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Interestingly myorelaxation and the stimulation of cGMP prod
2022-09-20
Interestingly, myorelaxation and the stimulation of cGMP production are properties also reported for sGC stimulators, such as YC-1 and BAY 41–2272 (i.e., indazole compounds that were discovered in the 1990s) [35]. They relax aortic ring contractions induced by phenylephrine, and their effects are si
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br Materials and methods br Results br
2022-09-20
Materials and methods Results Discussion Although there is general agreement that GPR109A has anti-lipolytic activity and that the NEFA reduction in response to nicotinic CPI-455 is mediated by GPR109A, whether GPR109A activation has any impact on plasma TG levels is unclear. Since the phe
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In previous work we showed that benzophenanthridines do not
2022-09-19
In previous work we showed that benzophenanthridines do not affect the surface expression of GlyT1 (Jursky and Baliova, 2011). The results from the surface biotinylation studies reported in Fig. 3 show that the surface expression of the Y370F mutant is not significanly affected by the alkaloids in t
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To this end we evaluated novel
2022-09-19
To this end, we evaluated novel D22 analogs for selectivity to inhibit substrate transport in OCT2, OCT3, and PMAT heterologous cell Senexin B australia systems, and in mouse hippocampal and striatal preparations. Chosen analogs were based upon availability of essential chemical precursors (e.g. 6-
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With rare exceptions the biological role of secretase cleava
2022-09-17
With rare exceptions, the biological role of γ-secretase cleavage of substrates other than Notch 1 has been ignored during proof of concept preclinical repurposing studies. For example, in the GSI AD trial, many individuals noted changes in hair color, apparently due to inhibition of tyrosinase, an
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An advantage of photolabeling with tritiated photoprobes fol
2022-09-17
An advantage of photolabeling with tritiated photoprobes followed by microsequencing with Edman degradation is the ability to both identify the photolabeled Chelerythrine Chloride and to quantify photoincorporation which enables assessment of pharmacological specificity and allosteric interactions
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To obviate the mitogenic FGF activity several engineered FGF
2022-09-17
To obviate the mitogenic FGF19 activity, several engineered FGF19 variants have been generated aiming to maintain the metabolic activity excluding the protumorigenic ones. One variant, M70, that differs from wild-type FGF19 by 5-amino acids deletion at the N-terminus and the substitution of 3-amino
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A great number of proteins entering the nucleus
2022-09-17
A great number of proteins entering the nucleus possess a characteristic nuclear localization sequence (NLS) in their primary structure. One of such sequences is the KKKGK motif [30]. It is present in all known muscle (but not liver – except human liver) FBPase sequences (human, rabbit, rat and mous
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The multiple sequence analysis showed that the
2022-09-17
The multiple sequence analysis showed that the putative amino opioid receptors sequence of HbFDP had 80–99% identity to the FDPs from H. brasiliensis, Lupinus and T. wilfordii, Malus×domestica, Centella asiatica, M. sativa, M.recutita, accession H. annuus, and A. thaliana. The present results are i
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In conclusion the data reported in this study have demonstra
2022-09-17
In conclusion, the data reported in this study have demonstrated an important role for FAAH substrates in the XCT790 in the modulation of TLR4-induced neuroinflammatory and associated anhedonic responses, but not acute sickness behaviour. Such potent neuroimmunomodulatory effects were shown to be li
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Throughout our studies we used CBD under
2022-09-16
Throughout our studies we used CBD under the assumption that it binds to the GPR55 receptor and has antagonist properties at the GPR55 receptor, as previously suggested (Whyte et al., 2009). To clarify whether the GPR55 receptor is involved in the O-1602-mediated effects on GI motility, we performed
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Evaluating the plausibility of this selective scenario is ch
2022-09-16
Evaluating the plausibility of this selective scenario is challenging because of the uncertainties concerning the biological role of calpain-10 and the significance of its variants with regard to gene function and disease susceptibility. However, from a strictly evolutionary standpoint, our findings
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In this study we further expanded the antitumor
2022-09-16
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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br Acknowledgements This work was supported
2022-09-16
Acknowledgements This work was supported by the National Key Research and Development Program of China [2017YFD0400106]; Innovation of modern Project[F18R02-03]. Introduction The Vesiculovirus genus is one of the six genera of the rhabdovirus family. The prototype vesiculovirus is vesicular s
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During pain signal transmission glutamate is released into t
2022-09-16
During pain signal transmission, glutamate is released into the synaptic cleft, which, in turn, causes activation of N-methyl-d-aspartate (NMDA) receptors and hence neurotransmission across the synapse occurs. The synaptic concentration and resultant activity of glutamate are controlled by excitator
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