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The dopamine substrate currents IDA
2022-03-09

The dopamine substrate currents (IDA – IControl) were determined at different holding potentials (IV curves) in transfected HT22 cells (Fig. 5A). The plot for HT22 cells transfected with DAT exhibited the typical behavior of dopamine transporter currents (Ingram et al., 2002; Sonders et al., 1997),
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br Materials and methods br
2022-03-09

Materials and methods Results Discussion The glucose transporter GLUT1 can be acutely activated or inhibited in L929 fibroblast 1,2-Dimyristoyl-sn-glycerol by a wide variety of reagents or nutrient conditions [[9], [10], [11], [12],36,50]. This abrupt change in the activity of GLUT1 occurs
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Next we focused on B part the phthalazine ring
2022-03-09

Next, we focused on B-part, the phthalazine ring. While both nitrogen atoms of the phthalazine ring were found to be important (data not shown), replacing the benzene ring of the phthalazine part was attempted, and shows the results of the substituted pyridazine rings with bearing 2-methoxy benzene
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GCK MODY is the most common form
2022-03-09

GCK-MODY is the most common form of MODY diabetes in many populations (Chevre et al., 1998; Massa et al., 2001; Barrio et al., 2002; Estalella et al., 2007; Pruhova et al., 2010; Capuano et al., 2012; Giuffrida et al., 2017). However, data about GCK-MODY among North African populations are very rare
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It is notable that pharmacological
2022-03-09

It is notable that pharmacological or genetic inhibition of GCGR signaling results in the engagement of a number of compensatory mechanisms that potentially impact glucose control. These include alpha-cell hyperplasia [2], [11], [12], [13] and increased beta-cell proliferation under low insulin cond
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Another consistent observation in our studies was the lower
2022-03-09

Another consistent observation in our studies was the lower plasma catecholamine concentrations in the exercised GHSR-null mice, suggesting a diminished sympathoadrenal response. A proper sympathoadrenal response is essential for increasing substrate utilization during exercise [81]. Thus, the reduc
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br Secretase modulators a loss of pharmacology A lack of
2022-03-09

γ-Secretase modulators: a loss of pharmacology? A lack of translation from in vitro to in vivo pharmacology is an unresolved issue among most GSMs. R-flurbiprofen was tested in clinical trials, however, it did not achieve statistical significance on either of its primary endpoints – cognition or
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In fish little information about
2022-03-09

In fish, little information about Gpr84 is available. We have revealed that lipopolysaccharide (LPS) induces significantly up-regulation of zebrafish , and zebrafish overexpression markedly increased the LPS-stimulated production of the cytokine []. Here we expanded on these studies to further inv
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This SAR work led to the identification of compound
2022-03-09

This SAR work led to the identification of compound 10r ((±)-2-[3-fluoro-4-[3-(hexylcarbamoyloxy)phenyl]phenyl]propanoic acid, ARN2508) [51] as a potent in vivo active inhibitor of intracellular FAAH and COX activities, which exerts profound anti-inflammatory effects in mouse models of IBD without c
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br Prostaglandins meet Hippo The prostaglandins lie
2022-03-08

Prostaglandins meet Hippo The prostaglandins lie at the crossroads between inflammation, regeneration and tumorigenesis (Figure 3). Prostaglandins are synthesized from archidonic dan shen by Cox1 and Cox2 enzymes [40, 41] and in the gut, prostaglandin E2 (PGE2) protects against DSS-induced colit
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br Conclusion br Author contributions br Ethics
2022-03-08

Conclusion Author contributions Ethics approval Competing interests Introduction VHL is a well-known tumor suppressor and works as a target recruitment subunit of an E3 ubiquitin ligase complex that recruits hydroxylated hypoxia inducible factor α (HIF-α) for proteasomal degradation u
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The rationale for developing HDACi
2022-03-08

The rationale for developing HDACi as anticancer agents was based on their ability to induce the hyperacetylation of histones and nonhistone proteins, resulting in increased differentiation, apoptosis, and Adox arrest of cancer cells 1, 2, 3. HDACi have been used in the treatment of hematological m
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The inhibitory concentration of atrial
2022-03-08

The 50% inhibitory concentration of atrial natriuretic factor at midgestation and term are –7.4 ± 0.12 and –7.38 ± 0.11, respectively, demonstrating no gestational age dependency in the effect of atrial natriuretic factor on spontaneous contractile activity. Diethyl amine/nitric oxide starts to inh
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NCT-503 CgtA is involved in stringent response and it
2022-03-08

CgtA is involved in stringent response and it interacts with SpoT to maintain optimal (p)ppGpp/ppGpp quotient in bacteria. Depletion of CgtA results in increased ppGpp levels [8]. CgtA is also important for cellular development [12] and involved in synchronization of DNA replication initiation and c
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It has been proposed that HCA may be
2022-03-08

It has been proposed that HCA1 may be a better target than HCA2 to treat dyslipidemia and to prevent progression of atherosclerosis, because HCA1 is less widely expressed, and HCA1 activation does not result in flushing. However, since the antilipolytic effects mediated by HCA2 appear to be not the
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