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Ligand selectivity may directly be related to the conformati
2022-03-16

Ligand selectivity may directly be related to the conformational landscape explored by GPCRs despite that most GPCRs do not require dimerization for ligand recognition (Mary et al., 2012). Monomer FPRs have traditionally been perceived as receptors that can recognize N-formyl peptides and LXA4. This
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The physicochemical properties of the prodrugs provided impo
2022-03-15

The physicochemical properties of the prodrugs provided important clues for understanding a broad range of inhibitory activities in the cell assays (Table 2). Some physicochemical properties are useful in predicting drug absorption. Considering Lipinski’s rules and the polar surface area (PSA),l-ala
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Over the years a number of studies
2022-03-15

Over the years, a number of studies have reported results concerning the behavior of the two endothelin receptor subtypes, ETA and ETB, that do not fit the classical model of two G protein-coupled receptors acting independently of one another. For example, in the rat anterior pituitary gland, both E
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Surface enhanced Raman spectroscopy SERS
2022-03-15

Surface-enhanced Raman spectroscopy (SERS) is one of the most powerful and ultra-sensitive analytical tools, which has been widely applied to food security analysis and many other fields (Craig, Franca, & Irudayaraj, 2013; Gukowsky, Xie, Gao, Qu, & He, 2018; Qi et al., 2013; Zhang et al., 2015). For
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All these recent results show the
2022-03-15

All these recent results show the interconnection between the Hippo pathway as a tumor-suppressor on the one hand and its function as regulator of metabolic homeostasis on the other. Disruption of the Hippo pathway leads to cancer growth, which is often associated with pathological disturbances in t
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The study by Pigna and collaborators
2022-03-15

The study by Pigna and collaborators provides an elegant demonstration why class IIa HDAC inhibition may not be suitable to protect the neuromuscular function in ALS, consistent with a recent study that showed only a transient protection of motor performance after treatment of the same ALS model wit
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br Acknowledgements This work was supported by
2022-03-15

Acknowledgements This work was supported by a grant from the BBSRC (BB/D011809/1) to GJL and The Royal Society to SHS (Uf090321). SIM and AH were the recipients of scholarships from HEC Pakistan. Introduction Iron (Fe) is the fourth most abundant element in the earth’s crust. However, Fe is o
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Fibronectin protein level was not
2022-03-15

Fibronectin protein level was not affected by DIF-1, although fibronectin has also been considered a canonical Wnt signaling pathway target gene product [39]. Thus, the canonical Wnt signaling pathway may not be critical for the regulation of the expression of fibronectin in malignant melanoma cells
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In this study we describe the role
2022-03-15

In this study, we describe the role of a specific species of LPI in the secretion of GLP-1 from enteroendocrine L-cells and primary cell preparations. We further demonstrate the specific role of GPR119 in LPI-dependent GLP-1 secretion. To achieve this, we downregulated GPR119 and GPR55 protein expre
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With an ever increasing incidence
2022-03-15

With an ever-increasing incidence rate of type 2 diabetes and obesity, it is imperative to develop new therapeutic regimes that may provide a benefit both in terms of efficacy and tolerability. The existing portfolio of drugs for the treatment of metabolic disorders, primarily type 2 diabetes and ob
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br Funding This work was supported by the Deutsche
2022-03-14

Funding This work was supported by the Deutsche Forschungsgemeinschaft (SFB766 and GRK1708). Conflict of interest Acknowledgements Introduction Hepatitis C virus (HCV) infection is a global problem affecting about 3% of the world’s population [1], [2]. Mother-to-child transmission of HC
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NF 449 In order to facilitate the preparation of
2022-03-14

In order to facilitate the preparation of 2-aminothiazoles containing novel D-ring substitutions, a convergent synthetic route was selected which requires the synthesis of common precursor . Straightforward aromatic substitution of 3,4-difluoroacetophenone using 4-methylimidazole provided access to
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Psoriasis is an inflammatory skin disease characterized by
2022-03-14

Psoriasis is an inflammatory skin disease characterized by epidermal hyperplasia; micro-abscesses; neo-angiogenesis; a proinflammatory cytokine environment involving alterations of IL-17A, IL-23, and TNF-α; and activation of and infiltration by macrophages, mast cells, neutrophils, CD11c+ dendritic
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Studies on FXR knockout mice demonstrated that FXR activity
2022-03-14

Studies on FXR knockout mice demonstrated that FXR activity is necessary to maintain a proper integrity of intestinal tight junction [18]. HF diet-induced bowel dysfunction impaired FXR activity and affected fecal BA profile. Generally, it augmented the concentration of secondary BAs in the colon e.
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Fpr which belongs the family of
2022-03-14

Fpr1, which belongs the family of the formyl peptide receptors with FPRL1 and FPRL2, is the principal receptor for formylated peptides which prototype is the tri-peptide fMLF. Fpr1 is highly expressed on neutrophils and macrophages [6,30], promotes their migration into the mucosa and lumen in respon
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