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Lorlatinib is an orally active brain penetrant cyclic aminop
2023-02-20
Lorlatinib is an orally active brain penetrant cyclic 2-aminopyridine derivative that is a type I½ B ALK inhibitor (Fig. 5F) [61]. This medicinal is an effective antagonist against the more common L1196M and G1269A crizotinib-resistant mutations as well as the less common T1151Ins, L1152R, C1156Y, F
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br Applications of ATN in clinical trials In pivotal trials
2023-02-20
Applications of ATN in clinical trials In pivotal trials, the use of biomarkers will also have to be considered in the context of regulatory risk and scrutiny. Although an important intended application of the framework is in research studies, its use will undoubtedly impact clinical development
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The present study determined the effect of
2023-02-20
The present study determined the effect of DCA on VSMC calcification in vitro and in atherosclerotic ApoE-/- mice in vivo. We found that BIBF1120 non-toxic concentrations of DCA, did not affect VSMC viability, induced calcification of VSMC in culture and increased atherosclerotic vascular calcifica
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There are two ways to transport FFAs into
2023-02-20
There are two ways to transport FFAs into cells. First by passive diffusion. Second as the putative long-chain fatty dacomitinib transporters are proposed, CD36 the plasma membrane-associated fatty acid-binding protein (FABPpm) and fatty acid transport proteins (FATP) [11], where CD36 is responsible
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Herein we employ an adapted
2023-02-20
Herein we employ an adapted targeted quantitative proteomic isotope dilution method, developed in our laboratory [[18], [19], [20], [21]], to quantify membrane transporters in fresh lung from five donors, in four immortalized human lung cell lines and in three control cell lines. We quantify twelve
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Several tertiary prevention studies are currently underway
2023-02-15
Several tertiary prevention studies are currently underway examining the use of dutasteride for prostate cancer treatment: (1) during expectant management of prostate cancer, (2) after radical prostatectomy in men at high risk for relapse, and (3) in men with metastatic disease. The Reduction by Dut
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The reaction of LOX with unlabeled AA generated
2023-02-15
The reaction of 5-LOX with unlabeled AA generated products from hydrogen abstraction at C7 (95% 5-HETE) with minor products derived from abstraction at C10 (5% 8-HETE). With 7,7--AA the selectivity remained skewed towards C7 hydrogen abstraction (59%) compared to C10 hydrogen abstraction products (4
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br Experimental Procedures br Acknowledgments
2023-02-13
Experimental Procedures Acknowledgments This work was supported by NIH/National Human Genome Research Institute (NHGRI)R00 HG006922 and NIH/NHGRIR01 HG008974 (to J.G.), the Huntsman Cancer Institute, and the Women’s Cancers Disease-Oriented Team at the Huntsman Cancer Institute. Research repor
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br Materials and methods br Results br Discussion The transc
2023-02-13
Materials and methods Results Discussion The transcriptional activity of PGC-1α is regulated by a number of stimuli, exemplifying the range of settings in which mitochondrial biogenesis is induced. The mechanisms governing this regulation have been extensively studied and have been determin
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Our results lead to the
2023-02-13
Our results lead to the discovery and characterization of VvAAT2, a gene potentially involved in acetate accumulation in grape berries discovered through amino-acid feeding experiments. Incubation with exogenous amino acids has also been a key in the discovery of new genes affecting fruit aromas [13
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It is also possible that
2023-02-13
It is also possible that α2-adrenoceptor activation may inhibit glutamate accumulation by upregulating the glutamate-buffering activity of Müller IOX2 through EAAT1 or adjusting EAAT2 in bipolar cells, as well as the NMDA receptor. Therefore, we investigated whether topical administration of brimon
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Ion Channel Compound Library Herein we employ an adapted tar
2023-02-13
Herein we employ an adapted targeted quantitative proteomic isotope dilution method, developed in our laboratory [[18], [19], [20], [21]], to quantify membrane transporters in fresh lung from five donors, in four immortalized human lung cell lines and in three control cell lines. We quantify twelve
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Ambient levels of ppm ozone were recorded
2023-02-13
Ambient levels of 0.2ppm ozone were recorded during a recent 2017 weather event in Texas, United States (EPA, 2007). This concentration or higher levels have been used in several human clinical studies during intermittent exercise (Miller et al., 2016c). Although ozone concentration of 0.8ppm used i
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A clear link between ADR stimulation
2023-02-13
A clear link between α2-ADR stimulation and decreased respiration in β-cells is established and consistent with proteomics data. Current discoveries in islets have identified physical interactions between ADR-coupled G proteins and cellular components such as insulin vesicles and ion channels (Zhao
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Losmapimod br There are three types of HT receptors
2023-02-13
There are three types of 5-HT2 receptors. 5-HT2A, 5-HT2B and 5-HT2C receptors Exhibit 46–50% overall sequence identity and couple preferentially to Gq/11 to increase inositol phosphates and cytosolic [Ca2+] and in agreement with their long known role in muscle contraction and stimulation in the br
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