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Taken together our results show that at least in
2021-10-28
Taken together, our results show that, at least in the in vitro cell line model, methylation within the proximal promoter region of GHSR is an important determinant of its expression; however, to determine whether this represents a physiologically and or pathophysiologically relevant event, further
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hsp90 inhibitor In an immunohistochemical analysis of gastri
2021-10-28
In an immunohistochemical analysis of 117 gastric cancer samples, reduced Cx43 and E-cadherin expression were shown to contribute to the development of primary gastric cancer; however, increased Cx43 and E-cadherin expression contributed to lymph node metastasis [13]. In primary urothelial hsp90 inh
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Comparison of dlGALRs deduced amino acid
2021-10-28
Comparison of dlGALRs deduced amino dopamine beta hydroxylase sequences with that of human GALRs demonstrate that the GALR1 ortholog sequences have diverged less than those of GALR2. Since often duplicate genes undergo divergent evolution through sub-functionalization, loss or gain of new functions
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A species specific diverse number of FPPS genes
2021-10-28
A species-specific diverse number of FPPS genes are present in insect genomes (Zhang and Li, 2008, Cusson et al., 2006). The genome of the yellow fever mosquito Aedes aegypti contains a single FPPS gene (AaFPPS) that is highly expressed in the CA (Nouzova et al., 2011). FPPS catalytic activity in th
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Methods br Results br Discussion SV exocytosis
2021-10-28
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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Phenacetin In vitro studies suggest that the increase
2021-10-27
In vitro studies suggest that the increase in Hx activity seen in normal pregnancy may contribute to the down-regulation of the vascular expression of Angiotensin II receptor 1 thereby promoting a relaxed and dilated maternal vascular bed [25]. It has further been suggested that the decreased Hx act
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br Positive regulation of gene
2021-10-27
Positive regulation of gene Nogo-66 (1-40) by Nrf2 Repression of Nrf2 by Keap1 Because many xenobiotic inducers of NQO1 and GST enzyme activities contain a thiol-reactive electrophilic moiety (i.e. are soft electrophiles), Paul Talalay and colleagues predicted in 1988 that they would be recog
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While a role for YAP TAZ signaling in oligodendrocytes
2021-10-27
While a role for YAP/TAZ signaling in oligodendrocytes has not been described, these SR 8278 are also responsive to mechanical stimuli. OPC proliferation and migration can be altered by plating on substrates of varying stiffness [20], resulting in differentiation in a density-dependent manner. Plati
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In normal tissues the expression patterns of GPR and
2021-10-27
In normal tissues, the expression patterns of GPR120 and GPR40 are not uniform. GPR120 is highly expressed in adipocytes, lung and intestinal tract, while GPR40 is shown to be expressed in pancreatic islet aa dutp and intestinal tract [7], [20]. It is considered that the distribution of the GPR120
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A number of synthetic GPR
2021-10-27
A number of synthetic GPR119 agonists have been reported to date, several of which have advanced into clinical trials. Reported GPR119 agonists are often composed of three parts as depicted in : a piperidine or a piperazine ring -substituted with a carbamate or a heteroaryl group at the right side,
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In parallel we were also preparing and evaluating other
2021-10-27
In parallel, we were also preparing and evaluating other piperidine bioisosteres and modifications to – to further access additional novel intellectual property (IP) space. Modeling work suggested that 4-position homologated piperidines, as well as 3-position homologated azetidines overlapped favora
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Overall ABC transporters are hypothesised to prevent
2021-10-27
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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k j and d were then submitted
2021-10-27
15k, 15j and 14d, were then submitted to metabolic stability studies in human and mouse liver microsomes and permeability test with Caco-2 cells (Table 7). 15k, 15j and 14d all retained excellent permeability (Papp value greater than 15.2 × 10−6 cm/s) and displayed modestly improved metabolic stabil
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br A small conductance chloride channel
2021-10-27
A small conductance chloride channel (SCC) In addition to the above-described channels, a 5pS SCC has been encountered in electrophysiological recordings. This channel, exhibiting long periods of opening separated by long intervals of closing, showed the same characteristics as the SCC described
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ceramide kinase br Materials and methods br Results and
2021-10-27
Materials and methods Results and discussion Conclusions Acknowledgements This study was supported by the Portuguese Foundation for Science and Technology (FCT) under the scope of the strategic funding of UID/BIO/04469/2013 unit and COMPETE 2020 (POCI-01-0145-FEDER-006684), and also by t
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