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In our studies the EC
2022-03-28

In our studies, the EC50 values for long-chain unsaturated fatty acids added to the short form of human GPR120 receptor (BC101175), were higher than the EC50 values previously reported (Hirasawa et al., 2005) for the long form of GPR120 (NM_181745), which was co-expressed with Gα16 protein.(Table 2)
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rucaparib synthesis Our results on the association of seleni
2022-03-28

Our results on the association of selenium deficiency and vitamin A deficiency being associated with greater CD4 recovery during treatment were surprising. As we had hypothesized a relationship in the opposite direction (deficiency being associated with lower CD4 recovery), we can only reflect on po
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We suggest that the FRET enhancement
2022-03-28

We suggest that the FRET enhancement observed when the modified mD1 protein containing Acd at position 28 was excited at 260nm (), may differ from the diminution in fluorescence observed following excitation at 280nm due to the excitation of different transitions in Trp (i.e., the L and L transition
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We noticed that the spontaneous openings of
2022-03-28

We noticed that the spontaneous openings of the D97R α1 GlyR appeared to be quite similar to those elicited by a maximally-effective glycine concentration on wildtype GlyR; both generated similar open and shut dwell-time histograms, both exhibited openings grouped into clusters with Popen values gre
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The receptor binding assay used
2022-03-26

The receptor binding assay used in our previous study demonstrated that propofol competitively binds to FPR1, thus blocking the downstream signal transduction of FPR1 and inhibiting neutrophil immune activities [8]. In this study, we assessed the pharmacological action of fMMYALF in the presence of
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br Acknowledgements br Introduction Muscle FBPase is very
2022-03-26

Acknowledgements Introduction Muscle FBPase is very sensitive to AMP inhibition and in the presence of physiological concentrations of this effector in muscle fibres FBPase should be almost completely inactive [1], [2]. Recently, we have presented evidence that, in vitro, muscle aldolase binds
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In conclusion we have shown
2022-03-26

In conclusion, we have shown that the brain penetrating ability of heteroaryl piperazine and piperadine ureas can be modulated through small structural changes to the heteroarenes, the piperazine or piperidine core, and the biaryl ether tail. Compounds exhibiting / ratios ranging as high as 4.2:1 to
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br Introduction Adenosine triphosphate ATP is an organic mol
2022-03-26

Introduction Adenosine-5′-triphosphate (ATP) is an organic molecule (nucleoside triphosphate) which consists of adenine, ribose, and three phosphoric Kif15-IN-2 receptor residues. ATP serves as a temporary carrier of energy in all living cells, so it is a common substance in any organism. In the
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ICLs represent of all generated DNA adducts
2022-03-26

ICLs represent ICL Inducers in Cancer Therapy Nitrogen mustards with aromatic substituents (chlorambucil, melphalan) or a bioactivatable phosphoramide group (cyclophosphamide) were one of the first identified DNA crosslinkers. These agents are still used in combined schemes for the therapy of chr
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The relationship between increased GPR expression in the EDL
2022-03-25

The relationship between increased GPR120 expression in the EDL skeletal muscle and systemic glucose control is yet to be investigated. However, if the increased expression of GPR120 correlates with enhanced insulin-stimulated glucose uptake in skeletal muscle, particularly the EDL muscle, this migh
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Overall ABC transporters are hypothesised to prevent
2022-03-25

Overall, ABC transporters are hypothesised to prevent the penetration of AEDs and other pharmacological compounds into the brain, being a hurdle for therapeutic delivery in neurological diseases. DRE is thought to be in part related to an increased expression of efflux transporters in the BBB, altho
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ICH induced striatal lesion produced a reduction
2022-03-25

ICH-induced striatal lesion produced a reduction of EAAT1 expression analogous to the decreased glutamate uptake at 6 h. The combined reduction of excitatory amino fak pathway transporters and of glutamate uptake activity might explain the well-known glutamate excitotoxicity following brain ischemi
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Herein we report the discovery of AM AM maintains the
2022-03-25

Herein, we report the discovery of AM-3189 (). AM-3189 maintains the in vivo efficacy of AMG 837 while displaying a superior pharmacokinetic profile and minimal CNS exposure. As we reported previously, activity on the GPR40 receptor varies significantly with substitution at the β-carbon relative to
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Glutamate aspartate transporters or excitatory amino acid
2022-03-25

Glutamate-aspartate transporters or excitatory amino Nitecapone transporters (EAATs) are essential for the maintenance of glutamate homeostasis. EAATs are widely distributed in central neurons and glial cells (Danbolt, 2001, Martinez-Lozada et al., 2011). They are driven by Na + and K+ gradients (J
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A oligomers increased ubiquitination of GLT in astrocytes Pr
2022-03-25

Aβ1-42 oligomers increased ubiquitination of GLT-1 in astrocytes. Previous studies found that astrocytic GLT-1 is internalized from the cell surface by ubiquitination of lysines located in the cytoplasmic C-terminus of the transporter (Gonzalez-Gonzalez et al., 2008, Martinez-Villarreal et al., 2012
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