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It was recently shown that AHR and HIF cooperate
2023-10-10
It was recently shown that AHR and HIF-1α cooperate to support the metabolism of Tr1 bromophenol blue [6]. Interestingly, AHR and HIF-1α act sequentially to orchestrate the metabolic remodeling of lymphocytes. While HIF-1α regulates the early metabolic reprogramming of Tr1 cells, AHR takes over at
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Corticosterone induced inhibition of OCT mediated transport
2023-10-10
Corticosterone-induced inhibition of OCT-mediated transport is rapid and appears to involve direct interaction of the steroid with the transporter at a specific site. Volk et al. (2003) studied OCT2-mediated transport by measuring substrate-induced currents using patch clamp of Xenopus oocytes exoge
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In conclusion we have demonstrated that
2023-10-09
In conclusion, we have demonstrated that ,-diaryl-1-pyrazolo[3,4-]pyrimidine-3,6-diamines represent a novel class of ACK1 inhibitors. The presence of a polar substituent at C-4 of the N-6 aryl ring was shown to be unnecessary for maintaining high levels of inhibitory activity. Furthermore, selectivi
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Thirty six of the analogs synthesized showed ATX inhibition
2023-10-09
Thirty-six of the analogs synthesized showed ATX inhibition greater than 50% at 10μM with FS-3, twelve of which had improved potency over the lead (Fig. 5). Of these, 22 was sub-micromolar (IC50 670nM). The 3,5-dichlorophenoxy ring of 22 is reminiscent of the 3,5-dichlorophenylthiourea ring in Hoegl
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Functional enhancers are often composed of
2023-10-09
Functional enhancers are often composed of binding motifs of multiple key transcription factors to confer spatial and temporal regulation of genes in a certain context. In the uterus, the difference between the number of genes that have associated PGR occupancy and that of progesterone responsive ge
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Recent progress has been made in
2023-10-09
Recent progress has been made in translating animal findings on memory performance and amnestic effects – that are largely determined by tonically active receptors in which α5 contributes to the benzodiazepine binding site. Based on the observation that deletion of this subunit led to improved spati
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Angiogenesis is a process of
2023-10-09
Angiogenesis is a process of formation of new vessels from arterial vascularization created by endothelial cells. It is essential for the continuous growth of the tumor because it supplies the tumor with nutrients and oxygen, and eliminates cellular waste, which can be toxic to cancer cells [8]. Inf
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Besides the described changes in protein
2023-10-09
Besides the described changes in protein expression and thus in current amplitudes, Radotinib of PORCN also leads to accelerated decay kinetics of evoked and spontaneous AMPAR currents. These changes in channel kinetics are most likely a secondary effect due to the selective depletion of γ-8 but not
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br Experimental section br Abbreviations PSA puromycin sensi
2023-10-09
Experimental section Abbreviations PSA, puromycin–sensitive aminopeptidase; APN, aminopeptidase N; AML, acute myeloid Leukemia; ALL, acute lymphoblastic leukemia; AADR, amino Asunaprevir deprivation response; PAN, puromycin aminonucleoside; DCC, dicyclohexyl carbodiimide; NHS, N–hydroxy succ
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Sperm total motility and hyperactivated motility
2023-10-08
Sperm total motility and hyperactivated motility are mediated by PLD-dependent R547 sale polymerization [20]. Reduction of PIP2 synthesis inhibited actin polymerization and motility, and increasing PIP2 synthesis enhanced these activities. Furthermore, sperm demonstrating low motility contained low
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We found that several anticancer
2023-10-08
We found that several anticancer drugs inhibit 5-HT3 (S)-Crizotinib current in vitro. Several studies have suggested that 5-HT3 receptor antagonists have anti-mitogenic and apoptotic effects on colorectal and breast cancer cell lines (Ataee et al., 2010, Hejazi et al., 2015). Irinotecan is used freq
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All scientific data over the years points
2023-10-08
All scientific data over the years points that 5α-reductase inhibitors undoubtedly are an effective treatment for BPH and associated LUTS, having a favorable risk-benefit profile. In contrast, although some studies indicated positive results, there is still no consensus about their use in BPH or PC
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Consistent with the observation that mutations
2023-10-08
Consistent with the observation that mutations in the redox-partner binding site of P450c17 that reverse charge from basic to acidic (R347H, R358Q) cause 17,20-lyase deficiency (Geller et al, 1997, Geller et al, 1999), at least one POR mutation that changes a residue in the FMN domain from neutral t
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Many reports have well documented that
2023-10-08
Many reports have well documented that signaling pathways play a pivotal role in controlling longevity. The most studied of these pathways is the IGF-1 pathway [11,12]. A disruption of this pathway has been found to extend longevity in different groups of species starting from Caenorhabditis elegans
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The first description of autophagy as a tumour suppression
2023-10-08
The first description of autophagy as a tumour suppression process arises from the observation that the initial step regulatory gene, Atg6/BECN1, was monoallelically lost in 40% to 75% of human prostate, breast, and ovarian cancers [31]. However, while BECN1 heterozygous mutant mice develop, with lo
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