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Over recent decades there were
2021-09-10
Over recent decades, there were three breakthroughs of high intensity heavy-ion acceleration [6]. The first is the invention of radio frequency quadrupole (RFQ) type accelerator, which could accelerate more than dozens of milli-ampere ion beams and is a good solution to space-charge-effect of heavy-
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In order to study the role of
2021-09-10
In order to study the role of haspin’s kinase activity in mitosis (and other cellular processes) and its potential role in cancer, we sought to identify and optimize inhibitors. Utilizing a recently developed time-resolved fluorescence resonance energy transfer (TR-FRET) high throughput screening (H
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Initial structural and biochemical work
2021-09-10
Initial structural and biochemical work showed that Get3 forms an obligate dimer whose conformation is regulated by the bound nucleotide. Analogous to SRP and SR, Get3 contains a P-loop nucleotide hydrolase domain in which the bound ATPs face one another at the dimer interface (Figure 3A, top right
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br Synthetic Antagonists for FFA
2021-09-10
Synthetic Antagonists for FFA4 To date, only compounds from a single chemical series have been reported as FFA4 ‘antagonists’ (Table 1). ‘Compound 39’ (4-methyl-N-9H-xanthen-9-yl-benzenesulfonamide), now available from commercial vendors as AH-7614, was initially reported as an antagonist at this
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Our last area of exploration was
2021-09-10
Our last area of exploration was the piperidine core as shown in . We rationalised that the basicity of the nitrogen (measured p=7.0) may be responsible for the affinity for the hERG receptor and we therefore sought to moderate this by incorporation of electronegative groups at the 3-position. To th
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Migratory properties of Treg are extremely important for the
2021-09-10
Migratory properties of Treg are extremely important for the potential in vivo application. Therefore, the observed expression of CXCR3 on almost all obtained insulin-specific Treg is crucial for directing AL 8810 into the inflamed tissue (in this case pancreatic islets). CXCR3 responds to CXCL9, C
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Introduction Cancer is known as a renegade system of
2021-09-10
Introduction Cancer is known as a renegade system of expansion that initiate in human body. It is distinguished, in spite of its category, by one universal characteristic, which is uncontrolled cell division. Cancerous MCB-613 have the ability to bypass the normal apoptosis mechanism (National Canc
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In conclusion we have shown that AKR
2021-09-09
In conclusion, we have shown that AKR1D1 regulates glucocorticoid availability and GR activation and therefore represents a key pre-receptor regulator of hormonal action in human liver. However, there are additional questions that need to be addressed including dissecting the broader role of AKR1D1
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The relationship between estrogen and the Hedgehog pathway a
2021-09-09
The relationship between estrogen and the Hedgehog pathway as well as the associated mechanism have already been investigated in many tissues, especially in breast cancer (Chang et al., 2012, Katayama et al., 2006, Ramaswamy et al., 2012). Hitherto, even though we have proved that HH-Gli pathway pro
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br Materials and methods br Results br Discussion Our study
2021-09-09
Materials and methods Results Discussion Our study demonstrates that human GIP(3-30)NH2 is a selective GIPR antagonist that inhibits both GIP-mediated cAMP signaling, β-arrestin recruitment, and GIPR internalization. Furthermore, we demonstrate that human GIP(3-30)NH2 binds with high affini
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Saracatinib In a series of experiments the
2021-09-09
In a series of experiments, the clotrimazole concentration was varied and the NSVDC channel conductances were calculated from Eq. (1) to obtain the dose-response relation (Fig. 3). The data were fitted to the Michaelis–Menten-type activation curve (Eq. (3)) and gave an EC50 value of 14 μM and a dose
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In contrast with the above results in our
2021-09-09
In ci-1033 with the above results, in our GC model system, FPR1-, but not FPR2-knockout, enhanced tumour formation. However, it should be noted that the prominent role of mFPR2 with respect to mFPR1 in the mouse colon might be due to the significantly higher expression of mFPR2 than mFPR1 in this ti
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Compounds were tested for GPR activity in a
2021-09-09
Compounds , were tested for GPR40 activity in a functional assay monitoring calcium flux in CHO Sertraline HCl 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 structure activity
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In this study we intended to
2021-09-09
In this study, we intended to explore the efficacy of artesunate on liver fibrosis and further clarify its potential molecular mechanism. Artemisinin, a sesquiterpene lactone obtained from a Chinese plant Artemisia annua [27]. Artesunate, as a stable derivative of artemisinin, is an effective drug f
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NG,NG-dimethyl-L-Arginine hydrochloride br Application of TI
2021-09-09
Application of TIRFM to visualizing exocytosis TIRFM was first used to visualize exocytosis from large secretory granules from chromaffin NG,NG-dimethyl-L-Arginine hydrochloride (Steyer et al., 1997). Before that, visualization of secretory organelle was strictly limited to a few exceptions, suc
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