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Compounds were tested for GPR activity in
2022-07-16
Compounds , were tested for GPR40 activity in a functional assay monitoring calcium flux in CHO Psalmotoxin 1 receptor transiently transfected with human GPR40 gene. As shown in , compound was found to be a nanomolar GPR40 agonist, while compound was much less potent than . To explore the structu
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LY2584702 In addition we assessed the viability
2022-07-16
In addition, we assessed the viability of 1,2,3,4-tetrahydroquinoline (13t) and 1,2,3,4-tetrahydroisoquinoline (13u) as the tail on account of our previous SAR results. To our delight, 13t and 13u each had comparable activity to that of 13c, with 13u being slightly more potent than 13c. Further stru
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The therapeutic potential of acetate has
2022-07-15
The therapeutic potential of acetate has been advocated by research on neurodegenerative disorders such as Canavan's disease (Arun et al., 2010, Mathew et al., 2005), where oral acetate improved motor function in a genetic model of the disorder, and in studies of behavioural phenotypes associated wi
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In addition to GABA mediated mIPSCs glutamate mediated
2022-07-14
In addition to GABA-mediated mIPSCs, glutamate-mediated miniature excitatory postsynaptic potentials (mEPSCs) regulate the excitability of the nervous system. GluRs can be divided into ionic and metabotropic GluRs. Ionotropic GluRs can be pharmacologically differentiated by specific binding of the a
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To evaluate SLC A abundance
2022-07-14
To evaluate SLC45A1 abundance after transfection, we performed western blots. Transfected COS-7 BADGE were lysed and separated for membrane fraction. Equal amounts of proteins from membrane fractions were resolved by SDS-PAGE, transferred to a nitrocellulose filter, and immunoblotted with an anti-S
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cdk1 mg The HH Gli pathway has been demonstrated to
2022-07-14
The HH-Gli pathway has been demonstrated to play an extensive role in skeletal development. India Hedgehog, derived from hypertrophic chondrocytes, and Parathyroid Hormone-like related Protein (PTHrP), derived from peri-articular chondrocytes, form a negative feedback loop to inhibit chondrocyte hyp
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Ghrelin is a brain gut
2022-07-14
Ghrelin is a brain-gut peptide hormone secreted from the stomach to stimulate food intake by acting on its receptor, growth hormone secretagogue receptor (GHSR). GHSR is expressed throughout the brain and in NPY/AgRP neurons in the ARC (Cowley et al., 2003, Willesen et al., 1999). Ghrelin-expressing
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Regarding IAV types of hemagglutinin and types of neuraminid
2022-07-14
Regarding IAV, 18 types of hemagglutinin and 11 types of neuraminidase were described and none of the commercialized antiviral drugs are susceptible to protect against all strains that will emerge from the animal reservoir (Webby and Webster, 2003). The strong dependencies of influenza viruses on we
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The present study showed that the FPR
2022-07-14
The present study showed that the FPR2 antagonists PBP10 and BOC2 are potent antiviral molecules in vitro against a broad range of IAV and B viruses. Consistently, our previous report showed that FPR2 plays a deleterious role during IAV infections and that another FPR2 antagonist WRW4 inhibits IAV r
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We thus asked whether enhanced AEA levels in
2022-07-14
We thus asked whether enhanced AEA levels in the Propidium iodide reduce the level of age-related inflammatory changes and slow down brain ageing. To answer this question we compared the morphology of microglia and level of pro-inflammatory cytokines in the hippocampus of young and old wild-type an
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br Parkinson disease Idiopathic PD is a hypodopaminergic
2022-07-14
Parkinson disease Idiopathic PD is a hypodopaminergic movement disorder of uncertain etiology that affects 3% of persons over age 65 (Dexter and Jenner, 2013). Cardinal signs of this common neurodegenerative condition include bradykinesia, rigidity, rest tremor and postural instability. Autonomic
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br Introduction The signaling molecule nitric oxide NO plays
2022-07-13
Introduction The signaling molecule nitric oxide (NO) plays an essential role in vessel homeostasis by initiating vasodilation [1], [2], [3]. After biosynthesis in endothelial cells, NO diffuses into the subjacent smooth muscle layer to reach its target enzyme, soluble guanylyl cyclase (sGC, EC 4
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The first report of GUCY
2022-07-13
The first report of GUCY2D-related gene augmentation therapy in mammalians was also reported in 2006 in the KO mouse model (section 4.1.1). In this study, an AAV5 vector by using AAV5-mediated transfer of the bovine cDNA (the same used in the chicken study) was injected to the post-natal KO retina a
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Recently a G protein coupled receptor GPR a
2022-07-13
Recently, a G-protein-coupled receptor, GPR109a, was identified as a molecular target for niacin. Following this breakthrough, our group initiated a drug discovery program focused on the development of a high affinity ‘flush-free’ niacin-like agonist. Previously, we reported on the identification of
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br Several reports have shown an anti proliferative effect
2022-07-13
Several reports have shown an anti-proliferative effect of type I IFNs on CD4+ T Epothilone D activated in vitro either upon anti-CD3 antibody treatment [28,29] or upon cognate antigen stimulation [29]. However, the in vivo setting is a lot more complex, since the final outcome is the net effect
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