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br Experimental br Results and discussion One of
2021-11-25
Experimental Results and discussion One of the major challenges of oral drug delivery via nanocarriers is the fairly low efficiency of crossing the intestinal barrier. While there is the possibility of a paracellular transport for polar substances below 1000 Dalton [26], the key mechanism of o
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Hyperhomocysteinemia HHcy is a clinical condition characteri
2021-11-25
Hyperhomocysteinemia (HHcy) is a clinical condition characterized by increased levels of plasma homocysteine (Hcy) and a well-known risk factor for CVDs. Hcy is a sulfur-containing non-protein amino FMK receptor formed during the intracellular conversion of methionine to cysteine. Previous study dem
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While considering the molecular pathogenesis of
2021-11-25
While considering the molecular pathogenesis of an MPNST, the Ras/Raf/MEK/ERK, mTOR/AKT, p53, and PTEN pathways associated with tumor growth have been described (McCubrey et al., 2012). The involvement of receptor tyrosine kinases such as EGFR and TAM receptor families, and its associated molecular
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Studies conducted in our laboratory thus far have
2021-11-25
Studies conducted in our laboratory, thus far, have shown that HKDC1 is broadly expressed [28]. Using the first developed HKDC1 mouse model, we found that complete loss of HKDC1 function is embryonic lethal, similar to other HKs [29,30]. Further studies using HKDC1 heterozygous knockout mice showed
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In diseased blood vessels increased production of reactive
2021-11-25
In diseased blood vessels, increased production of reactive oxygen species (ROS), such as peroxynitrite, superoxide, and hydrogen peroxide, have been found [[53], [54], [55]]. Peroxynitrite was suggested to alter the redox state of sGC [53] while hydrogen peroxide interfered with the action of NO bu
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GLPG0634 Whilst it has long been appreciated that Rho
2021-11-25
Whilst it has long been appreciated that Rho-family GTPases are able to signal directly to focal adhesions, it is also becoming increasingly clear that they can achieve this indirectly, through their influence on the extracellular matrix to which the integrins bind. Cdc42 and RhoA have long been kno
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While the specific set of challenges associated with
2021-11-24
While the specific set of challenges associated with deorphanization and transforming each poorly characterized GPCR into a useful drug target will be unique, much can be learned by considering how these issues have been addressed for other receptors. One group of poorly characterized GPCRs that hav
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The occurrence of MDR in cancer patients undergoing
2021-11-24
The occurrence of MDR in cancer patients undergoing chemotherapy can be mimicked in the laboratory by culturing cancer indoximod mg in the presence of chemotherapeutic drugs, thereby enforcing the evolution of acquired drug resistance. This has been described in multiple model systems including the
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To further implicate the role of
2021-11-24
To further implicate the role of EAAT3 in morphine-induced place preference, the effects of morphine on EAAT3 PHA 543613 hydrochloride was determined. Interestingly, morphine increased EAAT3 protein expression in the plasma membrane of mPFC, nucleus accumbens and VTA but not in the hippocampus of w
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Moreover we examined inhibition of GLI mediated mRNA express
2021-11-24
Moreover, we examined inhibition of GLI-mediated mRNA expression by 1. Colubrinic put off (1) inhibited the mRNA production of PTCH in PANC1 cells in the dose-dependent manner. This result clearly shows 1 inhibits GLI-mediated transcription (Fig. 6). Discussion In this study, we identified three
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Analgesic activity was evaluated by
2021-11-24
Analgesic activity was evaluated by measuring tail flick latencies to the immersion of rat’s tail in water, maintained at ∼51°C [18] after recovery from anesthesia. Typically, rats were immobilized inside a restrainer, leaving only the tail exposed, which was then immersed into the hot water bath, a
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Acquiring resistance to the FGFR inhibitor may determine tre
2021-11-24
Acquiring resistance to the FGFR inhibitor may determine treatment outcomes in patients with GC dependent on FGFR2 amplification, and we investigated the mechanism of AZD4547 resistance in FGFR2-amplified GC cells. We established a FGFR2-amplified GC cell line resistant to the selective FGFR inhibit
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In studies described earlier IRL was
2021-11-24
In studies described earlier, IRL-1620 was administered intravenously; however, because of its short half-life (Rubin and Levin, 1994) (about 7–8min), the dosing had to be repeated three times. Also, a dose-dependent hypotension was observed with repeated doses of IRL-1620 in rats (Leonard and Gulat
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Wnt-C59 br Histamine and glycaemia Histamine
2021-11-24
Histamine and glycaemia Histamine is involved in a wide variety of pathophysiological events mostly related to the inflammatory response through four receptors, namely H1-4Rs. The first studies of Wnt-C59 and diabetes date back to the 1950s. Since that time the involvement of histamine in diabete
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In this current study we not only demonstrated the growth
2021-11-24
In this current study, we not only demonstrated the growth-inhibitory effects of the 2nd generation analog SL-1-39 on the HER2+ breast cancer cells, MDA-MB-453 and SKBR3 (Table 1), but we also demonstrated that the decrease in cell number was associated with an interruption of PP 2 progression thro
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