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TDG furthermore is inhibited in its excision of U
2021-10-02
TDG, furthermore, is inhibited in its excision of U on the NCP relative to duplex, though not to the same extent as SMUG1. There is no significant difference between TDGFL and TDG82−308, consistent with a previous report that the N- and C-termini missing from TDG82−308 do not affect the excision of
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somatostatin receptor To test our refinement protocol we con
2021-10-02
To test our refinement protocol, we considered a benchmark set of 12 N-linked glycan-containing protein structures determined by X-ray crystallography at resolutions ranging between 1.9 Å and 3.5 Å and comprising a total of 133 glycan units. We identified four incorrect anomeric configurations and 2
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Acarbose and voglibose the classic
2021-10-02
Acarbose and voglibose, the classic α-glucosidase inhibitors, were clinically used to inhibit α-glucosidase activity for the treatment of type 2 diabetes. However, the intake of these drugs may cause some undesirable gastrointestinal side effects and weight gain (Xu et al., 2015). The synthetic drug
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EDC.HCl synthesis In a meta analysis of genome wide associat
2021-10-02
In a meta-analysis of genome-wide association studies, a variant (rs10423928) in the GIPR gene has been found to be associated with elevated postprandial glucose and insulin (Saxena et al., 2010) as well as lean body composition including decreased BMI, lean mass and waist circumference (Lyssenko et
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Fmoc-Leu-OH Ghrelin contains an n octanoylation at its Ser
2021-10-02
Ghrelin contains an n-octanoylation at its Ser3 residue (Kojima et al., 1999). While des-acyl ghrelin is found in high concentrations in the blood, only the lipidated form is active at GHSR (Bednarek et al., 2000). We previously showed that ghrelin interacts with the membrane via its lipid modificat
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Chlorocresol In addition to FAK P
2021-10-01
In addition to FAK, P-38 MAPK (38 kDa polypeptide) serves as cross-talk effector for signal transduction, enabling this factor to play a vital role in numerous biological processes (Cuenda and Rousseau, 2007). Pharmacologically modulation of P-38 has shown to be an effective approach in the orientat
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Here we report a new human genetic
2021-10-01
Here, we report a new human genetic disorder in a patient with hypoalgesia, altered fear and memory symptoms, and a non-anxious disposition. This disorder is attributable to co-inheritance of a microdeletion in a novel pseudogene and a known FAAH hypomorphic SNP. The microdeletion is flanked by repe
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The imidazopyridines and related imidazopyrimidines
2021-10-01
The imidazopyridines and related imidazopyrimidines – and – were constructed from the key amine intermediates – ( X=CH and Ar=2-FPh, X=N and Ar=2-FPh, X=CH and Ar=5-pyrimidine, X=CH and Ar=2-methyl-5-pyrimidine, and X=CF and Ar=2-methyl-5-pyrimidine). These were synthesized a modified Horner–Em
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GR activity prevents GSSG overaccumulation by reducing this
2021-10-01
GR activity prevents GSSG overaccumulation by reducing this molecule to GSH (Kranner et al., 2006). High GR activity seems to be essential for undisturbed seed germination as GR and other enzymatic antioxidants maintain sunflower (Helianthus annuus L.) seeds vigour (Bailly et al., 2002). Germination
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The absolute requirement for substrate prephosphorylation ra
2021-10-01
The absolute requirement for substrate prephosphorylation raised the possibility that short phosphorylated peptides might serve as selective substrate competitive inhibitors. A set of phosphorylated peptides patterned after known GSK-3 substrates was generated and shown to inhibit GSK-3 in vitro in
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Waldeck Weiermair et al demonstrated that in endothelial cel
2021-10-01
Waldeck-Weiermair et al. (2008) demonstrated that in endothelial cells, the activation of GPR55 by application of 10µM anandamide resulted in a marked increase of ERK1/2 phosphorylation that was evident 2min following drug activation and was sustained for up to 3h. Another example comes from our unp
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GLP is known to be expressed in a subset
2021-10-01
GLP-1 is known to be expressed in a subset of taste bud cells and has been shown to co-localize with GPR120 in the circumvallate papillae [22]. Local GLP-1 regulates taste preference for sucrose [54]. Analogous to intestinal mediation of GLP-1 by GPR120, Martin et al.[22] report induction of GLP-1 s
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A number of synthetic GPR agonists have been reported to
2021-10-01
A number of synthetic GPR119 agonists have been reported to date, several of which have advanced into clinical trials. Reported GPR119 agonists are often composed of three parts as depicted in : a piperidine or a piperazine ring -substituted with a carbamate or a heteroaryl group at the right side,
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In this study we further expanded the antitumor bioactivity
2021-10-01
In this study, we further expanded the antitumor bioactivity, with the BALB/c S-180 tumor model, which is long-established due to its highly aggressive in all strains of laboratory mice and rats (Cui et al., 2003). We investigated the tumor-regressing ability of β-glucan by different modes of admini
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Always some extra effort may make great progress in
2021-10-01
Always, some extra effort may make great progress in sensing platform, for example, Ma's group discovered luminescent iridium (Ⅲ) complexes which were highly selective for G-quadruplex DNA and Al3+, then they utilized these complexes to develop a series of G-quadruplex-based probes and chemosensor r
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