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To directly address whether pharmacological attenuation
2022-10-03
To directly address whether pharmacological attenuation of physiological GIP provides therapeutic benefits in obese mice, we pursued a selective long-acting antagonist to complement the work we report on GIPR agonism. We report a GIP analog of sufficient aqueous solubility that employs a shortened N
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The caseins are a family of milk phosphoproteins
2022-10-03
The caseins are a family of milk phosphoproteins whose biological function is to provide supersaturating concentrations of calcium, phosphates, and essential SAR405 to the neonate (Vonderhaar and Ziska, 1989). α- and β-caseins, the most abundant of the milk caseins, are described as calcium sensiti
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NLG919 In a mouse model of hyperhomocysteinemia a
2022-10-03
In a mouse model of hyperhomocysteinemia (a risk factor for the development of vascular dysfunction) it has been shown that myoendothelial communication is enhanced due to increased expression of Cx37 and IK1 NLG919 [], allowing the propagation of endothelial signals to VSMC and thereby decreasing
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As recently reviewed a picture is
2022-10-02
As recently reviewed, a picture is emerging where metabolites through GPCR sensors act as important autocrine and paracrine regulators of basic metabolic mechanisms (Husted et al., 2017). The concept of 20-HETE acting through FFAR1 as an autocrine amplifier of GDIS on β substance p sale together wi
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In summary we have discovered the first examples of
2022-10-02
In summary, we have discovered the first examples of movement of Asp189 upon binding to fXa inhibitors. A series of novel and potent fXa inhibitors with a phenyltriazolinone P moiety were identified. Although the general binding mode compared to our previously-reported fXa inhibitors was maintained,
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It is well established that transcription factors are the
2022-10-02
It is well established that transcription factors are the major key players in regulating the transcriptional state of the targeted gene. 15 TFs were found in the present study, which were predicted to have the binding affinity with the EZH2 promoter region. Out of these, GCF, AP-2 and Sp1 were most
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Recent studies are beginning to explore this complex
2022-10-02
Recent studies are beginning to explore this complex interplay of pathways. For example, intracellular trafficking of poly(lactic-co-glycolic acid)(PLGA) based nanoparticles was studied in detail using 30 different Rab proteins as markers for intracellular transport vesicles (involved in exocytosis,
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Organisms can adapt to increasing
2022-10-01
Organisms can adapt to increasing ROS production by up-regulating antioxidant defences, such as the activities of antioxidant enzymes (Livingstone, 2003). Failure of antioxidant defences to detoxify excess ROS production can lead to significant oxidative damage including enzyme inactivation, protein
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br Introduction Inflammatory bowel diseases IBDs including
2022-10-01
Introduction Inflammatory bowel diseases (IBDs) including Crohn's disease and ulcerative colitis (Baumgart and Sandborn, 2012; Beaugerie et al., 2006) are typically characterized by chronic, progressive, and relapsing inflammation of the intestine. Although the exact pathogenesis of IBD is unknow
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Mongolian gerbils Meriones unguiculatus a social rodent spec
2022-10-01
Mongolian gerbils (Meriones unguiculatus), a social rodent species, are widely distributed in the typical steppe, desert steppe and desert habitats of northern China, Mongolia, and Trans-Baikal region of Russia. In wild, the recorded maximum lifespan (apparent longevity) was 29.5 months for female M
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As discussed above both endogenous
2022-09-30
As discussed above, both endogenous and exogenous lesions can lead to adverse health effects [43]. Damaged nucleobases can block DNA replication which is often lethal to cells [44]. The effectiveness of DNA restoration by DNA glycosylases should be closely monitored to gain an insight of the functio
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Next we investigated the accumulation
2022-09-30
Next, we investigated the accumulation of [3H]-ribavirin in fresh villous fragments of human placenta, which provide a physiologically relevant, well-described and validated model for assessing drug interactions with ENTs [32], [35], [69], [70]. The uptake of [3H]-ribavirin was time-dependent and si
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br Introduction As is now well known
2022-09-30
Introduction As is now well known, obesity is major risk factor for various diseases such as nonalcoholic fatty liver disease, cardiovascular disease, some cancers (McWilliams and Petersen, 2009), type-2 diabetes mellitus (Jakobsen et al., 2007), and hypertension (Aneja et al., 2004), among other
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Asiatic acid The biological actions of ghrelin are mainly du
2022-09-30
The biological actions of ghrelin are mainly due to its interaction with GHSR-1a (Howard et al., 1996). The pharmacological properties of D-Lys3-GHRP-6, a selective antagonist of GHSR-1a, have been extensively studied (Beck et al., 2004, Benso et al., 2007, Sibilia et al., 2006). To study the recept
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NMS-E973 Studies have indicated that formylated
2022-09-30
Studies have indicated that formylated peptides, FPRs, and in particular FPR-1 may be principal conductors in inflammatory processes in sterile-24, 26 and infection-related diseases. FPR-1 and formylated peptides, which are active components of CS, have been involved in smoking-induced lung damage,
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