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br Funding This work was supported by grants to
2020-05-21

Funding This work was supported by grants to A.S. from the Swedish Cancer Foundation, Sweden (Grant number: CAN, 2015/637), the Swedish Medical Council, Sweden (Grant number: 2017- 01274), the Foundations at Skåne University Hospital, Sweden and to KB, SRS, NC, BCS, and SS from the Royal Physiogr
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Flexible alignment of isopropylphenylaminobenzimidazole with
2020-05-21

Flexible alignment of 7-isopropylphenylaminobenzimidazole 16 with the lead 2-Phenyl-2-(1-piperidinyl)propane sale 1 was performed using MOE. It was found that the aryl group of compound 16, exemplified as a yellow circle in Figure 2, overlapped well with the corresponding alkyl chain of compound 1
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Amyloid Beta-Peptide (1-40) br Thermodynamic modeling br Sel
2020-05-21

Thermodynamic modeling Selection of data The solutes were selected based on the set of data needed to evaluate the CPA-EoS for prediction of their solubility in CO2 + cosolvent, as shown in Fig. 1. Critical temperatures, melting temperatures and enthalpies of fusion of the solutes are required
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Mass spectrometry has previously been used to
2020-05-21

Mass spectrometry has previously been used to examine the presence of Hyp in recombinant collagen, using hydrolysates to identify the individual imino acid, equivalent to an amino BCECF-AM analysis [33], and also by analysis of mass changes to tryptic peptides [34]. The present study, however, has
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Next to organophosphates carbamates and metals cholinesteras
2020-05-21

Next to organophosphates, carbamates and metals, cholinesterase activity can also be affected by other pesticides, such as newer generation neonicotinoid insecticides (NN). NNs do not inhibit AChE activity via the organophosphate-sensitive binding site of the enzyme, but rather, by acting as a struc
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Exposure to UV instead of DMBA also produced a
2020-05-21

Exposure to UV instead of DMBA also produced a sloughing and angiogenic response in transgenic, but not WT, mice, indicating that the epidermis of the BK5.EP4 mice has a much lower apoptosis threshold than WT mice, as suggested by others (Chun and Langenbach, 2007). Overall, these studies suggest th
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Ageing is associated with increased reactive oxygen species
2020-05-21

Ageing is associated with increased reactive oxygen species (ROS) production, oxidative stress and oxidative damage [43,44]. Overproduction of ROS can impair endothelial function by suppressing NO synthesis and scavenging NO thereby decreasing its overall bioavailability. Moreover, sustained oxidati
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br Materials and methods br Results br Discussion CHIKV is
2020-05-21

Materials and methods Results Discussion CHIKV is an important arthropod borne virus with substantial impact on global health and cause a major viral disease that requires the development of antiviral drug to combat chikungunya disease. Virus specific proteases have particularly become an a
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In addition we investigated if the
2020-05-21

In addition, we investigated if the previously reported papain inhibitor can inhibit rhodesain, and found that it was not active at inhibiting rhodesain. The vinyl sulfone analogue of () was then synthesized and tested, and it was also inactive towards rhodesain. We then determined the time dependen
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In these studies the inflammatory cytokine IL was demonstrat
2020-05-21

In these studies, the inflammatory cytokine IL-8 was demonstrated as one of the responsible molecules induced by CysLTs via activating CysLT2 receptors. IL-8 is synthesized in and released from mononuclear cells, macrophages, fibroblasts and airway epithelial cells, and it promotes inflammation as a
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br Acknowledgement This research was supported by a grant
2020-05-21

Acknowledgement This research was supported by a grant from the National Research Foundation of Korea (NRF-2013R1A1A2011238) funded to Young-Mi Lee. Introduction Stroke is considered a serious disease with high morbidity and high mortality. More than 6 million deaths are reported each year wo
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In our preliminary evaluation of this series we
2020-05-21

In our preliminary evaluation of this series, we were surprised to discover that CA-074 Me synthesis was found to bind CSF-1R in a classical DFG-in binding mode (a). Dramatic conformational differences in the juxtamembrane domain and activation loops are apparent when this DFG-in structure is comp
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br Clinical trials of CRM inhibitors KPT
2020-05-21

Clinical trials of CRM1 inhibitors KPT-330 clinical trials have been initiated with promising very early results. One trial includes patients with advanced solid tumors whose disease has progressed after at least one prior therapy for metastatic disease (NCT01607905). Another trial includes patie
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egfr inhibitor The observed increase in Bdnf mRNA occurred
2020-05-20

The observed increase in Bdnf1 mRNA occurred 1 h after treatment indicates participation of BDNF in early plasticity and subsequently mnemonic processes. Most of the evidence regarding the importance of BDNF for memory formation derived from electrophysiological studies that utilized the molecular c
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P H is a nonheme iron II
2020-05-20

P4H is a nonheme iron(II) dioxygenase that uses O2 and α-ketoglutarate as co-substrates (Fig. 1A). The three-dimensional structure of mammalian P4H is unknown. We reasoned that an electrophilic analog of α-ketoglutarate could serve as an irreversible inhibitor of the enzyme and, hence, a useful prob
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