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exemplifies three of the compounds
2024-03-08
exemplifies three of the compounds investigated in the selection for a candidate drug (CD). Our first criteria was an IC PF 4800567 hydrochloride as such did not show any genotoxicity in the SOS/umu assay, but this does not say anything about any possible genotoxicity of its metabolites or degrada
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In pancreatic islets we found
2024-03-08
In pancreatic islets we found an increase in protein expression of leukocyte 12/15-LO that paralleled the metabolic decline characterized by severe hyperglycemia and reduced islet numbers. Similar increase in 12/15-LO expression by Western blot was found in the control mice, which have a normal meta
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Our results clearly demonstrate that inhibition of ATM
2024-03-08
Our results clearly demonstrate that inhibition of ATM pathway activation results in resistance to Vγ2Vδ2 T cell-mediated cell death. Therefore, enhancing ATM activation along with Vγ2Vδ2 T cell treatment would promote the cytotoxicity of resistant ovarian cancer cells. To our knowledge, this is the
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Introduction It has long been
2024-03-07
Introduction It has long been recognized that angiogenesis is critical to the growth, progression, and metastasis of many solid tumor types [1], and thus, drugs targeting the angiogenic pathway have been a topic of clinical investigation in the oncology community for many years. Angiogenesis is reg
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Recently two distinct small molecule inhibitors of PHGDH
2024-03-07
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 Tryptone with high SSP flux [50,51]. The inhibitor NCT-503, which has an IC50 of 2.5μM, reduces the growth
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To guide our attempts at achieving AKT potency and
2024-03-07
To guide our attempts at achieving AKT potency and selectivity against p70S6K and other kinases from (p70 S6K IC: 0.004 μM) and , we took advantage of exploiting the subtle sequence differences in the active sites of the AGC family kinases, we utilized the information around crystal structure of AKT
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As regards feeding the ability to dissipate surplus
2024-03-07
As regards feeding, the ability to dissipate surplus energy in the form of heat is beneficial for animals if the protein concentration in the food is low, since it allows them then to meet the adequate protein intake requirement without getting fat. Some of the major dietary activators of the AHR ar
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In addition to the above
2024-03-07
In addition to the above-mentioned synaptic mechanisms, the serotonergic system also has a critical role in the antidepressant effects of mGlu2/3 receptor antagonists. Indeed, we previously reported that mGlu2/3 receptor antagonists increased the firing rate of serotonin neurons in the dorsal raphe
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In addition to the above
2024-03-07
In addition to the above-mentioned synaptic mechanisms, the serotonergic system also has a critical role in the antidepressant effects of mGlu2/3 receptor antagonists. Indeed, we previously reported that mGlu2/3 receptor antagonists increased the firing rate of serotonin neurons in the dorsal raphe
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In an attempt to complete the overview
2024-03-07
In an attempt to complete the overview of resistance mechanisms in Spanish codling moth populations, the aims of the present work were to assess the actual occurrence of AChE and kdr mutations in codling moth field populations from different pome fruit-growing areas of Spain, concurrently with the f
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YM 58483 In an insightful essay Heryanto writes that
2024-03-07
In an insightful essay, Heryanto (1990, 40) writes that language is “a phenomenon expressing the particular history of a society” that did not exist in many parts of the world. “Language is not a universal category or cultural activity. Though it may sound odd, not all people have a language in the
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Given the profound expression of HT A and HT A
2024-03-07
Given the profound Coumarin mg of 5-HT1A and 5-HT2A in the hippocampal CA1 region, and their potential to complex with mGluRs, the objective of this study was to examine if sleep deprivation alters the expression of 5-HT1A and 5-HT2A receptors and determine whether potential changes are reversible
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The take home message here is that although
2024-03-07
The take-home message here is that, although Aurora A phosphorylated on T288 is the activated isoform of Aurora A, measuring the level of phosphorylation of T288 does not reflect Aurora A kinase activity (Figure 5). What would be the most appropriate readout for an in vivo Aurora A kinase activity
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Another contributor for the G M
2024-03-06
Another contributor for the G2/M arrest in A549 and H1299 cells might be p21WAF1/CIP1 which was up-regulated upon ovatodiolide treatment. p21WAF1/CIP1 is a common CDKs inhibitor which blocks Genistein G2/M phase progression in various types of cancer cells (Kim et al., 2015, Liberio et al., 2015).
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In vascular endothelial cells L arginine produces nitric
2024-03-06
In vascular endothelial cells, L-arginine produces nitric oxide (NO) under the action of nitric oxide synthase (NOS), and nitric oxide can activate guanylate cyclase to produce a large amount of cGMP, thereby relaxing vascular smooth muscle and expanding blood vessels. Numerous studies have confirme
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