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GW was also the starting point
2022-05-13
GW4064 was also the starting point for a study by an independent research group. The co-crystal structure of GW4064 with FXR suggested the potential for favorable hydrogen bond interactions between the isoxazole 3-aryl group and several receptor residues such as Tyr373 and Ser336. Replacing the 2,6-
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Our supF forward mutation assay revealed for the first
2022-05-13
Our supF forward mutation assay revealed, for the first time, that 5OHU predominantly induced the C→T mutation in human cells. The mechanism underlying the induction of the C→T mutation in human cells by 5OHU remains unclear, however, the finding that 5OHU predominantly induced the C→T mutation was
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Glial cells have emerged as important
2022-05-13
Glial cells have emerged as important protagonists of the central nervous system (CNS) physiology (Chen and Swanson, 2003; Kettenmann and Verkhratsky, 2008; Parpura and Verkhratsky, 2012). As widely described in the literature, astrocytes regulate glutamatergic synapses by clearance of glutamate in
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PBI is an agonist of GPR and
2022-05-13
PBI-4050 is an agonist of GPR40 and acts as an antagonist or inverse agonist of GPR84. It cannot be excluded that other targets besides GPR40 and GPR84 could be implicated in the mechanism of action of PBI-4050 and could be explored in future studies. However, the present study, and in particular th
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GPCR Compound Library br Investigations br Genetics GLUT is
2022-05-13
Investigations Genetics GLUT1 is a membrane-bound glycoprotein that provides base-rate glucose transport across blood-tissue barriers. It is constituitively expressed in erythrocytes, GPCR Compound Library microvessels and astroglia. The gene exclusively associated with GLUT1 is SLC2A1, locat
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Pyrogallol is an organic gallic acid converting compound tha
2022-05-13
Pyrogallol is an organic gallic acid-converting compound that has three hydroxyl groups and belongs to the phenol family. Gallic snx is obtainable from the galls and barks of various trees, and a simple heating procedure can induce the decarboxylation of gallic acid to produce pyrogallol (alias: py
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Murine models of sickle disease have been
2022-05-13
Murine models of sickle disease have been valuable tools in the study of human SCD pathogenesis [15], [16], and will continue to be central to development of novel approaches to disease treatment. The SAD mouse model of sickle disease is particularly remarkable for its erythrocyte dehydration phenot
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As recently reviewed a picture is emerging where
2022-05-12
As recently reviewed, a picture is emerging where metabolites through GPCR sensors act as important autocrine and paracrine regulators of basic metabolic mechanisms (Husted et al., 2017). The concept of 20-HETE acting through FFAR1 as an autocrine amplifier of GDIS on β Atovaquone receptor together
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A few previous studies have examined Factor Xa inhibitors
2022-05-12
A few previous studies have examined Factor Xa inhibitors for VTE prophylaxis in hip fracture patients. In a 2001 paper, Eriksson et al. studied 1250 patients with hip fractures that had been randomized to either postoperative Factor Xa inhibitor or enoxaparin [13]. Each patient received bilateral v
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During the activation of the coagulation cascade factor Xa
2022-05-12
During the activation of the coagulation cascade, factor Xa (FXa) forms a complex with activated factor V and calcium P005091 sale on the surface of platelet membrane (so called prothrombinase complex) and converts prothrombin to thrombin [5], [6]. Selective FXa inhibitors do not directly inhibit p
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Accumulating evidence suggests that the NGF family
2022-05-12
Accumulating evidence suggests that the NGF family of neurotrophins have important modulatory roles in opioid analgesia and addiction [36]. The NGF family of neurotrophins include NGF, matrix metalloproteinase derived neurotrophic factor (BDNF), neurotrophin-3 (NT3), and neurotrophin-4 (NT4) [37].
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The mechanism study demonstrated that BDNF is one
2022-05-12
The mechanism study demonstrated that BDNF is one of the fundamental mechanisms underlying JMJD2A effects during neuropathic pain. BDNF is a neurotrophin with essential functions in neuronal development and neuroplasticity. Accumulating evidence suggests that alterations in BDNF expression levels un
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The H R antagonist cimetidine Tagamet became the
2022-05-12
The H2R antagonist cimetidine (Tagamet™) became the first billion-dollar drug in the 1980s for the treatment of peptic ulcer disease. Other H2R antagonists include ranitidine, famotidine, nizatidine, and zolantidine, the latter showing good BBB penetration with a steady-state brain/blood ratio of 1.
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In various models histamine has been shown
2022-05-12
In various models, histamine has been shown to induce chemotaxis. This was first appreciated over 40 years’ ago in studies with eosinophils (Clark et al., 1977). At that time, only histamine H1 and histamine H2 receptors were recognized and studies with ligands to these receptors indicated that neit
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br Results br Discussion Our current study demonstrates that
2022-05-12
Results Discussion Our current study demonstrates that the sustained activation of Yap overrides the p27-mediated checkpoint, at least in part, through the degradation of FoxO family proteins, allowing polyploid cells to proliferate inappropriately with mitotic defects and resulting in centros
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