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In order to validate the ATP competitive mode
2020-03-16
In order to validate the ATP competitive mode of inhibition, compound 12 was selected as a representative inhibitor of this series, and the IC50 values were determined at eight different concentrations of compound 12 ranging from 0.001 to 100 μM, and repeated four times using different ATP concentra
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br STAR Methods br Acknowledgments We are
2020-03-16
STAR★Methods Acknowledgments We are grateful to Amaia Lujambio, James Fagin, and Ramon Parsons for providing cell lines and Evripidis Gavathiotis for critical reading of the manuscript. We would like to thank Saboor Hekmaty for providing expertise with RNA-seq analysis. P.I.P. would like to ac
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In the present study we investigated the role of EP
2020-03-16
In the present study, we investigated the role of EP1R after ICH and its mechanism of action. We hypothesized that EP1R activation aggravates ICH injury but that its blockade reduces injury through the Src kinases and the MMP-9 signaling pathway. To test this hypothesis, we examined the effects of s
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br Materials and methods br
2020-03-16
Materials and methods Results and discussion Concluding remarks Together, the results of the theoretical kinetic simulations and of the analysis of the experimentally determined kinetic data of SoBADH performed in this work show that ignoring substrate inhibition causes potentially importan
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br Target enzyme attributes and substrate peptide
2020-03-16
Target enzyme attributes and substrate peptide selection Protein kinases catalyze the phosphorylation of serine, threonine, and tyrosine residues in both proteins and peptides using ATP as the phosphoryl donor. The human kinome is comprised of 518 protein kinases and 40 lipid kinases. The vast ma
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The Acat gene was identified by functional complementation
2020-03-16
The Acat1 gene was identified by functional complementation of a Chinese hamster ovary cell mutant lacking ACAT activity [12]. Unlike most other genes, human Acat1 is located in two different chromosomes, FPH2 1 and 7, with each site containing a distinct promoter: chromosome 1 contains exons 1–16,
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In addition to tissue resident stromal and myeloid
2020-03-13
In addition to tissue-resident stromal and myeloid cell populations, ILCs also readily engage in positive-feedback loops with myeloid KPT-9274 recruited from the circulation. TNF-α produced by inflammatory monocytes recruited to the lungs of mice infected with Klebsiella pneumoniae markedly increas
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Our studies approached this problem using integrative omics
2020-03-13
Our studies approached this problem using integrative -omics analysis of human NK-ieILC1s from distinct microenvironments and functional subsets, including helper and adaptive phenotypes. At both the transcriptional and epigenetic levels, we find that the adaptive subset, CD57+ cytotoxic NK cells, s
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br Coactivator Binding Sets APC C Catalytic Core in
2020-03-13
Coactivator Binding Sets APC/C Catalytic Core in Motion A coactivator not only recruits substrates to APC/C [18] (Figure 3B), but also stimulates repositioning of the catalytic core 19, 24. High-resolution cryo-EM maps of apo forms of APC/C without a coactivator show the catalytic core and platfo
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br Author Contributions br Acknowledgments br
2020-03-13
Author Contributions Acknowledgments Introduction Osteoporosis is a common bone disease that frequently leads to disruption of the alveolar and systemic bones with age. Novel osteoanabolic strategies to treat osteoporotic bone loss or augment fracture repair efficiently are desired. Since b
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Since the initial identification of DNA ligase
2020-03-13
Since the initial identification of DNA ligase inhibitors by a structure-based approach [[18], [26]], there have been several reports describing LigI inhibitors using computer modelling and derivatives of the original DNA ligase inhibitors [[49], [50], [51]]. While these studies have shown that the
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The field of synthetic cytokine biology
2020-03-13
The field of synthetic cytokine biology continues to grow through molecular, physiological and pathophysiological insights, as well as via new methodical advances. The approval of chimeric antigen receptor (CAR) T cell immunotherapy by the US Food and Drug administration (FDA) in August 2017 for rel
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Among the other mediators which have been reported to
2020-03-13
Among the other mediators which have been reported to play a role in erection are prostaglandins (PGs). Several studies have reported that alprostadil- synthetic PGE1- showed high efficacy in management of erectile dysfunction as it induces corpus cavernosal relaxation. Alprostadil has been first de
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Semantics play an important role in software component based
2020-03-13
Semantics play an important role in software component-based development as they improve components identification, selection and integration through, among others, the use of ontologies (Kaur and Mishra, 2017). Analogously, they allow to improve discovery, composition and reuse in the context of We
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AR-A014418 The presence of a vicious cycle established betwe
2020-03-13
The presence of a “vicious cycle” established between tumor proliferation and paratumor osteolysis plays a crucial role in the development of primary bone tumors [53]. Cancer cells produce soluble factors that activate directly or indirectly via osteoblasts, osteoclast differentiation and maturation
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