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CH5138303 Conversely we find that dysfunction in lysosomal a
2022-02-25
Conversely, we find that dysfunction in lysosomal-autophagy system observed in human APP and PSEN1 mutant neurons can be reversed by β-secretase inhibition, which reduces the supply of APP-β-CTF to the late endosome and/or lysosome (Jiang et al., 2010). These data argue that accumulation and/or alte
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In addition we assessed the viability of tetrahydroquinoline
2022-02-24
In addition, we assessed the viability of 1,2,3,4-tetrahydroquinoline (13t) and 1,2,3,4-tetrahydroisoquinoline (13u) as the tail on account of our previous SAR results. To our delight, 13t and 13u each had comparable activity to that of 13c, with 13u being slightly more potent than 13c. Further stru
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Consistent with our result Camacho Barquero and coworkers sh
2022-02-24
Consistent with our result, Camacho-Barquero and coworkers showed that curcumin reduced phospho-P38 MAPK. P-38 MAPK is a key effector of several downstream factors that eventually modulate the homing of monocytic cells during the onset of intestine inflammation (Camacho-Barquero et al., 2007). Along
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NeuroHIV is initiated by HIV
2022-02-24
NeuroHIV is initiated by HIV crossing the blood–brain barrier (BBB) to enter the CNS. This is thought to occur primarily via the transmigration of infected CD14+CD16+ monocytes (Williams, 2014), using the monocytes as “Trojan Horses” (Peluso, 1985), although some studies suggest alternate routes of
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Notably Cu labeled dimeric exendin
2022-02-24
Notably, 64Cu-labeled dimeric exendin-4 subunit, which was designated as 64Cu-Mal2Sar-(exendin-4)2, showed higher tumor uptake than that of the monomeric exendin-4 subunit [245]. Besides the most commonly-used GLP-1R agonists exendin-3 and -4 and their derivatives, exendin (9-39) exhibits strong bin
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Foreign polypeptide antigens can be incorporated into VLPs t
2022-02-23
Foreign polypeptide antigens can be incorporated into VLPs to create “chimeric” structures, either as fusions to either end of the VLP capsid (coat) protein (CP) or as additions to well-presented loops [18]. This kind of direct fusion to the coat is usually good for small peptides, however, larger p
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Generally replacement of the aryl group was well
2022-02-23
Generally, replacement of the aryl group was well tolerated, with tetrahydropyran () and hydroxyl () functionality providing potency equivalent to and . These substitutions had no effect on selectivity versus GlyT2 and taurine transporter (TauT)—no activity was observed at micromolar concentrations
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Next we investigated the accumulation of H ribavirin in fres
2022-02-23
Next, we investigated the accumulation of [3H]-ribavirin in fresh villous fragments of human placenta, which provide a physiologically relevant, well-described and validated model for assessing drug interactions with ENTs [32], [35], [69], [70]. The uptake of [3H]-ribavirin was time-dependent and si
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br Materials and methods br Results br Discussion Employment
2022-02-23
Materials and methods Results Discussion Employment of GIPR signaling, specifically the direction of this manipulation, as a strategy to improve body weight remains a contentious subject of intense scientific investigation [22], [32], [33]. Despite the physiological benefits of GIP on Momet
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INCB018424 br Conclusions br Introduction Bioinformatics ana
2022-02-23
Conclusions Introduction Bioinformatics analysis shows that there are about 300,000 G-rich sequences in human genome if searching with the consensus sequence (G3+N1-7G3+N1-7G3+N1-7G3+) [1], and their localizations are non-random. These G-rich sequences always localize in functional regions, su
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Analysis of the i motif structures
2022-02-23
Analysis of the i-motif structures during biased unfolding of G-quadruplexes leads to the conclusion that at acidic pH the i-motif is absolutely unaffected by that process. The hydrogen bonds within the i-motif are intact (Fig. 3D) and they only fluctuate around mean values. On the other hand, the i
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br Acute host defense Inflammation the host response to
2022-02-23
Acute host defense Inflammation, the host response to infection and tissue injury, is crucial for survival and restoration of tissue structure and function. This acute response is mediated and governed by a variety of pro-inflammatory circuits to ensure recognition of invading pathogens, coordina
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br Molecular aberrations in the FGFR signaling pathway
2022-02-23
Molecular aberrations in the FGFR signaling pathway Non–small cell lung cancer Small cell lung cancer Integrated 832 582 4016 mg analysis revealed focal amplification of FGFR1 in 6% of SCLC cases. In another study with PD173074, Pardo et al. used two human SCLC xenograft models, H-510 and
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PBI is an agonist of GPR and acts as
2022-02-23
PBI-4050 is an agonist of GPR40 and acts as an antagonist or inverse agonist of GPR84. It cannot be excluded that other targets besides GPR40 and GPR84 could be implicated in the mechanism of action of PBI-4050 and could be explored in future studies. However, the present study, and in particular th
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In soft agar colony formation assay transformed cells
2022-02-23
In soft agar colony formation assay, transformed Tolvaptan indicate anchorage-independent growth and colony formation without attachment on the bottom of cell culture plate. This assay can investigate transformation and tumorigenic activities [24]. Our recent study showed that the long-term 5-FU tr
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