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The optimization of the lead compound was initiated and the
2020-08-12
The optimization of the lead compound () was initiated and the initial key SAR and the results of the structural modifications of lead compound are summarized in . Replacement of the carboxylic SNDX275 moiety with other functional groups led to loss of functional activity against EP4 receptor. Alt
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In conclusion our study has demonstrated
2020-08-12
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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To be a qualified non specific CYP
2020-08-11
To be a qualified non-specific CYP inhibitor used as an in vitro or in vivo screening tool to distinguish CYP involvement in the overall metabolism, a complete inhibition of the entire metabolism catalyzed by CYPs in a simple experiment is desired. Based on our results, 100 μM atipamezole can comple
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The immune control of CMV replication in vivo is
2020-08-11
The immune control of CMV replication in vivo is primarily driven by the T-cell-mediated response, a characteristic that has been proposed as a tool to individualize and therefore to optimize antiviral treatment [6], [7], and it has been associated with spontaneous clearance of CMV viraemia in patie
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CK comprises a family of serine threonine protein kinases th
2020-08-11
CK1 comprises a family of serine/threonine protein kinases, that includes different CK1 isoforms namely α, β, δ, ε and γ their various splice variants [56]. It was reported that the pharmacological inhibitor IC261 shows an order of magnitude of higher selectivity for CK1δ or CK1ε isoforms (IC50 of 1
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br Results and Discussion br Conclusion What we
2020-08-11
Results and Discussion Conclusion What we have shown here is that highly specific antagonist can be a very useful tool, can mimic gene KO experiments or even further dissect receptor function. We just took ETA antagonist as an example and found that ETA mediates physiological closure of DA whi
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br Introduction Localized degenerative and progressive enlar
2020-08-10
Introduction Localized, degenerative and progressive enlargement of the aortic diameter involves all layers of the vessel wall may ultimately rupture creating a catastrophic cardiovascular event [1,2]. An aneurysm may be located in the thoracic or abdominal aortic wall with different clinical app
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Recent studies investigating the effects of mesenchymal stem
2020-08-10
Recent studies investigating the effects of mesenchymal stem cell (MSC) therapy in rodent models including chronic renal failure and glomerulonephritis have demonstrated that MSC therapy can result in beneficial effects [57], [58]. In cats, autologous intra-renal injections of either adipose tissue-
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Signal transduction through IL c FMS
2020-08-10
Signal transduction through IL-34/ c-FMS ligand receptor also leads to the differentiation, survival and, angiogenesis, proliferation, adhesion and migration of cells of the monocyte/macrophage lineage similar to that of CSF-1 through the various pathways-First is through FAK (Focal Adhesion Kinase)
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It is known that cigarette smoke increases
2020-08-10
It is known that cigarette smoke increases the oxidative burden in the lungs of mice with emphysema, which leads to oxidative stress [[34], [35], [36]]. However, in addition to cigarette smoke, studies have shown that endogenous oxidative stress is associated with proteolytic sodium salt in several
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The first example of a broadly acting antiviral
2020-08-08
The first example of a broadly-acting antiviral drug is ribavirin, a nucleoside analogue that was proposed to act directly at the level of the viral polymerase, although an indirect effect via inhibition of the host-cell IMP dehydrogenase and depletion of the GTP pool seems more plausible [9]. Anoth
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The two major families of E ubiquitin
2020-08-08
The two major TMP269 of E3 ubiquitin ligases (see Glossary) that coordinate cell division are SCFs (SKP1–CUL1–Fbox proteins), which were initially recognized for regulating interphase and are now known to control many stages of the cell cycle, and anaphase-promoting complex/cyclosome (APC/C), which
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br MARCH E ligases A specific family
2020-08-07
MARCH E3 ligases A specific family of eukaryotic E3 ligases that has received additional attention recently consists of the embrane-ssociated ING- (MARCH) proteins. Initially, two viral MARCH-homologue gene products were discovered in Kaposi\'s sarcoma (KS)-associated herpesvirus (KSHV), and subs
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The study looking at the recovery of cellular material
2020-08-07
The study looking at the recovery of cellular material showed that there was a higher percentage of recovery of DNA as a result of swabbing a non-stained fingermark than when applying DD to the fingermark and then collecting with a swab. DD, which is an external binder, binds to the sugar phosphate
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We next investigated the specificity of compounds and for TS
2020-08-07
We next investigated the specificity of compounds and for TS-DHFR over human DHFR, which does not have a cysteine residue corresponding to Cys44 of TS-DHFR (). Both compounds were incubated with human DHFR for 16 h to evaluate any inhibitory effects. Compound , was found to be highly selective for
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