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GLPG0634 australia Molecular docking quantitative structure
2024-04-23
Molecular docking, quantitative structure–activity relationship (QSAR) and high-throughput virtual screening (HTVS) studies have a very widespread use in computer-assisted drug design.25, 26, 27, 28 Suvannang et al. used the published X-ray crystallographic data to examine known aromatase inhibitors
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To enhance the accuracy of SEs in eliminating cancer
2024-04-23
To enhance the accuracy of SEs in eliminating cancer cells, the mAb recognized by specific Fostriecin sodium salt receptor on tumor cells were fused with SEs. Fab C215 or C242 fused with SEA promoted apoptosis in human colon carcinoma cells via Fas (Dohlsten et al., 1994, Litton et al., 1996). SEB-
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Natural compounds present in medicinal and or nutritional pl
2024-04-23
Natural compounds, present in medicinal and/or nutritional plants as well as in macrofungi sources, have stimulated a great interest from the pharmaceutical industry. Different natural compounds such as phenolic compounds, alkaloids, terpenoids among others, have shown strong antiangiogenic effects
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br Experimental procedures br Results br Discussion Our biop
2024-04-23
Experimental procedures Results Discussion Our biophysical and cellular analyses of mutant Aβ1–42 peptides support a role of the N-terminus of Aβ in peptide aggregation and toxicity. We demonstrate that double mutations constructed to humanize the rodent Aβ1–42 sequence result in a signific
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RNA interference assays have shown
2024-04-23
RNA interference assays have shown that the inhibition of AMPK expression leads to increases in TNF-α, IL-6 and cyclooxygenase-2 (COX-2) levels after LPS stimulus, whereas the transfection of macrophages with a constitutively active form of AMPKα1 results in decreased LPS-induced TNF-α and IL-6 prod
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Platelet derived growth factor PDGF and ciliary neurotrophic
2024-04-23
Platelet-derived growth factor (PDGF) and ciliary neurotrophic factor (CNTF) are expressed by glial cyclin dependent kinase and are important to neuron survival and the maintenance of oligodendrocytes. These neurotrophic factors contribute to the remyelination process by increasing the proliferatio
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In past Zebra fish Danio rerio
2024-04-23
In past, Zebra fish (Danio rerio) has emerged as a suitable model for early vertebrate development, and a number of targeted mutations in the zebrafish genome led to phenotypic alterations that resemble human diseases [34]. A 12-LOX in Zebra fish has been cloned and knock down of this zf12-LOX enzym
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br Co http www apexbt com media diy
2024-04-22
Conclusions This paper is the first meta-analysis about the association between SRD5A2 V89L polymorphism and hypospadias risk. The results of this meta-analysis have revealed that V89L polymorphism definitely increases the risk of hypospadias, and the C allele is a genetic risk factor for hypospa
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br Animals Female Sprague Dawley
2024-04-22
Animals Female Sprague Dawley (SD) rats, aged 3 months with body weight between 180-210 g were housed in cages and acclimatized to standardized lab conditions (temperature 23 ± 2°C, humidity 50 ± 5% and 12 h light-dark cycles). The rats were fed with standard rodent food pellet (Harlan Diet, Ross
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APJ is mainly coupled to PTX
2024-04-22
APJ is mainly coupled to PTX-sensitive Gi/o proteins [33], and thus, it is associated with the inhibition of adenylyl cyclase and the activations of PI3K/Akt signaling and MAPKs signaling pathways [23], [54], [55], [56]. In a previous study, apelin stimulations of the PI3K/Akt and/or the MAPK pathwa
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AP was originally described as a heterodimer
2024-04-22
AP-1 was originally described as a heterodimer of the bZIP proteins c-Jun and c-Fos. The experiments described here showed that stimulation of TRPV1 channels induced the expression of both of these classical constituents of AP-1. The essential role of both proteins was analyzed in a series of experi
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br Obstructing SNARE zippering Sharma
2024-04-22
Obstructing SNARE “zippering” Sharma et al. demonstrated for the first time that in the postmortem AD brains, the level of SNARE complex formation, which is necessary for driving synaptic vesicle fusion at the presynaptic active zone, is significantly reduced [123]. In the absence of changes in e
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br Material and methods br Results br
2024-04-22
Material and methods Results Discussion Aminopeptidase N is a transmembrane protease present in a wide variety of human tissues and cell types (endothelial, epithelial, fibroblast, leukocyte). APN expression is dysregulated in inflammatory diseases as well as in solid and hematologic tumors
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This development notwithstanding the chemotherapeutic treatm
2024-04-22
This development notwithstanding, the chemotherapeutic treatment for leukemia has stagnated over the last 40 years [35]. Main treatment options necessitate aggressive chemotherapy to target leukemic cells [36], [37], [38], [39]. Several limitations of current treatment options include the use of ant
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In this study we designed and synthesized two
2024-04-22
In this study, we designed and synthesized two ALK PROTACs (degraders), 5 (MS4077) and 6 (MS4078), by linking ceritinib and pomalidomide [45] through two different linkers. Using human ALCL and NSCLC cells, we characterized both compounds in a battery of assays to demonstrate their effects on reduci
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