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To obviate the mitogenic FGF activity several engineered FGF
2022-06-17

To obviate the mitogenic FGF19 activity, several engineered FGF19 variants have been generated aiming to maintain the metabolic activity excluding the protumorigenic ones. One variant, M70, that differs from wild-type FGF19 by 5-amino acids deletion at the N-terminus and the substitution of 3-amino
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To understand the impact of
2022-06-17

To understand the impact of alterations in Tranilast zinc homeostasis, the role of Zn2+ as a neurotransmitter has to be appreciated. Certain regions of the brain including the neocortex and hippocampus harbour so-called “zincergic” (or “gluzinergic”) neurons, where Zn2+ is co-released with glutamat
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Recently some researchers working in China Pharmaceutical Un
2022-06-17

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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In summary tail vein injection of
2022-06-16

In summary, tail vein injection of mmLDL activated the ERK1/2 signaling pathway, leading to increased serum concentrations and increased vascular wall expression of ICAM-1 and VCAM-1, and may cause increased expression of vascular smooth muscle ETB receptors and the ETB receptor-mediated contractile
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Introduction Histamine Imidazolyl ethylamine is an
2022-06-16

Introduction Histamine [2-(4-Imidazolyl)-ethylamine] is an important mediator of many physiological and pathological processes including inflammation, gastric Cy5 Firefly secretion, neuromodulation, regulation of immune function, cell proliferation and differentiation, among others. Histamine exer
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In the Hedgehog signaling pathway cholesterol is
2022-06-16

In the Hedgehog signaling pathway, cholesterol is required to activate SMO (Cooper et al., 2003), the downstream target of PTCH1. A previous study (Bidet et al., 2011) reported that Patched expression in yeast SKF 86002 dihydrochloride increased extrusion of a fluorescent boron dipyromethanene stero
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br Competing interests br Funding br
2022-06-16

Competing interests Funding Ethical approval Acknowledgement Introduction Hepatitis C is a disease that infects the liver through transmission of the hepatitis C virus (HCV). Because the symptoms of this infection are not pronounced, the infected individuals may not even be aware of t
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For some agonists these stable GPR responses were resistant
2022-06-16

For some agonists, these stable GPR119 responses were resistant to washing. Thus, sustained activation could continue, for at least a number of hours, even after removal of free agonist. These data are consistent with reports for other GPCR systems that do not desensitize (Calebiro et al., 2009, Fer
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Phentolamine Mesylate Activation of FXR or TGR inhibits infl
2022-06-15

Activation of FXR or TGR5 inhibits inflammatory response via repressing NF-κB activity [1]. FXR is not expressed or expressed at a very low level in macrophages [45] (data not shown), but highly expressed in hepatocytes. In contrast, TGR5 is expressed in macrophages but not in hepatocytes. Our data
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br Acknowledgements This work was
2022-06-15

Acknowledgements This work was in part supported by the FöFoLe program by Ludwig-Maximilians-Universität München (to T.S.), the Deutsche Forschungsgemeinschaft (DFG) CO 291/5-2, the Human Frontier Science Program (HFSP) RGP0013, the Helmholtz Validation Funds (Helmholtz Association of German Rese
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br Discussion The initial reduction and the subsequent incre
2022-06-15

Discussion The initial reduction and the subsequent increase in permeability proposes a regulatory process to control bleeding. However, following repeated injury, or during long-term presence of the inflammatory stimuli, these mechanisms may become defective and even detrimental. The expression
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In human cancers it has
2022-06-15

In human cancers, it has been identified that FOXC2-AS1 functions as an oncogenic RNA. For instance, in osteosarcoma, FOXC2-AS1 regulates the expression of FOXC2 at the transcription and post-transcription levels to promote doxorubicin resistance by facilitating ABCB1 expression (C.L. Zhang et al.,
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In neurons and neuroendocrine cells the productive fusion pa
2022-06-15

In neurons and neuroendocrine cells, the productive fusion pathway is thought to initiate with the Munc18-1/Syx1 complex (Ma et al., 2013, Hughson, 2013, Lai et al., 2017). The Munc13-1 MUN domain is able to catalyze opening of Syx1 (the transition from the Munc18-1/Syx1 complex to the SNARE complex
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It is apparent from the data
2022-06-15

It is apparent from the data in that none of the ligands exhibits significant toxicity as determined by the viability of human embryonic kidney (HEK 293) cells at a concentration of 100 μM. It is also apparent from the data in and that a number of the ligands inhibit the HIV-1 IN enzyme. However,
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br Materials and methods br
2022-06-15

Materials and methods Results Discussion The major findings of the present study are that: 1) the response to inverse agonists may be crossregulated by the activation of either YC 1 H1 or H2 receptors, 2) histamine H1 and H2 receptor inverse agonists crossdesensitize the receptor´s response
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