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The first ones class A receptors
2021-04-17
The first ones class A receptors found as heterodimers were reported by Gomes et al. (2000), who identified a heteromer constituted by two subtypes of opioid receptors (μ and δ) in heterologous cells. The same year, Ginés et al. (2000) showed the first heteromer composed of two different receptors,
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CFSs are recognized as a driver of genome instability in
2021-04-17
CFSs are recognized as a driver of genome instability in human cells and are hotspots for deletions or translocations in cancers (Richards, 2001). The generally accepted model for their expression is that the CFS locus shows a delay in chromatin condensation in early mitosis caused by the persistenc
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br Experimental section br Notes br PDB ID
2021-04-17
Experimental section Notes PDB ID codes The atomic coordinates and structure factors of hDHODH in complex with compounds 4 (PDB id: 5MVC), 5 (PDB id: 5MVD) and 6 (PDB id: 5MUT) have been deposited in the RCSB Protein Data Bank. Acknowledgements This research was financially supported by
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In LPS treated BV cells we found that the upregulated
2021-04-17
In LPS-treated BV-2 cells, we found that the upregulated CysLT2R was translocated into the nucleus. The nuclear localization of CysLT2Rs in microglia has not been reported previously. It is known that CysLT1Rs in endothelial AZ3146 mg translocated to the nucleus in a ligand-independent manner after
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Testosterone is inactivated through hydroxylation and
2021-04-17
Testosterone is inactivated through hydroxylation and conjugation pathways [3], [4]. 6β-Hydroxylation is the main pathway among testosterone hydroxylation processes in the liver microsome. Testosterone 6β-hydroxylation is mainly catalyzed by cytochrome P450 3A (CYP3A) [5], [6], which is expressed in
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Introduction Cytochrome P CYP A is the
2021-04-17
Introduction Cytochrome P450 (CYP)3A is the most important enzyme involved in the metabolism of 30–40% of currently prescribed drugs [1]. The EDC.HCl level and activity of CYP3A show large intra- and inter-individual variability, which contributes to unpredictable drug response and toxicity. A mul
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Mechanistically GW treatment modulated cytokine
2021-04-17
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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Unlike CRM exportins Cse and Xpot lack a C
2021-04-17
Unlike CRM1, exportins Cse1 and Xpot lack a C-extension and instead rely primarily on changes in HEAT-repeat conformation and direct Ran-cargo contacts to ensure low cargo-binding affinity in the cytosol and cooperative assembly of the exportin/Ran/cargo complex in the nucleus (Cook et al., 2005, Co
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br Materials and methods br Results Recombinant N terminally
2021-04-16
Materials and methods Results Recombinant, N-terminally His6-tagged vCPH was purified to near homogeneity via a modification of the reported procedure and its identity confirmed by intact protein mass spectrometry (Supplementary Fig. 1). As reported, vCPH catalysed two hydroxylations of a PAPK
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Resistance to avermectins has been
2021-04-16
Resistance to avermectins has been associated with point mutations of GluCls in C. elegans, D. melanogaster, T. urticae and P. xylostella (Dent et al., 2000; Dermauw et al., 2012; Kane et al., 2000; Kwon et al., 2010; Wang et al., 2016a, 2017). Our electrophysiological study found a 8.2-fold reducti
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Grapiprant is a selective antagonist
2021-04-16
Grapiprant () is a selective antagonist for prostaglandin E (PGE) receptor subtype 4 (EP4) identified as a clinical candidate for the treatment of inflammatory pain associated with osteoarthritis (OA). It is currently under development for use in humans and dogs. The projected dosing regimen of grap
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Neonatal hydronephrosis induced by TCDD
2021-04-16
Neonatal hydronephrosis induced by TCDD exposure via lactation has a critical window for onset: the incidence of this disease peaks around PNDs 1–4, followed by a rapid decrease to a substantially null level in adulthood (Couture-Haws et al., 1991; Yoshioka et al., 2016). The EP1 protein was localiz
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Introduction Enzymes have higher selectivity specificity and
2021-04-16
Introduction Enzymes have higher selectivity, specificity and efficiency than chemical catalysts. Due to their properties and their green chemistry, biocatalysts are widely used in food, textile and pharmaceutical industry [1], [2]. A high efficient biocatalyst for industrial applications must be s
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br O GlcNAc transferase OGT belongs to the
2021-04-16
O-GlcNAc transferase OGT belongs to the metal-independent GT-B superfamily of glycosyltransferases, which has been well-reviewed previously [14,15]. OGT is an essential gene encoded on the X-chromosome, and it has two main regions: a long N-terminal tetratricopeptide repeat (TPR) region and a C-t
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A growing body of data indicates that
2021-04-16
A growing body of data indicates that endothelial NOS (eNOS) is a rate-limiting enzyme for the synthesis of nitric oxide (NO), its downstream zj to j molecule. High pathological concentrations of NO produced from inducible NO synthase (iNOS) induce apoptosis, whereas a reduction in the concentratio
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