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Retinal GAL receptor distribution suggests an intrinsic neur
2021-11-06
Retinal GAL receptor distribution suggests an intrinsic neuronal control since retina lacks an autonomic innervation, and a signal modulation seems most likely here, acting via GALR1 while GALR2 and GALR3 seem to play a rather minor role in this signal transduction. While sources acting on these ret
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lck inhibitor br Role of FPRs in Cancer br Concluding
2021-11-06
Role of FPRs in Cancer Concluding Remarks Activation of FPRs by formylated bacterial peptides or by host-derived mitochondrial peptides is required for local control of infection and wound healing. Nevertheless, various detrimental effects can result from the release of formylated peptides int
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BMN673 Following the discovery of diketo compounds S and L
2021-11-06
Following the discovery of β-diketo compounds S-1360 [31] and L-731988 [32] as anti-HIV integrase inhibitors, a group of researchers discovered a potent BMN673 based derivative (1) as the inhibitor of HIV integrase functioning at the 3′-processing and strand transfer steps of HIV integrase. Bioassa
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A biochemical characterisation of this
2021-11-06
A biochemical characterisation of this functionally crucial LSD1-p53 interaction is the focus of this study. Using several complementary assays [29], [30], [31], [32], we find that a well-defined segment of p53-CTD is capable of binding to LSD1 active site, thereby inhibiting the enzymatic activity
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Histone acetylation is regulated by two groups
2021-11-06
Histone acetylation is regulated by two groups of enzymes, histone acetyltransferases (HATs) and deacetylases (HDACs), with antagonizing functions (Wang et al., 2009b). Among members of HATs, p300 and CBP are homologous. Both are global transcriptional co-activators (Ogryzko et al., 1996), and play
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Whether histamine receptor distribution is altered in canine
2021-11-06
Whether histamine receptor distribution is altered in canine GI diseases remains unknown, but human research has documented altered histamine receptor density in certain GI diseases (Sander et al., 2006, Deiteren et al., 2015, Von Rahden et al., 2011). Additionally, a novel H4 receptor antagonist, J
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The current study identified the presence
2021-11-06
The current study identified the presence and location of all four histamine receptors in the GI tract of 6 healthy adult dogs. Although no clinical signs of GI disease were noted, mild inflammation was noted in at least one section of the GI tract in all dogs based on WSAVA guidelines. Interpretati
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In an attempt to further optimize interactions in the lipoph
2021-11-06
In an attempt to further optimize interactions in the lipophilic P4 pocket, we next prepared compounds – () which possessed the preferred stereochemistry at P4, but with R-groups of varying size and shape. In addition to providing important structural information for maximizing potency, these compou
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Shikonin represents naphtoquinonic compound isolated from
2021-11-05
Shikonin represents naphtoquinonic compound isolated from the Chinese plant Lithospermum erythrorhizon[20]. Shikonin treatment inhibits AKT and ERK signaling pathways and induces apoptosis through FOXO transcription factors and mitochondrial pathway [21], [22]. Recent results suggest inhibition of l
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After the origin of the family of genes for receptors
2021-11-05
After the origin of the family of genes for receptors for peptides similar to glucagon, the genes have not remained static. Not only have their sequences evolved, but also like peptides similar to glucagon (Irwin, 2001, Irwin, 2009, Irwin, 2012, Ng et al., 2010, Hwang et al., 2013), the numbers of
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How do myofibroblast sources compare between bone
2021-11-05
How do myofibroblast sources compare between bone marrow and other organs? Perivascular mm stock with MSC properties significantly contribute to fibrosis in muscle, fat, skin, heart, kidney, lung, and liver (reviewed in Iwayama et al., 2015) and activate Gli1 in many of these organs (Kramann et al.
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Growth hormone secretagogue receptor GHSR
2021-11-05
Growth hormone secretagogue receptor (GHSR) is a member of G-protein-coupled receptor family [3]. GHSR is predominantly expressed in human pituitary, rhypothalamus and hippocampus [4]. GHSR is also expressed in peripheral tissues including lungs, liver, kidney, and adrenal gland. In cardiovascular s
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Cladribine australia NMDARs are glutamate gated ionotropic r
2021-11-05
NMDARs are glutamate-gated ionotropic receptors that are involved in excitatory neurotransmission and plasticity (Traynelis et al., 2010). There have been several reports showing that neurosteroids acting as negative modulators of NMDARs exert neuroprotective activity in both in vitro and in vivo mo
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odanacatib br BA induced activation of TGR TGR
2021-11-05
BA-induced activation of TGR5 TGR5 is a membrane-bound G protein-coupled receptor for BAs and its activation is dependent on cAMP formation and further stimulation of protein kinase A [53], [31]. The receptor is expressed in the enterochromaffin cells, smooth muscles, immune cells and more import
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br FREE FATTY ACID RECEPTOR GPR br G PROTEIN
2021-11-05
FREE FATTY ACID RECEPTOR 1 (GPR40) G-PROTEIN-COUPLED RECEPTOR 120 CONCLUSION Free fatty perhexiline receptor receptors whose natural ligands are identified as FFAs having various lengths have been reported. They act as novel nutrient sensing receptors independent of PPARs and FABPs, and th
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