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Of the acidic hydroxyazoles involved hydroxypyrazole had the
2020-04-06
Of the acidic hydroxyazoles involved, hydroxypyrazole had the weakest acidic profile (pKa in the range of 6–7), although highly deprotonated at physiological pH. During hit optimization, the two pyrazole ring positions available for substitution provide an opportunity for a better exploration of the
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br How does DDR receptor activated to induce
2020-04-06
How does DDR2 receptor activated to induce Osteoarthritis Alternation of joints by mechanical stress produces microcracks and deterioration of natural pores in subchondral bone provides FG-4592 for cross talk through diffusion of small molecules [26,27]. At early stage of OA, chondrocytes in the
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Confirmation of the presence of H PPase genes in
2020-04-06
Confirmation of the presence of H+-PPase genes in the genomes of the different protists tested was obtained by Southern blot analyses using the PCR-amplified DNA fragments as probes (Fig. 3). In the trypanosomatids L. major and T. cruzi and the euglenoid A. longa, a single band appeared in the filte
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Air trapping at the small airways is related to
2020-04-06
Air-trapping at the small airways is related to severe ESI-09 (Bjermer, 2014), and acute exacerbation (Mahut et al., 2010). Although asthma patients are generally treated with inhaled corticosteroid (ICS) or with ICS and long-acting β2 agonist (LABA), the efficacy of such treatment depends on drug
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As one of the two receptors for the
2020-04-06
As one of the two receptors for the primordial chemokine CXCL12, ACKR3 exists in jawless fish (Bajoghli, 2013, Nomiyama et al., 2011, Venkatesh et al., 2014). The sea lamprey genome contains two copies of the ACKR3 gene (Ensembl Acc. Nos.: ENSPMAP00000011187 and ENSPMAP00000011401) (Table 1), both e
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First we synthesized inhibitor following the patent procedur
2020-04-06
First, we synthesized inhibitor following the patent procedure reported by Shewchuk et al. to provide its first complete characterization (see ). Two different synthetic approaches were used to obtain compounds –. The first method relied on the alkylation of the common 5-phenol-2,4-diaminopyrimidin
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Because most fusion detection methods
2020-04-06
Because most fusion detection methods were developed to analyze paired-end reads (and especially Illumina data), they are not suitable for identifying fusion junction-spanning reads in single-end Ion Torrent libraries. Therefore, we developed the FusionDetect algorithm (implemented in the ChildDecod
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Recent studies have shown that the extracellular regulated p
2020-04-06
Recent studies have shown that the extracellular regulated protein kinase 1 and 2 (ERK1 and ERK2), commonly referred to collectively as ERK 1/2, are members of the mitogen-activated protein kinase (MAPK) family. This family of kinases transport signals from the surface of the cell to the nucleus, th
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In SLO permeabilized human sperm the
2020-04-06
In SLO-permeabilized human sperm, the AR elicited by calcium, persistently active Arf6 [41] and Rab3A, 8-pCPT-2′-O-Me-cAMP [8], diacylglycerol and a non-hydrolyzable analog [35], is sensitive to the PLC blocker U73122. Furthermore, 8-pCPT-2′-O-Me-cAMP elicits a calcium signal in non-permeabilized sp
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phalloidin synthesis br Effects of estrogen on vascular func
2020-04-06
Effects of estrogen on vascular function Atherosclerosis is a chronic inflammatory condition of the vascular wall (Figure 1) that can be converted to an acute clinical event by the induction of plaque rupture or erosion, leading to thrombosis [58]. This perpetuating process is characterized by ph
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Plasminogen is composed of five N terminal
2020-04-06
Plasminogen is composed of five N-terminal kringle domains and a C-terminal serine protease domain. The kringle domains have an affinity to lysine and binding of plasminogen with its receptors is dependent on its lysine interacting kringle domains [10], [28]. In the current report, we show that eno
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In general cellular senescence is
2020-04-06
In general, cellular senescence is considered a programmed response to stress that can be activated by oxidative stress, irradiation or action of substances or drugs. These stressors cause DNA damage and, through the action of specific proteins (p53 and p21), lead to cell senescence (di Fagagna, 20
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Based on the SUMO SIM interaction involved in SUMOD
2020-04-06
Based on the SUMO–SIM interaction involved in SUMOD positioning, a SUMO2ΔSBD (SIM-binding domain; Q30A, F31A, I33A) mutant can be investigated that disrupts this important binding interface (Eisenhardt et al., 2015; Meulmeester, Kunze, Hsiao, Urlaub, & Melchior, 2008). In Fig. 4A, multiturnover assa
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br Results and discussion br Conclusion Analogues
2020-04-06
Results and discussion Conclusion Analogues of 1,2,4-triazole and 1,3,4-oxadiazole have been designed, synthesized and characterized. To avoid late stage failure, it is important to study the preliminary pharmacokinetic parameters. The results of pharmacokinetic data suggested that, all molecu
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br Conflict of interest br Acknowledgements This work
2020-04-03
Conflict of interest Acknowledgements This work was supported by the Biotechnology Research Center, China Three Gorges University, Yichang, China (No. 2016KBC05), the National Natural Science Foundation of China (No. 31370600 and 31300508), the Zhejiang Science and Technology Major Program on
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