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ASC was reported as a potent antiviral and
2020-03-07
ASC was reported as a potent antiviral and antifungal agent, and its derivatives could modulate a variety of physiological activities, such as anti-tumor, anti-metastatic, and anti-diabetic activities in animals. Mie Tsuruga et al. found that 4-o-methylascochlorin had immunosuppressive activity, but
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Compound was advanced to a chronic efficacy
2020-03-07
Compound 52 was advanced to a chronic efficacy study in db/db mice maintained on a high fat diet. Animals were dosed with 0.5% methylcellulose vehicle, marbofloxacin 52 (1, 3 or 15mg/kg, po, Q.D.) or 1 (0.3mg/kg) for 14days. Over the course of the study body weight and food intake were measured dai
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br Fragment based drug discovery
2020-03-06
Fragment-based drug discovery (FBDD) is a powerful method to discover drug leads and has been widely adopted in both academia and industry. FBDD can be used to explore chemical cAMPS-Rp, triethylammonium salt space with libraries which are smaller in size, producing drug leads with high ligand-bi
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Introduction Postoperative delirium POD is a
2020-03-06
Introduction Postoperative delirium (POD) is a potentially debilitating disorder experienced by many elderly patients admitted to a surgical intensive care unit (ICU) after noncardiac surgery. Delirium is often defined as acute cognitive dysfunction that is characterized by an altered mental status
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In this report we established mouse models suitable for
2020-03-06
In this report, we established mouse models suitable for human retinal cell transplantation by introducing phosphodiesterase 6B (Pde6b) mutant allele from retinal degeneration (rd) mouse models into NOG background. Pde6b (rd1) and Pde6b (rd10) mice are well-studied and frequently used animal models
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Binding affinity was measured by a scintillation
2020-03-06
Binding affinity was measured by a scintillation proximity binding assay using [H]4-OHT (ERRγ) or [H]estradiol (ERα/β) as radioligand. In all cases, the ERβ affinity was not significantly different from ERα. Compounds were compared to , which showed high affinity for both receptors and moderate (si
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Molecular docking study of compound was performed
2020-03-06
Molecular docking study of KT 5720 was performed using the Schrödinger Small-Molecule Drug Discovery Suite taking advantage of known X-ray crystal structures of activated EPAC2 protein. The model shows that compound occupies the CBD of EPAC2 and forms hydrogen bonds with Arg448 and the cyano-hydraz
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In conclusion our study has
2020-03-06
In conclusion, our study has demonstrated that PGE2 stimulates expression of survivin in hepatocellular carcinoma cells. Although there are 4 subtypes of EP receptors, the EP1 receptor appears to be the predominant receptor that regulates PGE2-induced expression of survivin, mainly through trans-act
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The intracellular redox situation of MC T E cells
2020-03-06
The intracellular redox situation of MC3T3-E1 ephrin receptor after exposure with fluoride has been investigated and results revealed that the generation of ROS increased at a concentration-dependent manner, which indicated that NaF induced oxidative stress damage in MC3T3-E1 cells. Fluoride-mediat
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Several reports by us and others have
2020-03-06
Several reports by us and others have highlighted that dimerization or oligomerization of DDR1 ECD and DDR2 ECD enhances their binding to triple-helical collagen.18, 19, 22, 28, 29, 30, 31 The ECD of DDRs consists of a discoidin domain and a stalk region. It has been reported that independent CI994
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KU-55933 While a growing body of knowledge demonstrates
2020-03-06
While a growing body of knowledge demonstrates the importance of COX-1 and COX-2 accompanied with neuroinflammation in altitude related conditions. In fact, PGE2 has been widely thought to promote the neuronal inflammation and degeneration in many neurological maladies (Griffin et al., 2013, Jiang a
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The recombinant Scl collagen system has shown
2020-03-06
The recombinant Scl2 collagen system has shown capability as a biomaterial as well because of its adaptability and scalability. Scl2 was functionalized to crosslink into a hydrogel without disrupting its triple helix [130]. The Scl2–hydrogel crosslinking also did not disrupt cell adhesion and integr
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The absence of an observable time dependence
2020-03-06
The absence of an observable time dependence of kobs on inhibitor concentration for Candesartan 3 with AChE and compounds 1, 3 and 4 with BuChE parallels a similar absence of time dependence for some related fluoro ketones with AChE. Nair et al. found that trifluoromethyl acetophenones with small m
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br In order to determine the
2020-03-06
In order to determine the physiological roles of WT (wild type) EWSR1, Dr. Lee\'s group established a conventional Ewsr1 KO mouse [38]. Since then, the Ewsr1 KO (−/−) mouse model has successfully been utilized to decipher many important in vivo roles of EWSR1 (Fig. 1). EWSR1 deficiency alters m
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Little information is available regarding the expression of
2020-03-06
Little information is available regarding the expression of the different EP receptor subtypes on human monocytic cells, particularly those that are involved in downregulating cytokine production. The receptors are controlled by the respective genes for each receptor i.e. PTGER1–PTGER4 for EP1–EP4 r
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