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We have previously disclosed the discovery of
2020-07-08
We have previously disclosed the discovery of a 7-azaindole-3-acetic lamotrigine CRTh2 antagonist chemotype 1 from HTS and its subsequent optimization to give 2 as a potent and orally bioavailable inhibitor of eosinophil shape change (SC) in human whole blood. Subsequent to disclosure of that work,
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SB742457 synthesis Introduction Eicosanoid lipid prostagland
2020-07-08
Introduction Eicosanoid lipid prostaglandin D2 (PGD2) is the major prostaglandin produced by activated mast SB742457 synthesis (Lewis and Austen, 1981). The physiological function of PGD2 is mainly mediated by two G protein-coupled receptors (GPCRs), PGD2 receptor 1 and 2 (DP1 and DP2), which shar
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Introduction The physiological significance of
2020-07-08
Introduction The physiological significance of hypoxia is undisputed, although largely over looked in the cancer therapeutics field focused on DNA-damage induced by ionizing radiation or drug treatment. Regions of hypoxia occur during a range of diverse biological situations including embryogenesis
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Several of the plant extracts that showed interaction with E
2020-07-08
Several of the plant extracts that showed interaction with ERα and ERβ have differing reports concerning estrogenicity and receptor binding. Extracts of dong quai stimulated MCF-7 proliferation but failed to increase uterine weight or transactivate either ERα or ERβ in a cell assay (Amato et al., 20
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We have previously shown that sustained pCPT
2020-07-08
We have previously shown that sustained 8-pCPT treatment favored Ca2+-dependent arrhythmogenic activity in rat ventricular cardiomyocytes [8]. Fig. 2 shows line-scan Ca2+ images of myocyte incubated without (Fig. 2A left) and with 8-pCPT (Fig. 2A right) subjected to a train of electrical stimulation
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Interest in the PGE EP pathway is increasing given its
2020-07-08
Interest in the PGE2/EP4 pathway is increasing given its diverse capability of regulating central nervous system activity [13]. EP4 has a protective function by reducing cerebral injury and improving functional outcome after stroke [14], and in suppressing Cy5 NHS ester (non-sulfonated) inflammatio
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Among the down regulated genes
2020-07-08
Among the down-regulated genes were several of interest. Coronin2a (Coro2a), a component of the nuclear receptor co-repressor complexes, contributes to de-repression of inflammatory response genes (Huang et al., 2011). Mill1, an MHC family member expressed in hair follicles, represses wound healing
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Ligand independent constitutively active variants
2020-07-07
Ligand-independent, constitutively active variants have also been found in receptors with associated tyrosine kinases. In approximately 60% of patients harboring inflammatory hepatocellular adenomas (IHCAs), these adenomas have been caused by small in-frame deletions in the cytokine-binding domain o
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When a hour delay period
2020-07-07
When a 6-hour delay PRL-3 Inhibitor was implemented for the WRAM, neither of the E2-treated groups (E2-only and E2 + Levo) differed in WMC errors between the postdelay trials and the baseline trials. This suggests that exogenous E2 treatment protected from a delay-induced impairment in performance
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br Experimental Procedures br Acknowledgments br
2020-07-07
Experimental Procedures Acknowledgments Introduction Bisphenol A (BPA), 2,2-bis (4-hydroxyphenyl) propane, is widely used to manufacture consumer products including food and beverage containers (Vandenberg et al., 2007). It can be accumulated in human body via leaching from the polymers int
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br Results br Discussion Adaptive drug resistance is a major
2020-07-07
Results Discussion Adaptive drug resistance is a major challenge to the clinical success of cancer therapies. Incomplete inhibition of oncogenic signaling allows survival of “drug-tolerant” tumor cells, which persist in that state for variable periods before acquiring additional genetic mutati
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br Materials and methods br Results br Discussion Cisplatin
2020-07-07
Materials and methods Results Discussion Cisplatin, as one member of a class of platinum-containing anti-cancer drugs, which displays a great deal of clinical activity on a wide variety of solid tumors. In addition, cisplatin often used in combination with other chemotherapy drugs to treat
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To identify and characterize new
2020-07-07
To identify and characterize new possible molecular targets, the mechanisms of various kinds of TCDD toxicities that occur by abnormal regulation in the downstream of AhR signals have been studied (Yoshioka et al., 2011). Experimental evidence has revealed that prostanoids (i.e., prostaglandins and
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For immobilization of enzymes natural polymers depict
2020-07-07
For immobilization of enzymes, natural polymers depict several outstanding features as support. These materials are inert, non-toxic, biodegradable and biocompatible. As well as, they can be treated with different functional groups easily by chemical reactions that occur under gentle conditions in a
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Tropical theileriosis is caused by
2020-07-07
Tropical theileriosis is caused by the apicomplexan parasite Theileria annulata which is transmitted by a tick vector from the genus Hyalomma in cattle (Echebli et al., 2014, Li et al., 2014). Theileria parasites invade the leukocytes by sporozoites secreted from the vector, schizonts mature into me
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