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We next examined the effects of substituents around the
2020-11-11
We next examined the effects of substituents around the carboxylic Hyper Assembly moiety on CRTH2 binding (Table 4). The carboxylic acid moiety shared by the representative CRTH2 antagonists and is essential for the CRTH2 activity. Germinal dimethylation of the methylene moiety next to the carboxyl
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The results of bisaryl ether linker study
2020-11-11
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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Alternatively procedural factors may have contributed to
2020-11-11
Alternatively, procedural factors may have contributed to the conflicting results. For instance, in order to have a more circumscribed area of drug diffusion, a volume of 0.05μl was injected in experiment 1b, which is four times lower than the one used in the mentioned plus-maze investigation. Besid
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The synthesis of tricyclic analogs is described in Scheme Ox
2020-11-11
The synthesis of tricyclic analogs 28–33 is described in Scheme 3. Oxidative C–C bond cleavage of the terminal olefin of 39i afforded a tricyclic product 52 without isolation of an aldehyde expected as an intermediate. Aminolysis of the chloride 52 with optionally substituted anilines afforded 28–30
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In this study we observed alterations in mRNA levels of
2020-11-11
In this study, we observed alterations in mRNA levels of CRF receptors in the PFCx and Hip during the development of sensitization. In particular, in the Hip both CRF receptors showed significantly increased TCS 5861528 when the sensitization condition was established. Similarly, CRF2 receptor incr
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The mechanism by which these HIV
2020-11-11
The mechanism by which these HIV-PIs impair skeletal muscle palmitate transport and oxidation has been partially elucidated. CD36 (also referred to as fatty HC 067047 translocase; FAT) is a transmembrane protein involved in the transport of long-chain fatty acids (LCFA) across cellular membranes. It
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A further quandary concerning rediscoveries arises in habita
2020-11-11
A further quandary concerning rediscoveries arises in habitats modified and frequented by humans, where rediscovered species may occur through accidental or deliberate introductions (Metcalf et al., 2007) rather than having persisted despite adverse conditions. Confusion regarding origin could evoke
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In humans individual differences in
2020-11-11
In humans, individual differences in prefrontal dopamine are partially caused by the Val158Met single-nucleotide polymorphism on the catechol-O-methyltransferase gene (COMT). This gene controls activity of the COMT enzyme, which degrades extracellular catecholamines including dopamine. The Val varia
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The two SNPs rs rs
2020-11-11
The two SNPs rs4818-rs4680 presented above are part of the haploblock (rs6269, rs4633, rs4818, rs4680) presenting the 3 major haplotypes which influence the enzymatic activity of COMT. This activity is inversely related to the sensitivity of pain in a chronic pain syndrome; so the haplotype (GCGG) h
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In frame exon skipping of COL A
2020-11-11
In frame exon 41 skipping of COL6A3 has been suspected to be responsible for isolated dystonia in several human kindreds without muscular defects [94]. In order to validate their hypothesis, the authors used zebrafish to selectively knock down several exons in col6a3 and found a negative impact on m
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Cell swelling stimulates the release of
2020-11-11
Cell swelling stimulates the release of certain amino acids, in particular the non-protein amino alzheimer's disease taurine, via a pathway which has the characteristics of a channel rather than a carrier [54], [69]. Indeed, on the basis of pharmacological inhibition, it was suggested that volume-a
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Estrogen receptors ERs belong to the
2020-11-11
Estrogen receptors (ERs) belong to the third class of nuclear receptors (NR3) [23]. Two different forms of ER have been described, ERα and ERβ. They are coded by two distinct genes (ESR1 and ESR2, respectively) containing 8 transcribed exons that give rise to six conserved protein domains: domains A
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Because most fusion detection methods
2020-11-11
Because most fusion detection methods were developed to analyze paired-end reads (and especially Illumina data), they are not suitable for identifying fusion junction-spanning reads in single-end Ion Torrent libraries. Therefore, we developed the FusionDetect algorithm (implemented in the ChildDecod
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There may be an interplay of EP EP EP
2020-11-10
There may be an interplay of EP2, EP3, EP4 alone, or in combination, with EP1 for the onset of TCDD-induced neonatal hydronephrosis. EP2 and EP4 have been reported to increase AQP2 phosphorylation and membrane trafficking (Li et al., 2009; Olesen et al., 2011). The EP2 and EP4 mRNA concentrations we
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We can think of two ways
2020-11-10
We can think of two ways in which collagen binding could activate DDR (Figure 8). A single collagen triple helix could interact with both DS domains in the DDR dimer (“composite binding site”) and thereby activate the receptor, similar to the situation exemplified by the growth hormone-growth hormon
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