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IC values were obtained for an
2024-02-21
IC50 values were obtained for an expanded version of the fragment library using the previously described mobility shift assay. Subsequently, Ki values were estimated from IC50 values to allow better comparison of the activity against targets which were measured at different substrate concentrations
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In contrast to TPX members of the CPC Figure
2024-02-21
In DiscoveryProbe™ Inhibitor Library to TPX2, members of the CPC (Figure 1B), such as survivin, borealin, and INCEN-P, which associate with Aurora B/C in animals, do not appear to have obvious homologs in plants. Recently, however, a putative INCEN-P homolog, termed WYRD, has been identified [34].
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protease inhibitor cocktail Introduction the DNA damage resp
2024-02-21
Introduction: the DNA damage response — important implications for tumour development and treatment Cells are invariably challenged by tens of thousands of lesions inflicted on their DNA everyday (Lindhal, 1993). This DNA damage can be caused exogenously by exposure to different types of radiation
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br Mechanisms of GPCR internalization Like
2024-02-21
Mechanisms of GPCR internalization Like for other types of receptors, prolonged agonist stimulation often leads to GPCR internalization, which can occur via different pathways ∗[2], [20], [21], [22], [23]. Of these pathways, clathrin-mediated Caspase-6, human recombinant protein (CME) is the bes
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It is now well established that the cumulative exposure to
2024-02-21
It is now well established that the cumulative exposure to endogenous estrogens throughout a woman's life, mainly due to her reproductive history, has an impact on the risk of hormone-dependent breast cancer (Lambertini et al., 2016). Prolonged exposure to estrogens in the case of early age at menar
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What is the mechanism by
2024-02-20
What is the mechanism by which Wnt7a-Fz7 signaling enhances AMPAR localization and synaptic strength? Following induction of LTP, the number of AMPARs rapidly increases at extrasynaptic sites (Makino and Malinow, 2009, Yang et al., 2008a) through PKA-dependent phosphorylation of GluA1 at S845 (He et
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Based on the improved characteristics of the mutant ECDs we
2024-02-20
Based on the improved characteristics of the mutant ECDs we proceeded to crystallization trials, starting with the β1-BPloop as the most promising. We obtained rod shaped hexagonal crystals reproducibly, but with moderate diffraction ability (Fig. 5). Furthermore, the crystals were sensitive in moun
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Although effects of low concentrations
2024-02-20
Although effects of low concentrations of agonist were not as thoroughly documented for heteromeric receptors such as the major CHIR-090 α4β2 nAChR, a similar mechanism of action was described to explain the potentiation of these receptors with low concentrations of acetylcholine-esterase-inhibitin
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During myeloid cell maturation expression of
2024-02-20
During myeloid cell maturation, expression of 5-LO mRNA and protein is strongly induced (60–130-fold) by calcitriol (1,25(OH)2D3) and transforming growth factor-β (TGFβ) [6,7]. The upregulation of 5-LO mRNA transcription is mainly due to transcript elongation and mRNA maturation [8,9]. Interestingly
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br Conflict of interest statement br Benign prostatic hyperp
2024-02-20
Conflict of interest statement Benign prostatic hyperplasia (BPH) is a highly complex process characterized by an increased number of epithelial and stromal ret pathway in the transition zone. , , Autopsy studies by McNeal detail the evolution of histological changes within these 2 cellular com
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Compound was docked into the active site of
2024-02-20
Compound was docked into the active site of Aurora B kinase using Tripos sybyl-X ver. 2.1.1. The crystal structure of human Aurora B kinase cocrystallized with its potent inhibitor VX-680 was used for the docking analysis (PDB ID: ). The most likely binding conformations were selected based on the
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Although plant Aurora kinases can be clearly
2024-02-20
Although plant Aurora kinases can be clearly grouped into functional clades, the roles of the respective clades does not seem to be evolutionarily conserved. AtAurora 1 labels kinetochore microtubules [19], similarly to mammalian Aurora A, while its targeting to the cell plate resembles features of
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ATM dependent initiation of radiation induced G
2024-02-20
ATM-dependent initiation of radiation-induced G2/M checkpoint arrest is well established [11], [34], [35]. However, the ATR pathway may also be involved [36], [37]. Brown and Baltimore generated Cre/lox-conditional cell lines or Direct Mouse Genotyping Kit with a kinase inactive allele of ATR (ATRk
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In conclusion we report that the
2024-02-20
In conclusion, we report that the widely prescribed drug VPA exerts therapeutic effects on optic nerve demyelination and retinal degeneration in a mouse model of MS. Our findings raise an interesting possibility that combination therapy of VPA and ASK1 inhibition may be useful for treatment of autoi
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With wide spread use of
2024-02-19
With wide-spread use of corticosteroids to combat inflammation and allergies, even children are susceptible to corticosteroid-induced muscle wasting. Although non-steroidal SGRMs that spare muscle and bone, but have significant anti-inflammatory effects, have been preclinically developed and tested,
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