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Fatty acid amide hydrolase FAAH is a
2022-06-06
Fatty Ketorolac synthesis amide hydrolase (FAAH) is a membrane-bound enzyme which releases arachidonic acid and ethanolamine by breaking amide bond of AEA. It also controls the cellular uptake of AEA, by creating and maintaining an inward concentration gradient leading to AEA-facilitated diffusion
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br Funding The authors disclose the following
2022-06-06
Funding The authors disclose the following support for the research and/or authorship of this article: This work was supported by the Canadian Institutes for Health Research (CIHR). TM is the recipient of a BMS/CTN postdoctoral fellowship and PKQ was funded by a CAHR/CIHR doctoral scholarship. A
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Earlier findings from different cancer entities such
2022-06-06
Earlier findings from different cancer entities such as chronic myeloid leukemia (Yang et al., 2011), B cell chronic lymphocytic leukemia (Jantus Lewintre et al., 2009), prostate cancer (Zhu et al., 2009), epithelial ovarian cancer (Tokunaga et al., 2008), and colon cancer (Mazzoccoli et al., 2016,
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One of the key epithelium derived
2022-06-05
One of the key epithelium-derived factors required to maintain immune tolerance in the intestine is Indian Hedgehog (Ihh). Ihh is secreted exclusively by intestinal epithelial cells, and signals in a paracrine manner to the inhibitory receptor Patched1 (Ptch1) on MK-8931 in the mesenchyme. Binding
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Though studied less extensively than
2022-06-05
Though studied less extensively than in cholangiopathies and fatty liver diseases, the Hh pathway is active in other forms of human liver disease, such as Schistosomiasis[58], [101] and chronic viral hepatitis,[100], [125] as well as in several animal models of liver disease, including drug-induced
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Receptor guanylyl cyclases play essential roles in cardiovas
2022-06-05
Receptor guanylyl cyclases play essential roles in cardiovascular and gastrointestinal (patho-)physiology, reproduction biology, cell proliferation, bone growth and sensory signal transduction and, therefore, are important pharmacological targets. Accordingly, the receptor guanylyl cyclase agonists
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The present studies show that despite the
2022-06-05
The present studies show that, despite the high level of GSTP1-1 achieved in transfected cells, GSTP1-1 expression has no effect on sensitivities to the cytotoxicities of the oxazaphosphorines 4-OH-CP, 4-OOH-CP, and maf in MCF7 Anisomycin (Fig. 4). The failure of GSTP1-1 to augment resistance indica
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Despite the rapid development of synthetic ligands the
2022-06-05
Despite the rapid development of synthetic ligands, the endogenous ligands of GPR109A, GPR109B and GPR81 remained elusive until recently. This is probably the result of their relatively low potencies and their metabolite character (Table 1). Traditionally, agonists of GPCRs were believed to belong t
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Recently an increasing number of studies have highlighted
2022-06-05
Recently, an increasing number of studies have highlighted the crucial role of nociceptive factors produced by microglia under neuropathic pain conditions (Mika et al., 2013; Popiolek-Barczyk and Mika, 2016). iNOS is an important pronociceptive factor that is strictly expressed by microglia/macropha
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In normal tissues the expression patterns of GPR and GPR
2022-06-05
In normal tissues, the expression patterns of GPR120 and GPR40 are not uniform. GPR120 is highly expressed in adipocytes, lung and intestinal tract, while GPR40 is shown to be expressed in pancreatic islet SCH 58261 and intestinal tract [7], [20]. It is considered that the distribution of the GPR120
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Consistent with other studies on
2022-06-05
Consistent with other studies on the metabolic effects of an OM3 enriched diet [26,104,105], irrespective of gender, the lowest glucose levels were seen in the Bob-Cat groups fed OM3 diet. Sexual dimorphism was observed in insulin levels. The highest average levels were in the HFD fed [Tg(CAT)±] mal
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A general synthetic pathway to these tricyclic structures is
2022-06-05
A general synthetic pathway to these tricyclic structures is described in (detailed procedures can be accessed in the patent application WO 2011/014520 A2). Benzylation of the appropriate ketoester using KHMDS, followed by treatment with DMF-dimethyl acetal yielded the racemic (dimethylamino)-methyl
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The action of niacin in upregulating
2022-06-05
The action of niacin in upregulating cAMP is most likely determined by the milieu of adenylyl cyclase isoforms expressed in macrophages that are responsive to GPR109A activation. Several adenylyl cyclase isoforms, namely AC2, AC4 and AC7, are responsive to the stimulatory action of Gβγ G-protein sub
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Moreover the ubiquitous expression of the OTR and GHSR
2022-06-05
Moreover, the ubiquitous ionomycin receptor of the OTR and GHSR was also observed in hippocampal and hypothalamic primary culture, indicating that this expression pattern is likely due to basal activity of these receptors. GPCR trafficking under control conditions has been linked to biased signalli
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br Therapeutic approaches exploiting Cx function
2022-06-05
Therapeutic approaches exploiting Cx43 function Due to their potential role in cancer metastasis, attempts have been made to alter connexin function to inhibit cancer growth. Therapeutic approaches include Cx43 peptide mimetics, Cx43 inhibitors, chemical agents capable of enhancing Cx43 function,
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