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It is now widely known
2021-03-25
It is now widely known that blockade of CysLT1 receptors strongly inhibits antigen-induced bronchial contractions in specimens isolated from non-asthma subjects. However, this blockade is not complete as shown in the present study and in other literature.4, 15, 16 The results of the current study su
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Midazolam oral clearance is used for characterization of bot
2021-03-25
Midazolam oral clearance is used for characterization of both intestinal and hepatic CYP3A activity. However, the identification and subsequent use of metabolic markers of CYP3A activity can eliminate the need for unnecessary administration of probe drugs such as midazolam. Such metabolic markers wo
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CDK S phosphorylation status influences the differential cel
2021-03-25
CDK5-S47 phosphorylation status influences the differential cellular proliferation versus migration response: Previous work from our laboratory has shown CDK5 to be a critical determinant of the cellular proliferation-migration dichotomy whereby CDK5 activation downstream of stimulated epidermal gro
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Phylogenetic analysis indicates that in poikilothermic verte
2021-03-25
Phylogenetic analysis indicates that in poikilothermic vertebrates CXCR3a and CXCR3b have evolved independently from a common gene possibly after the 2nd round whole genome duplication but before the split of bony fish and tetrapods (Fig. 1 and Supplementary file 3). Owing to the extra round of whol
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The results of bisaryl ether linker
2021-03-25
The results of bisaryl ether linker study are shown in . It was found that the methylene linker () moderately improved the binding to the DP receptor. The increased binding potency was also diminished in the presence of plasma, possibly due to higher plasma protein binding. Other linkers, such as th
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br Acetylcholinesterase and cholinergic signaling
2021-03-24
Acetylcholinesterase and cholinergic signaling The concept of a synapse between a neuron and an innervated cell, and the receptors that mediated their interaction, was developed by Bernard, Ehrlich, Sherrington, Langley and others (see [7], [8], [9]. It was long debated whether transmission of ne
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Based upon these findings on portions A and B novel
2021-03-24
Based upon these findings on portions A and B, novel scaffolds of EP4 antagonist, and (R & R=()-Me; =Cl; R=H), shown in , were identified. We next focused on optimizing portion C of these scaffolds. We utilized for an alternative synthesis of nicotinamide scaffold , which is quite effective for
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To study systemic potential of the selected
2021-03-24
To study systemic potential of the selected compounds as EP1 receptor antagonist, they were evaluated with regard to the sulprostane-induced increase of intravesical bladder pressure in rats. Some of the analogs, 13 and 15–17, which were selected on the basis of their in vitro EP1 receptor affinity,
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br Summary and perspectives In recent
2021-03-24
Summary and perspectives In recent decades, enormous advances have been achieved in the development of enzyme-activatable imaging probes, enabling the accurate detection of enzyme activity in vivo to better understand the biological function of enzymes in disease processes. Activatable probes are
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Multiple protein species are known
2021-03-24
Multiple protein species are known to naturally exist for the transmembrane receptors DDR1 and DDR2. Five splice variants have been characterized for DDR1 (“a” through “e”). The d and e isoforms lack the intracellular kinase domain of DDR1. The splicing of DDR1 to various extents has been reported i
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br Results br Discussion Analysis of EBI expression showed t
2021-03-24
Results Discussion Analysis of EBI2 expression showed that EBI2 is highly expressed in central memory CD8+ T cells that is in line with previous data from human T cells in which these GDC-0068 express higher levels of EBI2 than naive or effector memory CD8+ T cells (Hannedouche et al., 2011).
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After incorporation of random nucleotides by TdT during heav
2021-03-24
After incorporation of random Phos-tag Biotin by TdT during heavy-chain rearrangements, both TdT and pol λ may perform in trans polymerase activity (in unknown proportions), whereas synthesis of the complementary strand can only be achieved by pol λ using its gap-filling activity, which TdT lacks b
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br Application of the screening system for
2021-03-24
Application of the screening system for ITP-binding proteins Inosine is a nucleoside with hypoxanthine as a base. Inosine nucleotides are relatively abundant in human ampa receptor because inosine monophosphate (IMP) is a general precursor molecule for the de novo synthesis of AMP and GMP or a pr
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Interaction between neutrophils and ECs represents the first
2021-03-24
Interaction between neutrophils and ECs represents the first step of the cellular phase of the inflammatory response, and provide the best condition for the transfer of the PMNL-derived LTA4 to the ECs, leading to the transcellular formation of cysteinyl-LTs. It is intriguing therefore to think that
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In a previous study we reported that
2021-03-24
In a previous study we reported that the systemic administration of the α1-adrenergic receptor antagonist prazosin attenuates the deficit in Thio-TEPA reward function associated with precipitated nicotine withdrawal (Bruijnzeel et al., 2010). One of the aims of the present experiments was to invest
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