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A novel series of DHODH inhibitors was developed
2020-06-11
A novel series of DHODH inhibitors was developed by us based on a lead that was discovered during a docking procedure and medicinal chemistry exploration. The activity of the initial lead was improved by a QSAR method and yielded low nanomolar inhibitors. Introduction The most common metabolic h
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Inopportunely normal aging brings about
2020-06-10
Inopportunely, normal aging brings about decreases in frontal D1 receptor densities and a gradual decline in postsynaptic markers of dopamine in striatal, neocortical, and limbic areas of the d cycloserine (Bäckman et al., 2006, de Keyser et al., 1990, Karrer et al., 2017, Suhara et al., 1991, Wang
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Previous studies have documented that SCFAs may elicit effec
2020-06-10
Previous studies have documented that SCFAs may elicit effects on lipid metabolism via de novo synthesis and transport. Acetate is not only used as an energy source, but is also constituted as a substrate for the cholesterol synthesis in the liver through acetyl-CoA, thus affecting plasma cholestero
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In conclusion substrate enabled effective detection of L ala
2020-06-10
In conclusion, substrate enabled effective detection of L-alanylaminopeptidase activity in all Gram-negative bacteria tested here. The chromogenic substrate showed high sensitivity at a relatively low concentration (50 mgL), with no diffusion of the coloured chelate into the surrounding agar. Lack
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br Results br Discussion The ubiquitin
2020-06-10
Results Discussion The ubiquitin system has in recent years become an exciting area for drug discovery (Cohen and Tcherpakov, 2010), as multiple enzymatic steps within the ubiquitylation process are druggable. The potential of targeting the ubiquitin-proteasome pathway was first demonstrated i
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br Materials and Methods br Acknowledgements
2020-06-10
Materials and Methods Acknowledgements We thank the staff of beamlines ID29 and ID30A-1 of the European Synchrotron Radiation Facility. This work was supported by, the Marie Curie Career Integration Grant (PCIG13-GA-2013-630755), the Israel Science Foundation (Grant 1383/17) and the Israeli Ca
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Studies carried out with LTRAs before the
2020-06-10
Studies carried out with LTRAs before the identification of the CysLT2R, showed a controversial picture, as results that suggest a role for cysteinyl-LTs in the expansion of ischemic damage and in cardiac dysfunction during reperfusion [5], [68], [69] were evenly balanced by others suggesting that t
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N methyl d aspartate NMDA receptor antagonists such as MK
2020-06-10
N-methyl-d-aspartate (NMDA) receptor antagonists, such as MK-801 and phencyclidine, induce cognitive dysfunction in both mice and humans [18]. In addition, antipsychotic drugs ameliorate MK-801-induced cognitive dysfunction; therefore, the acute application of MK-801 can be used as an animal model o
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It was recently reported that a functional single
2020-06-10
It was recently reported that a functional single nucleotide polymorphism (rs75932628) within Triggering receptor expressed on myeloid ONC201 2 (TREM2) is associated with AD (Guerreiro et al., 2013). Homozygous loss of function mutations in TREM2 are also associated with an autosomal recessive form
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Overexpression of EP and DDR
2020-06-09
Overexpression of EP300 and DDR1 has been sporadically reported in the pathogenesis of pulmonary fibrosis and other fibrotic diseases. Zeng et al. reported that EP300 was increased in TGF-β1 treated lung fibroblasts and mediated decreases of SIRT1 expression. Bhattacharyya et al. found that both EP3
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br Acknowledgments We thank the Lapaha Community and Nobles
2020-06-09
Acknowledgments We thank the Lapaha Community and Nobles (His Serene Highness Prince Kalaniuvalu Fotofili, Her Serene Highness Princess Marcella Taumoepeau Tupou Kalaniuvalu Fotofili and Her Royal Highness Mele Siu\'ilikutapu Kalaniuvalu Fotofili) and the Ministry of Internal Affairs (Government
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The four other mutations S T V I T
2020-06-09
The four other mutations (S281T, V317I, T328A and A329S) were not detected in the absence of the A286S. This could suggest that when all of them are present, there would be a tri-dimensional structural modification that would interfere with the binding of the insecticide and produce different levels
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Sepantronium br Funding This work was partly supported by th
2020-06-09
Funding This work was partly supported by the grant ‘Maria Grazia Cuccoli’ from Fondazione Cassa di Risparmio di Bologna. Declarations of interest Acknowledgements Introduction The main strategy of oncolytic viral therapy is based on the fact that naturally occurring or engineered virus
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In order to further understand the biological significance o
2020-06-09
In order to further understand the biological significance of cell-collagen X interactions, we have examined the possibilities of involvement of other collagen receptors in cell binding to collagen X. The present study demonstrates that collagen X is a ligand for DDR2. DDR2 has been observed to bind
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br Introduction Rhabdomyosarcoma RMS is a
2020-06-09
Introduction Rhabdomyosarcoma (RMS) is a myogenic tumor that accounts for approximately 50% of all pediatric soft tissue sarcomas. Diagnostic criteria for RMS PD173074 mg on the validation of proteins of the skeletal muscle lineage, such as Desmin, MyoD or Myogenin [1]. RMS cells are persistentl
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