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Formyl peptide receptors FPRs are a family of surface
2021-11-26
Formyl peptide receptors (FPRs) are a family of surface-expressed, G protein-coupled receptors [7]. The three members, FPR1, FPR2 and FPR3, share significant sequence homology, but have different functional properties [7]. While FPRs are mainly expressed by innate leukocytes, they are also found on
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5-Methoxy-UTP Due to the presence of all FGFRs in the epithe
2021-11-26
Due to the presence of all FGFRs in the epithelium, there are several FGFs ligands that could be binding to these FGF receptors, namely FGFs 1–4, 8–10, 16 and 18–20. By evaluating the known roles of FGFs in epithelial-mesenchymal interactions and in bone development, this list can be reduced. For ex
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However at variance with the well studied R
2021-11-26
However, at variance with the well-studied R form of FBP1 which is flat, the R state of FBP2 is diametrically different, with a perpendicular orientation of the upper and lower dimers (Barciszewski et al., 2016). The cruciform-like R state of FBP2 is stabilized by a unique hydrophobic motif called ‘
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Factor Xa FXa has emerged as a particularly promising
2021-11-26
Factor Xa (FXa) has emerged as a particularly promising target for the development of effective anticoagulant drugs because FXa acts at the convergence point of the extrinsic and intrinsic coagulation pathways. It efficiently catalyzes the conversion of prothrombin to thrombin with one molecule of F
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Our observation of LPS induced
2021-11-26
Our observation of LPS-induced increase in the sensitivity of cultured endothelium-intact coronary glucagon receptor antagonist towards stimulation with selective ETB receptor agonist (S6c) could be explained by activation of TLRs receptors located on the endothelium of rat coronary arteries. Howeve
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At baseline Hdc KO mice have alterations in the
2021-11-26
At baseline, Hdc-KO mice have alterations in the examined signaling cascades that resemble those seen in WT mice after RAMH challenge. Specifically, Scrambled 10Panx receptor of MSK1 at T581 and of rpS6 ad S235/236 are elevated in dMSNs to a similar extent after saline in KO mice and after RAMH cha
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br Structural studies of GCAP Recoverin was the first
2021-11-26
Structural studies of GCAP Recoverin was the first member of this subfamily of Ca2+-binding Estradiol sale to be investigated by structural methods [27], [54], [55], [56], [57], [58]. These proteins have four EF-hands arranged in pairs that give rise to amino- and carboxyl-terminal domains. The
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br Results br Discussion We have reported
2021-11-25
Results Discussion We have reported the crystal structures of VcmN, the high-resolution structures of this MATE transporter from a pathogenic bacterium. The structures display distinct conformations of TM1, as a consequence of their unique hydrogen-bonding networks. We interpret this result to
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br Xenobiotics and the Glucocorticoid
2021-11-25
Xenobiotics and the Glucocorticoid Receptor Conclusion Transparency document Acknowledgements The author wishes to thank Professor Wilhelm Engström from the Swedish University of Agricultural Sciences (Department of Biomedical Sciences and Veterinary Public Health) for his proof reading
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br Materials and methods br Results br
2021-11-25
Materials and methods Results Discussion Our study demonstrates that human GIP(3-30)NH2 is a selective GIPR antagonist that inhibits both GIP-mediated cAMP signaling, β-arrestin recruitment, and GIPR internalization. Furthermore, we demonstrate that human GIP(3-30)NH2 binds with high affini
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Many natural flavonoids have been identified
2021-11-25
Many natural flavonoids have been identified as influencing ionotropic GABA receptors through bioassay-guided fractionation of plant extracts (Fig. 4). HPLC-based activity profiling of extracts the traditional Chinese herbal drug Kushen (Sophora flavescens root) led to the identification of the 8-la
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Much is known about FPPS
2021-11-25
Much is known about FPPS structure and function, with over 120 FPPS crystal structures being currently available. This wealth of information is largely the consequence of human FPPS serving as a drug target for the treatment and/or prevention of pathologies such as osteoporosis, hypercalcemia and Pa
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As concerns TRPV assays benzylic
2021-11-25
As concerns TRPV1 assays, benzylic amides and benzylic reverse amides exhibited an overall superiority over their aryl counterparts and , and ureas and . A reversed trend was however observed with the 4-chlorostyryl and 4--butylphenyl moieties (compare compounds and ; , , and ; and ). The EC a
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It has been shown that mice
2021-11-25
It has been shown that mice lacking SMAD2 in T cells do not develop spontaneous lymphoproliferative autoimmunity (Malhotra et al., 2010). Further, FOXO1 is known to activate proinflammatory MCP-1 and IL-6 (Ito et al., 2009). To this end, we also validated the downstream target FOXO1 and SMAD2 after
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Some SNPs have been identified for HRH in
2021-11-25
Some SNPs have been identified for HRH in cancer (Table 4). Looking into breast cancer research, H4 receptor polymorphisms have been recently associated with the malignancy of the disease. This was evidenced upon the analysis of genotypes and haplotypes of a Chinese Han population; this study showed
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