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br The GLI code The
2022-04-12
The GLI code The GLI code model [21], [22] considers the total GLI function as a balance of positive activator (GLIA) and negative repressive (GLIR) activities with GLI1 being mostly a positive transcription factor and GLI3 mostly a transcriptional repressor. The GLIA:GLIR ratio is thus critical,
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br Materials and methods br Results br Discussion
2022-04-12
Materials and methods Results Discussion Our study demonstrates that human GIP(3-30)NH2 is a selective GIPR antagonist that inhibits both GIP-mediated cAMP signaling, β-arrestin recruitment, and GIPR internalization. Furthermore, we demonstrate that human GIP(3-30)NH2 binds with high affini
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No specific inhibitor of KCC has progressed to clinical
2022-04-12
No specific inhibitor of KCC has progressed to clinical trials, however, although compounds like H74 were shown to specifically target KCC over the related Na+-K+-2Cl− cotransporter (NKCC) (Ellory et al., 1990). This molecule, or its related analogues, represent compounds of promise. Simple Mg suppl
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In order to test whether the
2022-04-12
In order to test whether the enhanced hyperpolarization in the presence of increasing amounts of extracellular Ca2+ could be due to an ionophore effect of NS309, red cell uptake of 45Ca and partition of 45Ca into a water/n-octanol phase +/−100 μM NS309 were determined. However, no indication of iono
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The significance of A and tau as
2022-04-12
The significance of Aβ and tau as therapeutic targets is not only derived from pathological evidence of postmortem brain but also from biochemical analysis of cultured human neurons. This is largely based on the induced pluripotent stem cell (iPSC) technology that has been established to study Aβ, t
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Galanin was shown to play
2022-04-12
Galanin was shown to play an important role in pain and pain processing [14] and the involvement of neuropeptides in the development of migraine is well established [[24], [25], [26]], however, so far it has not been examined whether systemic galanin levels correlate with migraine. Therefore, we use
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br Financial support This work was
2022-04-12
Financial support This work was supported by Fondation pour la Recherche Médicale (Equipe labellisée, DEQ20150331724), Inserm, University of Lille, and Agence Nationale pour la Recherche (ANR-10-LBEX-46 and ANR-10-INBS-08; ProFI project, “Infrastructures Nationales en Biologie et Santé”; “Investi
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During the course of our optimization
2022-04-12
During the course of our optimization of the diarylsulfonamide chemotype as FFA4 agonists, we identified xanthene as a potent and selective antagonist of FFA4 (). Xanthene was able to block the agonist induced intracellular Ca response elicited by both linoleic 350 and compound in competition st
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The co crystal structure of GPR complexed
2022-04-12
The co-crystal structure of GPR40 complexed with TAK-875 provided precise structural information for the rational design of novel GPR40 agonists. The key interactions between the carboxylate with the residues Arg183, Arg258, Tyr91 and Tyr240 of GPR40 were observed. And Trp174ECL2 was oriented nearly
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Factor Xa FXa has emerged as a
2022-04-11
Factor Xa (FXa) has emerged as a particularly promising target for the development of effective anticoagulant drugs because FXa acts at the convergence point of the extrinsic and intrinsic coagulation pathways. It efficiently catalyzes the conversion of prothrombin to thrombin with one molecule of F
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Not only has the cortical
2022-04-11
Not only has the cortical LXR-623 mg network been found to influence plasma membrane properties but also to interact with exo- and endocytic vesicles (Gormal et al., 2015, Tomatis et al., 2013). The interplay between actin and membranes is integrally regulated by the phosphoinositide composition of
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Methods br Results br Discussion SV exocytosis from excitato
2022-04-11
Methods Results Discussion SV exocytosis from excitatory boutons is more sensitive to inhibition by isoflurane than exocytosis from inhibitory boutons,4, 31 but the mechanism(s) of this synaptic selectivity is unknown. Although P/Q-type VGCCs contributed quantitatively more to SV exocytosis t
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In order to establish proper folding
2022-04-11
In order to establish proper folding and enzymatic activity, G9a and GLP methyltransferases each contain four structural zinc ions. Both Xylazine HCl contain two distinguishable types of zinc fingers; three Zn(II) ions are chelated in a triangular cluster by 9 cysteines (b, top left), whereas one Zn
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Aberrant expression of HKII may be a
2022-04-11
Aberrant expression of HKII may be a required feature for cancer development and progression. Overexpression of HKII has been reported in tumor tissues of cancer patients with liver [9], ovary [8], [24] and larynx [25]. The clinical significance of HKII in cancer was noted as overexpression of HKII
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It is not established if
2022-04-11
It is not established if ONOO− also induces tyrosine nitration of ANT and affects VDAC1 and ANT interaction, as well as the interaction of VDAC1 with HK II, all of which are events that may lead to altered mitochondrial and cellular function. Thus, in this study we examined tyrosine nitration of bot
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