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br Author Contributions br Acknowledgments br
2020-12-08

Author Contributions Acknowledgments Introduction Many anticancer agents bind covalently to DNA, introduce bulky adducts, and inhibit DNA metabolic processes including repair, replication and transcription.1., 2., 3. Frequently, the first enzymes to encounter DNA adducts are DNA helicases.
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The discoidin domain receptors DDR and DDR are receptor
2020-12-08

The discoidin domain receptors, DDR1 and DDR2, are receptor tyrosine kinases (RTKs) that are stimulated by collagen in the extracellular matrix (ECM). Unlike most other RTKs, they form ligand-independent stable dimers that are non-covalently linked. This ECM activation induces receptor phosphorylati
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It is well established that Shp
2020-12-08

It is well established that Shp-2 can function as a substrate for several RTK, such as PDGF or EGFR [23], [36]. To test whether DDR1 recognizes Shp-2 as its substrate, we overexpressed a catalytically inactive Shp-2 mutant together with DDR1b in 293 cells [31]. Immunoprecipitation of Shp-2 followed
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The genomic DNA sequences of CXCL and CXCRs were
2020-12-08

The genomic DNA sequences of CXCL8 and CXCRs were retrieved from the fugu genome database v4.0. The intron–exon boundaries were identified with the corresponding cDNA sequences. This comparison revealed that the fugu gene is about 1.13kb long and contains four exons separated by three introns (top p
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cox 2 inhibitors We propose two hypotheses to interpret our
2020-12-08

We propose two hypotheses to interpret our findings. The first, ELR (+) CXC chemokines stimulate both CXCR-1 and CXCR-2 chemokine receptor while activating neutrophils; however CXCR-1 chemokine receptor seems to play more active role in the process of neutrophil migration as shown in previous studie
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Mechanistically GW treatment modulated cytokine expression w
2020-12-08

Mechanistically, GW2580 treatment modulated cytokine expression within the kidney. We noted a decrease in the levels of TNF, MCP-1, IL-1β, IL-27, and GM-CSF in GW2580 treated mice. Decreased levels of these proinflammatory cytokines likely contributed to the attenuated proteinuria and improved renal
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Conversely to the reduction in restraint evoked
2020-12-08

Conversely to the reduction in restraint-evoked HR increase following the blockade of CRF receptors, Nijsen et al. [28] demonstrated that BNST treatment with a nonselective CRF fluoxetine hydrochloride antagonist enhanced the tachycardia evoked by contextual fear conditioning. Taken together, these
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Physiological changes induced by CRF are mediated through CR
2020-12-08

Physiological changes induced by CRF are mediated through CRF1 and CRF2 receptors (Chang et al., 1993, Lovenberg et al., 1995). Previous findings with CRF1 receptor antagonists showed that activation of CRF1 receptor is involved in maternal separation-induced ultrasonic vocalizations (Kehne et al.,
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The aim of the present
2020-12-08

The aim of the present study was to investigate the participation of CRF1 and CRF2 in the alterations of the dorsal and ventral striatal dopamine release and the vertical and horizontal locomotor activity observed in rats following chronic nicotine treatment and consequent acute withdrawal. In this
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In previous works Gotor Vila et al
2020-12-08

In previous works (Gotor-Vila et al., 2017c), differences in solubility between the two carriers used during formulation were evidenced. Summarizing, maltodextrin (BA3 product) resulted in a much more soluble product since this polysaccharide is typically composed of an amount of reducing sugars bet
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br Results br Discussion Here we establish a key kinase
2020-12-08

Results Discussion Here we establish a key kinase cascade that acts at PCs to promote homolog pairing and synapsis. CHK-2 phosphorylates the zinc finger proteins that specify PCs, which, in turn, primes their recruitment of PLK-2 (Figure 7D). By recruiting these two kinases, PCs serve as signa
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Estrogen receptor related receptor ERR like other members of
2020-12-07

Estrogen receptor-related receptor γ (ERRγ), like other members of the ERR subfamily, is a constitutively active orphan nuclear receptor, though unlike ERRα and β, it is more selectively expressed in metabolically active and highly vascularized tissues such as heart, kidney, brain, and skeletal musc
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Prostaglandin E receptor subtype EP is a transmembrane G cou
2020-12-07

Prostaglandin E receptor subtype 4 (EP4) is a transmembrane G-coupled protein receptor activated by prostaglandin E2 (PGE2). EP4 activation exerts anti-inflammatory effects in adipose tissue by dampening the levels of inflammatory chemokines [12]. In the mouse, EP4 deficiency aggravates fragmentatio
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Compounds and possessed relatively low clogP values and tend
2020-12-07

Compounds 11–13 and 15 possessed relatively low clogP values and tended to show relatively weak antagonist activity regardless of their potent EP1 receptor affinity. Compounds 2–4, which were selected based on their potent in vivo antagonist activity, were found to be effective in an animal model.
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nampt inhibitor Conventional assays rely on a comparable tra
2020-12-07

Conventional assays rely on a comparable transformation of the target analytes and the structurally similar (but not identical) proxy substrates and are commonly used to measure individual enzyme activities in (pre-treated) intact sludge flocs (Burgess and Pletschke, 2008a, Gessesse et al., 2003, Yu
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