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One possible pitfall of using EPAC activators in
2020-11-30

One possible pitfall of using EPAC2 activators in the treatment of T2DM is their potential to increase glucagon levels. As discussed previously, although the ability of EPAC2 to increase glucagon expression and production is controversial, several studies show that this protein increases Gcg mRNA le
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ddhGTP While showing that deletion of EP maintains femur bon
2020-11-30

While showing that deletion of EP1 maintains femur bone volume fraction and trabecular bone parameters during aging, perhaps more importantly we have also demonstrated that increased initial BV/TV in EP1 is protective against OVX-induced bone loss. That is, while mice lose an approximately equal per
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From an industrial perspective the
2020-11-30

From an industrial perspective, the low turnover numbers and limited substrate scope of α-KG halogenases still represents a significant challenge. However, in light of the fact that currently no chemical processes are available for the selective halogenation of aliphatic carbon centers in complex mo
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Both the kK and kK mediated ubiquitination
2020-11-30

Both, the kK3 and kK5-mediated ubiquitination leads to rapid internalisation of target proteins followed by lysosomal degradation, similar to that seen for MARCH-1/8 [77]. Ubiquitination activity of kK3 and kK5 depends on the positioning of the targeted lysine (or cysteine) residues [22]. The positi
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Concerning family A GPCRs although
2020-11-28

Concerning family A GPCRs, although it has been described that several receptors are able to operate as monomers (Arcemisbéhère et al., 2010; Bayburt et al., 2011; Chabre & le Maire, 2005; Ernst, Gramse, Kolbe, Hofmann, & Heck, 2007; Hanson et al., 2007; Kuszak et al., 2009; Whorton et al., 2007), e
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43 7 This project was funded by the Deutsche Forschungsgemei
2020-11-28

This project was funded by the Deutsche Forschungsgemeinschaft within FOR 2251 (project grants EB 285/2-1 and WI 3272/3-1) and in part by additional contributions from the Bundesministerium für Bildung und Forschung (D.I.S award Nos. BIOSCAT [05K12YE1]) and the Horizon 2020 programme of the European
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Then we explored the MCLEIA methodology parameters including
2020-11-28

Then, we explored the MCLEIA methodology parameters including precision, accuracy and specificity. In the 0.5–128 ng/mL, the standard curve equation was = 0.5014 + 1.769 ( was log, was RLU/RLU with a correlation coefficient of 0.9907) (). On the one hand, same sample (0.5, 4.0, 32.0 ng/mL) detected
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This hydrophobic biphenyl tail gave good binding
2020-11-28

This hydrophobic biphenyl tail gave good binding affinity for human DHODH enzyme (IC Istaroxime hydrochloride was found to be the main metabolite in human microsomes and it was 100-fold less active against hDHODH than the ester. In an attempt to identify the specific non-covalent binding interacti
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Due to cell cell interactions high concentrations
2020-11-28

Due to cell-cell interactions, high concentrations of LTs can be locally generated in a short period of time during an inflammatory response, thus potentiating LT function. The cellular communication can be mediated between immune cells as well as between immune cells other cell types. Several studi
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To date methods for the
2020-11-28

To date, methods for the simultaneous analysis of multiple probe drugs in the plasma have been described by using HPLC-DAD or LC–MS/MS. Although previous cocktail methods have used combinations of those four or other probe drugs with LC–MS/MS methods, most of those studies focused on only the analys
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br Conclusions Taken together the roles of CDK and miR
2020-11-28

Conclusions Taken together, the roles of CDK8 and miR-152-3p in the process of HCC likely performed opposite effect completely. Both CDK8 and miR-152-3p could serve as the independent prognostic factors for predicting the OS and DFS in HCC patients. We identified that miR-152-3p as a post-transcr
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br Materials and methods br Results br Discussion Intra BNST
2020-11-28

Materials and methods Results Discussion Intra-BNST injections of NOC-9 (at all doses) were able to produce freezing and anxiogenic-like effects. Freezing was observed immediately after the NO donor injection and lasted about 2–3min (data not shown). When exposed to the EPM 5min after intra
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Following Duncan as a ritualized site Tyne Cot provides
2020-11-28

Following Duncan (1995), as a ritualized site Tyne Cot provides an opportunity for individual tourists to conduct their own acts of remembrance (Edensor, 2000, Iles, 2006). The analysis has also shown that individual acts of writing particular words and phrases in the visitor books are socially shar
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Two additional hydrogen bonds are formed by the substituted
2020-11-27

Two additional hydrogen-bonds are formed by the -substituted methoxy-group with Ser and Asp. Ser exerts the role of a gate keeper in CK1: Entry of the ATP in the binding-site causes a conformational change into the closed form by Ser, which locks the binding-site and prevents ATP-diffusion out of th
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Molecular docking study of compound was performed
2020-11-27

Molecular docking study of PF-670462 was performed using the Schrödinger Small-Molecule Drug Discovery Suite taking advantage of known X-ray crystal structures of activated EPAC2 protein. The model shows that compound occupies the CBD of EPAC2 and forms hydrogen bonds with Arg448 and the cyano-hy
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