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Transduction of cellular signals by
2019-09-03
Transduction of cellular signals by G protein-coupled receptors (GPCRs) is stringently regulated to prevent the deleterious effects of unrestrained GPCR signaling. The rapid termination of signaling mediated by agonist-occupied GPCRs is referred to as homologous desensitization and involves the foll
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Two additional hydrogen bonds are formed by the substituted
2019-09-03
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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Where does this transfer process occur
2019-09-03
Where does this transfer process occur? The maternal side of the placenta is textured and spongy looking. The surface has 20–30 distinctive compartments named cotyledons, inside of which are the chorionic villi that form the principal functional structural unit of the placenta. These villi are compl
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Given that dimethylamine substitution was tolerated as in SR
2019-09-03
Given that dimethylamine substitution was tolerated as in SR106447 (), we investigated fasudil mass amine substitutions as replacements for the -butyl group (). Cyclic amines (SR19880, 19882) or simple mono-substituted anilines (SR20037) were not active, nor was an acetylated version (SR20039). The
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Within the X CX PX RX motif of
2019-09-03
Within the X1CX3PX5RX7 motif of several prokaryotic FGE substrates, the residues of X3, X5, and X7 are variably found as mixtures of alanine, glycine, threonine, or serine residues [26], [27]. The docked model of our identified HCTPRRP motif revealed that position X1 (H1) and position X7 (P7) were n
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br Conflict of interest br Acknowledgements We wish to thank
2019-09-03
Conflict of interest Acknowledgements We wish to thank Arantza Pérez (University of the Basque Country) for her technical contribution to this study. This work was supported by grants from the Jesús Gangoiti-Barrera Foundation, Gobierno Vasco (GIC07/84), MEC () and SAIOTEK (SA-2008/00046).
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Just as Dorin et al and Nguyen et al write
2019-09-03
Just as Dorin et al. [2] and Nguyen et al. [3] write in regard to their models, our static model can be used to estimate the affinities of 324 4 to albumin and CBG. Dorin et al. [2] estimates the K, but not K, since they find that their model is not particular sensitive towards changes in K. Our se
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Most remarkably an essentially identical collagen binding mo
2019-09-03
Most remarkably, an essentially identical collagen-binding mode to DDR2 is employed by SPARC, an α-helical matricellular protein unrelated to DDR2 that also recognizes the GVMGFO motif in collagen (Giudici et al., 2008, Hohenester et al., 2008). The convergence of binding mechanisms suggests that th
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Herbal products may alter the metabolism
2019-09-03
Herbal products may alter the metabolism of certain drugs and, likewise, the metabolism of components of herbal products may be altered by some drugs, specifically those that affect cytochrome P450 Kartogenin (CYP). These can bring about an alteration of the pharmacokinetics and pharmacological act
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The development of C S mutation has been reported
2019-09-03
The development of C797S mutation has been reported in vivo in a small cohort (15 subjects) of EGFR T790M positive patients progressing after Osimertinib: this tertiary mutation was found, using a droplet digital PCR (ddPCR) assay, in 40% of patients after AR to this agent, while 33% of the cases ex
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Substitutions on the benzene ring
2019-09-02
Substitutions on the benzene ring of the phenyl acetic MS023 and moiety were evaluated to study their effect on DP and CRTH2 selectivity (). Compound has strong affinity for CRTH2, but it only has moderate affinity for DP. Small substitutions such as methoxy () and fluorine () next to the aryloxy
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Previously we have shown that complexes of protein PKs with
2019-09-02
Previously, we have shown that complexes of protein PKs with inhibitors that comprised sulfur or selenium atoms in aromatic structures were phosphorescent at room temperature, while the long-lifetime signal emitted by the free inhibitor was negligible.34, 35, 36 This phenomenon was caused by stabili
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br Experimental protocols br Acknowledgements This
2019-09-02
Experimental protocols Acknowledgements This research was funded by the Croatian Ministry of Science, Education and Sports (Programmes 098-0982915-2948 and 098-0982522-2525), the Austrian Science Fund FWF (DK-MCD W1226, SFB LIPOTOX F30, P22832), and the Croatian-Austrian Intergovernmental S&T
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br ILCs anticipate neuronal derived factors Recent studies h
2019-09-02
ILCs anticipate neuronal-derived factors Recent studies have revealed that ILCs express receptors for neural peptides, thus enabling cross-talk with the peripheral nervous system. ILC3s express RET (Figure 2), which is a receptor for members of the glial cell-derived neurotrophic factor family of
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br Materials and methods br Results
2019-09-02
Materials and methods Results Discussion Natural compounds and their derivatives have been investigated as candidates for the treatment of bone diseases and can also be the sources of nutraceutical agents and therapeutic agents [28]. Using peptides as therapeutic effects on bone-related dis
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