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The present study sought to determine if chlorodifluoroaceto
2020-07-09

The present study sought to determine if chlorodifluoroacetophenones, such as 3 and 4, were amenable to a radiolabelling methodology to generate potential 18F imaging agents with high cholinesterase affinity. A number of procedures have been reported for the synthesis of trifluoromethyl ketones, inc
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A large fraction of UCEs are transcribed T UCEs in
2020-07-09

A large fraction of UCEs are transcribed (T-UCEs) in a tissue specific manner, and are deregulated in several human cancers (Calin et al., 2007, Fabbri et al., 2008, Fassan et al., 2014, Olivieri et al., 2016). Indeed, it has been shown that T-UCEs may also act as long non-coding RNAs (lncRNAs) regu
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br Conflict of interest br Acknowledgements This work
2020-07-09

Conflict of interest Acknowledgements This work was supported by Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP: 2014/00926-3). Introduction The metacestodes of Taenia solium are the causative agent of cysticercosis, which mainly resides the skeletal muscles and the central n
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EBI remains an orphan GPCR and the identity
2020-07-09

EBI2 remains an orphan GPCR and the identity and source of its ligand are yet to be described. Molecular studies of EBI2 have suggested that this receptor has constitutive activity, similar to that observed for many herpesvirus-encoded 7TM receptors (Benned-Jensen and Rosenkilde, 2008, Rosenkilde et
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The structure of the HOIP RBR LDD module bound
2020-07-09

The structure of the HOIP RBR–LDD module bound to UbcH5~Ub reveals insights into an activated HOIP component [47]. Contacts between the E2~Ub and the non-cognate RBR module in the crystal suggest how a structure in which the active sites of the E2 and the E3 are in close proximity might look. In thi
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Besides being the only enzyme E is also the
2020-07-09

Besides being the only enzyme, E1 is also the largest and arguably most complex protein encoded by papillomaviruses. As the replicative helicase, E1 plays a central role in the viral life cycle. To do so, E1 engages in multiple protein–protein and protein–nucleic hippo pathway interactions to creat
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Protein expression and purification A mL
2020-07-09

Protein expression and purification. A 3 mL overnight culture of E. coli BL21 (DE3) pLysS pGEX-6P-3-A1S_0222 was grown in Luria-Bertani (LB)-Medium (10 g/L tryptone, 5 g/L yeast extract, 5 g/L NaCl, pH 7.4, 100 μg/mL Amp) at 37 °C and 160 rpm. The overnight culture was diluted 1:100 into 200 mL LB (
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ARRY-614 mg In the present study it was particularly of
2020-07-08

In the present study, it was particularly of interest that intravesical administration of PGE2 evoked ONO-8130-reversible rapid phosphorylation of ERK in the L6 spinal cord. Detection of phosphorylated ERK is now often used as a marker for somatic and visceral nociception, including ARRY-614 mg pai
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Diacylglycerol kinases DGK and are lipid kinases that limit
2020-07-08

Diacylglycerol kinases (DGK) α and ζ are lipid kinases that limit diacylglycerol (DAG)-dependent activation pathways downstream of the TCR (Merida et al., 2015). Their upregulation in tumor infiltrating lymphocytes (TIL) has been linked to generation of hyporesponsive states that contribute to immun
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The data from drug screening in P berghei Fig
2020-07-08

The data from drug screening in P. berghei (Fig. 3D) provide proof of concept that chemogenomic profiling can be accomplished in P. berghei in the same manner as P. falciparum, in that significant increases in the EC50 ratio were found only for antifolate drugs in the parasite with attenuated TgDHFR
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Various domains of DDR have been shown to be
2020-07-08

Various domains of DDR1 have been shown to be important for receptor clustering and its oligomeric status. It is now understood that (i) dimerization [7] and higher-order oligomerization [12], [18] of the DDR1 extracellular domain (ECD) enhance its binding to collagen; (ii) DDR1 exists as non-covale
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Autophagy alterations are frequently reported as one of the
2020-07-08

Autophagy alterations are frequently reported as one of the pathological mechanisms contributing to neurodegenerative diseases, due to incomplete removal of protein TG101209 mg in the brain [30,41]. It was over a decade ago when mutations in PARK8 encoding for the LRRK2 protein were described as a
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In solid tumors such as those in breast
2020-07-08

In solid tumors, such as those in breast and pancreatic cancer, infiltrating CD68+ or CD163+ tumor-associated macrophages (TAMs) correlate with poor outcome (DeNardo et al., 2011, Kurahara et al., 2011, Shabo et al., 2008). The tumor-promoting function of TAMs is based on their capacity to secrete p
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In the cytoplasm the ternary CRM cargo
2020-07-08

In the cytoplasm, the ternary CRM1–cargo–RanGTP complex is disassembled by the action of Ran-binding proteins RanBP1/2 and RanGAP. A recent kinetic study showed that the Ran-binding domains (RanBDs) of the cytoplasmic proteins RanBP1 and RanBP2, but not RanGAP, accelerate dissociation of NES from CR
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Although the findings detailed above provide ample evidence
2020-07-08

Although the findings detailed above provide ample evidence that the activity of the CRF1 receptor in the amygdala plays a role in the acute and chronic effects of alcohol exposure, several important areas of investigation remain understudied. The majority of the work on CRF1-alcohol interactions ha
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