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br Acknowledgments The authors thank Claudia Wittrock for
2023-12-01
Acknowledgments The authors thank Claudia Wittrock for her excellent technical assistance. The work was supported by grants of the Deutsche Forschungsgemeinschaft (SFB974 TP B05) and of the Anton-Betz-Stiftung to N.K. A.M. is an associate member of the iBrain graduate school at the University of
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br Conflicts of interest br Funding br Introduction Brassica
2023-12-01
Conflicts of interest Funding Introduction Brassicaceae is an economically important family of plants containing rapeseed, cabbage, broccoli, brussels, radish and mustard. Among them rapeseed plays a crucial role, because of its application in food and also in fuel industry. According to th
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Mometasone furoate Recently two distinct small molecule inhi
2023-11-30
Recently, two distinct small-molecule inhibitors of PHGDH were identified using high-throughput screens, both of which inhibit de novo serine biosynthesis and show selective toxicity to cancer Mometasone furoate with high SSP flux [50,51]. The inhibitor NCT-503, which has an IC50 of 2.5μM, reduces t
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Heat shock protein Hsp is a molecular chaperone that
2023-11-30
Heat shock protein 90 (Hsp90) is a molecular chaperone that plays a central role in regulating the maturation, activation and stability of numerous “client proteins” that drive the development and progression of many cancers. Therefore, inhibition of Hsp90 would result in degradation of the client p
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The mechanisms that control Ahr transcription are poorly und
2023-11-30
The mechanisms that control Ahr transcription are poorly understood, especially when considering cell type-specific regulation. A recent report suggested that the Ahr transcription might be directly promoted by RORγt [retinoic Disuflo Cy5 azide receptor (RAR)-related orphan receptor γt] based on ChI
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Liver plays a pivotal role
2023-11-30
Liver plays a pivotal role in metabolism of xenobiotic compounds, such as environmental contaminants and drugs. Some of these compounds generate hepatic damage and impair its function. It was well-known that 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) could induce pathological changes in mouse and ra
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There are human genes in
2023-11-30
There are 12 human genes in the SLC5A family, and 6 of these are expressed in human heart (Table 2). Little is known about SGLT proteins in the heart. Zhou et al. [56] reported the presence of SGLT1 mRNA in the human heart. Researchers have found that levels of SGLT1 mRNA in heart are approximately
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This chemistry paved way for multi gram synthesis of which
2023-11-30
This chemistry paved way for multi-gram synthesis of which was utilized for extensive piperazine benzamide SAR exploration. Depicted in , the two-step operation towards final targets involved standard amide coupling conditions with EDC or HATU followed by Boc deprotection under acidic conditions.
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L 006235 The extent to which GPCR oligomerization is a regul
2023-11-30
The extent to which GPCR oligomerization is a regulated process still remains unclear. Reported effects of ligands on both GPCR homo- and heteromers are highly variable and depend on GPCR subtypes and the specific ligand used. According to our data, chronic treatment of mice with both paroxetine or
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br Materials and methods br Results and discussion
2023-11-30
Materials and methods Results and discussion Conclusion Amino-functionalized mesoporous TiO2-NH2 microparticles were used to immobilize ADA, followed by GLU cross-linking. The mesopores provided a natural microenvironment with sufficient room for the enzyme to efficiently perform its cataly
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Overexpression of SMAD and SMAD strongly enhanced luciferase
2023-11-30
Overexpression of SMAD3 and SMAD4 strongly enhanced luciferase activity of the new pN10 reporter gene construct which was further reinforced by addition of TGFβ. Serial mutations of SBE-1 and SBE-2 led to a slight loss in 5-LO promoter inducibility. The data demonstrate that the two SBEs within the
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In fact serotonin is a major modulator of
2023-11-30
In fact, serotonin is a major modulator of dopaminergic (DA) neuronal activity through the 5-HT2C receptor. Studies have shown that the selective 5-HT2C receptor agonist Ro60-0175 blocks the burst-firing of mesolimbic DA neurons, which project from the ventral tegmental area (VTA) to the nucleus acc
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In conclusion we have designed
2023-11-30
In conclusion, we have designed and synthesized a series of 4-phenyl-thiazole analogues as potent ATX inhibitors. Total twenty-five compounds were synthesized and evaluated for their inhibitory activity on ATX using FS-3 and human plasma assays. Compound was found to be the most potent derivative p
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The synthesis of compounds in which the ethyl linker has
2023-11-30
The synthesis of compounds in which the ethyl linker has been modified to the carbamate and urea derivatives , and is shown in . Thus the diamine was reacted with glycolic Fmoc-Ala-OH to give the alcohol followed by Mitsunobu reaction with phthalimide to give . Deprotection with hydrazine gave the a
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As in humans and other mammalians spontaneous activity of
2023-11-30
As in humans and other mammalians spontaneous activity of sinoatrial pacemaker Cy3.5 NHS ester (non-sulfonated) synthesis in in the zebrafish heart crucially depends on proper HCN4 channel activity (If) and spontaneous diastolic depolarization [15,81]. Whether Na+/K+-ATPase currents regulate next t
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