GIP generate analogues that are completely resistant to the actions of DPP-IV and
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Subsequently we decided to test whether the orexin
2021-11-06
Subsequently, we decided to test whether the orexin pathway was involved (Delhanty et al, 2012, Delhanty et al, 2013, Pei et al, 2014). Orexin neuronal systems are known to control limbic and neocortical structures (Bonnavion, de Lecea, 2010, Sakurai, 2007). Orexin receptors and possibly orexin synt
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Cx is the major molecule involved in the dynamic
2021-11-06
Cx43 is the major molecule involved in the dynamic life cycle of GJIC (Cusato et al., 2006). Initially generated Cx43 exist in the cytoplasm and correctly transfer it to the plasma membrane during its life cycle (Ji et al., 2018). To understand the toxic effects of MC-LR on GJIC, Cx43 localization w
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1,4-DPCA Natural products are a diverse
2021-11-06
Natural products are a diverse and interesting source for the discovery of new lead structures (Newman and Cragg, 2016). After a successful era of natural product research, many pharmaceutical companies stopped their investment in natural product-driven drug discovery in the 1990s. The reason behind
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nitric oxide synthase inhibitors All models used here rely o
2021-11-06
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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Data are expressed as means SE Statistical significance was
2021-11-06
Data are expressed as means±SE. Statistical significance was determined by the Student's -test or ANOVA with post hoc Bonferroni test. A value of U87MG pde-5 inhibitors expressing human FPPS. Western blot analysis showed a clear band, which indicated the overexpression of FPPS, in U87MG cells (A, in
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3-AP br Declarations of interest br Founding information Thi
2021-11-06
Declarations of interest Founding information This work was partially supported by the New Energy and Industrial Technology Development Organization (NEDO) Japan [grant number P03043]; and Grants-in-Aid for Scientific Research [grant number 16H00738 to H.M.] from the Japan Society for the Prom
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In an effort to more fully
2021-11-06
In an effort to more fully explore the structure–activity relationships of the ALLINIs and potentially attenuate resistance to known mutants, the central scaffold of these compounds was identified as a potential site for structural manipulation. Specifically, we wished to examine whether a scaffold
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One limitation of our study was that
2021-11-06
One limitation of our study was that all control dogs had histologic evidence of mild GI inflammation according to established WSAVA guidelines (Washabau et al., 2010), despite being apparently healthy purpose-bred research dogs housed in a controlled environment with no history of vomiting, diarrhe
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