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It is important to underline that although
2021-10-21

It is important to underline that PCP inhibitor although ghrelin increases the motivation to eat even in fed state, its effects on food intake and reward are blunted in obese animal models (Zigman et al., 2016). This emphasizes also the interconnection between homeostatic regulation of food intake
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The pharmacokinetic properties of were amenable to oral
2021-10-21

The pharmacokinetic properties of 12 were amenable to oral dosing allowing in vivo comparison to 6. Compared to a maximum efficacious dose of 6 (60mg/kg), 12 demonstrated improved glycemic control during OGTT in high-fat fed/STZ treated (HF/STZ) and BDF/diet-induced obesity (DIO) mouse models of typ
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Tetrazole is one of the most commonly used
2021-10-21

1-Tetrazole is one of the most commonly used bioisosteres for carboxylic acids arising from their similarity in pKa (ca. 4.5–4.9 vs 4.2–4.4, respectively)., Metabolically, tetrazoles may exhibit an advantage over carboxylic acids because they form -glucuronides which are not as chemically reactive
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br Materials and methods br
2021-10-21

Materials and methods Results Estimations of OMP generated by the proposed mechanism (Fig. 1) were first performed for the range of 0.001–2 mM of c-Myc tag concentration in the cytosol. It was assumed that only 5% of all VDACs in MOM form the ANT-VDAC1-HKI contact sites, and that the fraction
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The occurrence of naturally HCV NS resistance associated sub
2021-10-21

The occurrence of naturally HCV NS3 resistance-associated substitutions (RAS) affects virological outcome of DAA-based combination therapies [14], [15], [16], [17], [18], [19]. For the majority of NS3 protease inhibitors the frequency of natural occurrence of single RASs in HCV genotype 1-infected p
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Background Chronic hepatitis C virus HCV
2021-10-21

Background Chronic hepatitis C virus (HCV) infection is a major public health concern, with 71 million people infected worldwide [1]. Treatment options have improved with the availability of interferon-free direct-acting antiviral (DAA) therapies with cure in >95% of people [2]. However, broadening
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Over the last years numerous
2021-10-21

Over the last 15 years, numerous studies gave insights into sGC activation and binding of activators: Photoaffinity labelling studies with cinaciguat suggested the N-terminus of the β1 subunit as target region for this new drug [17]. Schmidt et al. identified the amino acids tyrosine 135, serine 137
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In human platelets only and isoforms of sGC
2021-10-20

In human platelets, only α1 and β1 isoforms of sGC are expressed in equimolar concentrations (3700 copies for β1, and 3500 copies for α1 per platelet) [57] [62]. sGC, is usually a heterodimer and contains heme as cofactor which is required for high-affinity NO binding and stimulation of its activity
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As GSH cellular redox status is critical
2021-10-20

As GSH cellular redox status is critical for various biological phenomena including apoptosis and inflammation [34], [35] we hypothesized that inflammation could modulate GSTP1-1 gene expression. Indeed, reactive oxygen species (ROS) are released at inflammation sites and can be eliminated from drop
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Foreign polypeptide antigens can be incorporated into VLPs t
2021-10-20

Foreign polypeptide antigens can be incorporated into VLPs to create “chimeric” structures, either as fusions to either end of the VLP capsid (coat) protein (CP) or as additions to well-presented loops [18]. This kind of direct fusion to the coat is usually good for small peptides, however, larger p
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br Short Communication Free fatty acid receptors
2021-10-20

Short Communication Free fatty DMH-1 receptors (FFAR) play significant roles in energy metabolism (Brown et al., 2005; Ichimura et al., 2009). The receptor FFAR1 is involved in insulin secretion in humans (Meidute Abaraviciene et al., 2013). Activation of the receptor FFAR2 increases lipid accret
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br Role of FPRs in regulating the
2021-10-20

Role of FPRs in regulating the inflammatory response Annexin I is a glucocorticoid-regulated protein possessing both pro- and anti-inflammatory activity that might be mediated, in part, by FPR activation [35]. Expressed in a variety of cell types, annexin I is particularly abundant in neutrophils
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FBP ALDOA complex is located on both sides
2021-10-20

FBP2-ALDOA complex is located on both sides of Z-line in striated muscles (Rakus et al., 2003a; Gizak et al., 2003) and its stability is regulated by calcium ions (Mamczur et al., 2005; Rakus et al., 2013) (Fig. 3). An increasing titre of [Ca2+] which occurs during muscle contraction stimulates diss
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PIK-III br Challenges and open questions Deepening our
2021-10-20

Challenges and open questions Deepening our understanding of PKC’s role in GSIS will require harnessing recently developed techniques and developing new tools. Here we describe three challenges remaining in the field and offer suggestions on experimental approaches to address them. PKC plays an
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Septic shock a condition where endothelium derived substance
2021-10-20

Septic shock, a condition where endothelium-derived substances most likely play an important role, is often accompanied by cardiac dysfunction, pulmonary hypertension, systemic hypotension and impaired oxygen utilisation with systemic acidosis (Vincent, 1998). Experimental endotoxaemia shows a simil
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