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br Conclusion In summary screening a small
2023-12-08
Conclusion In summary, screening a small compound library based on the 3-aminopyridin-2-one motif in a target-blind manner against a 26-kinase panel, representative of the kinome, identified hits that possess good activity and excellent ligand efficiency against MPS1, Aurora A and Aurora B. The b
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Previously using a P lacZ reporter gene
2023-12-08
Previously, using a P-lacZ reporter gene system, it has been shown that the β-galactosidase activity was 9-fold higher in the stationary phase cotransporter when compared with those of the exponential phase [15]. Furthermore, inositol supplementation did not have a major effect on the expression of
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The co crystal structure of
2023-12-08
The co-crystal structure of ()-blebbistatin ()- bound to myosin II (PDB: ) was used to scout for possible favorable interactions with the residues lining the binding pocket. Looking at A, we hypothesized that -oriented hydrophilic moieties (e.g. hydroxymethyl) on C of the blebbistatin scaffold migh
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HET0016 synthesis br Results br Discussion Both ATM
2023-12-08
Results Discussion Both ATM and ATR are key regulators of the cellular response to DSBs, yet how exactly they function in concert is not well understood. Recent studies revealed that ATM is required for the resection of DSBs (Jazayeri et al., 2006, Myers and Cortez, 2006), a process necessary
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br Introduction Hepatocellular carcinoma HCC is
2023-12-08
Introduction Hepatocellular carcinoma (HCC) is an aggressive and malignant cancer detected in clinical practice, as it is the third key reason of tumor-related deaths worldwide, with > 800, 000 mortalities every year (Torre et al., 2015). Current treatments for HCC are surgical therapy, liver tra
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Apelin is a peptide hormone and an
2023-12-08
Apelin is a peptide hormone and an endogenous ligand for a G protein-coupled receptor named APJ [7], [8], and apelin and APJ are widely expressed in human organs including hypothalamus, heart, lungs, kidneys, adipose tissue, muscles, and others [9]. Apelin is initially synthesized as a 77-amino-acid
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Reactive oxygen species is an aspect of oxidative stress
2023-12-08
Reactive oxygen species is an aspect of oxidative stress which are associated with many diseases such as rheumatoid arthritis, diabetes, inflammation, atherosclerosis and cancers (Collins, 2005; Halliwell, 1994). Thus, the need for naturally occurring antioxidants is of crucial importance. Some biop
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Spautin-1 mg We report here the first
2023-12-08
We report here the first study on the inhibitory effects of the organic nitrates – on human erythrocyte GR. The previous reports by Becker et al., investigated other nitro derivatives (including arylizoalloxazines) by using Beutler’s method, monitoring GR inhibition. Data of show inhibition of hGR b
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br Conclusions br Funding This work
2023-12-08
Conclusions Funding This work was supported by a Finnish government subsidy for health science research [grant numbers TYH2012141, TYH 2013218, and TYH 2014216]; the SSAC Foundation [grant numbers SLS-504141 and SLS-693781]; and the Paulo Foundation. The funding sources had no involvement in s
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br HIF Signaling in AA Therapy Resistance An important
2023-12-08
HIF-α Signaling in AA Therapy Resistance An important result emerging from Phase 3 clinical trials testing AA therapies is improvement of progression-free survival (PFS) that is not accompanied by enhanced overall survival (OS) [26]. This dichotomy has been attributed to mechanisms of acquired re
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We designed SSOs that block APP exon splicing and
2023-12-08
We designed SSOs that block APP exon 17 splicing and induce the production of an alternatively spliced APP mRNA lacking exon 17 (APPΔex17). APPΔex17 mRNA encodes an APP protein isoform that lacks 49 Nutlin-3 including the γ-secretase cleavage sites that give rise to the toxic, AD-associated Aβ42 pe
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The anorexic effect observed when AR
2023-12-07
The anorexic effect observed when AR231630 is infused into the VTA could be the result of the DA release inhibition, as previously described [11]. However, there is also a hedonic aspect in feeding that possibly involves dopaminergic mechanisms of reward. Helm et al. showed a functional link between
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Adenosine receptors activate a number of
2023-12-07
Adenosine receptors activate a number of signalling pathways involved in tissue survival including several mitogen-activated protein kinases (Fredholm et al., 2001). The common feature of all adenosine receptors is the positive coupling to ERK1/2, whilst A2B and A3 receptors can also activate the st
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Streptomycetes are a group of filamentous
2023-12-07
Streptomycetes are a group of filamentous Gram-positive, soil-inhabiting bacteria which have captured enormous screening interest because of their ability to produce and secrete a variety of SNOG synthesis and extracellular proteins [7]. Among the diverse antibiotics produced by Streptomycetes are
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Anisodamine receptor A weakness of our technique
2023-12-07
A weakness of our technique is that during the early post-operative period without the scaffold of an enteric channel patients can be at risk for traumatic or difficult catheterization, with 3 of 6 requiring a visit. This appeared to be offset by having skilled and educated housestaff capable of rec
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