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cyp450 inhibitors In earlier experiments on snails a behavio
2023-10-30
In earlier experiments on snails, a behavioral model was employed of certain food rejection to study the mechanisms of the reconsolidation of long-term associative memory. It was found that conditioned food stimuli (reminder) presentation, combined with injections of NMDA glutamate receptor antagoni
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The gene SRD A encodes
2023-10-30
The gene SRD5A2 encodes the 5-α-reductase enzyme, which converts testosterone into dihydrotestosterone. Although dihydrotestosterone levels are considerably lower than testosterone, dihydrotestosterone has a five-fold stronger binding capacity to the androgen receptor and, thereby, a considerably mo
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Given these findings above we hypothesized that hypernocicep
2023-10-30
Given these findings above, we hypothesized that hypernociception produced by intra-amygdala 8-OH-DPAT is result of hyperpolarization in this area. This neuronal inhibition of the amygdaloid complex might result in an inactivation of crucial neurotransmitter systems of the descending inhibitory pain
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br Animals Female Sprague Dawley SD rats aged months
2023-10-30
Animals Female Sprague Dawley (SD) rats, aged 3 months with body weight between 180-210 g were housed in cages and acclimatized to standardized lab conditions (temperature 23 ± 2°C, humidity 50 ± 5% and 12 h light-dark cycles). The rats were fed with standard rodent food pellet (Harlan Diet, Ross
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Thymoquinone TQ is the major
2023-10-30
Thymoquinone (TQ) is the major active lomitapide derived from Nigella sativa (Woo et al., 2012). Recent animal studies support the potential of TQ for the treatment of a variety of inflammatory disorders like inflammatory bowel disease (IBD), RA, and osteoarthritis (OA) (Salem, 2005, Badr et al., 2
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br Methods and materials br Results br Discussion
2023-10-30
Methods and materials Results Discussion GPCR regulation in response to agonist stimulation is common to nearly all GPCRs and is essential in physiological systems to limit persistent signalling. In this study we have investigated the [Pyr1]apelin-13-induced trafficking and desensitization
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br Genetic analysis of polarity complexes Model
2023-10-30
Genetic analysis of polarity complexes Model organisms such as Caenorhabditis elegans and Drosophila melanogaster provide useful means of describing basic biological processes. They lend themselves particularly well to addressing some of the questions arising in this field because of their struct
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br Declarations Funding None for the paper in question
2023-10-30
Declarations Funding: None for the paper in question. Competing interests: Florent Morio has received speaker's fees from Gilead, Basilea, and MSD and travel grants from Gilead, MSD, Pfizer, Basilea, and Astellas. Ethical approval: Not relevant for the paper in question. Introduction Lactic
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Several enzymes in serine and glycine metabolism have
2023-10-27
Several enzymes in serine and glycine metabolism have been proposed as biomarkers for cancer stage and prognosis. Phosphoglycerate dehydrogenase (PHGDH), phosphoserine phosphatase (PSPH), and serine hydroxymethyltransferase (SHMT) levels are high in TNBC and low in luminal-A breast cancers (Kim et a
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APPL was the first adaptor protein identified that
2023-10-27
APPL1 was the first adaptor protein identified that interacts directly with adiponectin receptors [18]. A two-hybrid study by Dong and colleagues revealed that the C-terminal extracellular domain of AdipoR1 interacts with adiponectin, whereas the N-terminal cytoplasmic domain of AdipoR1 interacts wi
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The same applies also to intermediate formally obtained by
2023-10-27
The same applies also to intermediate , formally obtained by elimination of the R substituent from compound . If compared to the thienopyrimidine derivatives (series , C), the thieno[3,2-]pyridazin-5(4H)-ones – explored herein seem to maintain similar size and shape and also analogue structural char
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pexidartinib The observation that vortioxetine blocks HT ind
2023-10-27
The observation that vortioxetine blocks 5-HT-induced currents in 5-HT3 receptor-expressing oocytes suggests that vortioxetine acts to functionally antagonize these receptors, and is in line with previously published data (Bang-Andersen et al., 2011). For example, Mørk et al. (2012) demonstrated tha
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In conclusion we have produced some highly potent inhibitors
2023-10-27
In conclusion, we have produced some highly potent inhibitors of P450 in comparison to the standard WP1066 KTZ. Also, due to the limited specificity of these compounds against lyase in comparison to the 17α-OHase component, these compounds would be expected to have a major impact on corticosteroid
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Optimization of the B ring specifically
2023-10-27
Optimization of the B-ring specifically targeted preventing the oxidation of the ring system (). As described above, the 4-position of the phenyl ring provides the appropriate vector towards bulk solvent. - and -linked substitutions at the 4-position of the B-ring from the 4-fluoro-nitrophenyl inter
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br Acknowledgment br Introduction The yeast Cdc ATPase and i
2023-10-27
Acknowledgment Introduction The yeast Cdc48 ATPase and its metazoan ortholog p97 (or VCP) are critical components of many ubiquitin-dependent cellular pathways that require the segregation of individual proteins from binding partners or membranes (for review, see Buchberger, 2013, Meyer and We
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