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Acknowledgments We acknowledge the Danish Council for
2019-11-02
Acknowledgments We acknowledge the Danish Council for Independent Research (Grant no. 11-105250) and the Carlsberg Foundation (Grant no. 2011-01-0567) for funding this work. Introduction DNA is vital as a biological target to design diagnostic agents as well as therapeutic drugs. The recognitio
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We next focused our design building
2019-11-02
We next focused our design building into the ribose binding site, which had not been yet utilized in this effort. Compounds bearing a series of five-membered aromatic heterocycles (compound , ) showed reduced inhibition of the Gram-positive isozymes compared with compound , but a 20-fold improved po
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To overcome problems with the biochemical reconstitution
2019-11-02
To overcome problems with the biochemical reconstitution of these heterodimeric cytokines fusion strategies linking both subunits together have been proposed inspired by the “hyper-IL-6” [28]. Much like fusing a protein to a solubility enhancing protein such as MBP or SUMO, fusing two subunits of a
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BINA mg Previous study showed that CXCR plays an important r
2019-11-02
Previous study showed that CXCR plays an important role in viral infection and that CXCR1, as an important molecule in CXCR, also plays important roles in viral pathogenesis [[39], [40], [41], [42]]. In mammals, CXCR1 plays an important role in resisting viral infection [43,44], and CXCR1 plays an i
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Numerous small molecule CRF receptor antagonists
2019-11-02
Numerous small molecule CRF receptor antagonists have been reported in the literature. Some representative examples are shown in . In preclinical studies (DMP696), , was found to be efficacious in preclinical behavioral models for anxiety and depression. In an open label clinical trial with (R121
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Although many neurotransmitters e g
2019-11-02
Although many neurotransmitters (e.g., catecholamines, serotonin, and excitatory/inhibitory amino acids) have been implicated in the modulation of anxiety-like responses (Carobrez et al., 2001, Molchanov and Guimaraes, 2002, Vianna et al., 2001), the so-called atypical neurotransmitters, endocannab
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TH287 br Materials and methods br Results br Discussion
2019-11-02
Materials and methods Results Discussion DAS and nilotinib, as the second potent, oral generation TKIs, bind to both the active and inactive conformation of the ABL1 kinase domain, have been found to be effective in treating patients with IM resistant or intolerant CML-CP, and inhibit all t
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It has been reported that Eph Ephrin are involved
2019-11-02
It has been reported that Eph/Ephrin are involved in the regulation of the tumor angiogenesis [10], [11], [12]. The distinct and specific involvement of MLN 2480 receptor and veins in tumor angiogenesis is unclear. EphrinB2 is expressed in arteries and its receptor EphB4 is expressed in veins; thes
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Nitrid oxide NO and its potential endogenous production
2019-11-02
Nitrid oxide (NO) and its potential endogenous production as an endothelium-derived factor was the first gaseous molecule accepted to be a signaling mediator in the organism [4,5]. NO plays a key role in physiological regulation of the tipiracil and exerts physiological functions in the nervous and
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Therefore HNE is an attractive therapeutic target and the de
2019-11-02
Therefore, HNE is an attractive therapeutic target and the design of new HNE inhibitors is a demanding field that has been extensively investigated in order to provide inhibitors with new molecular architectures, including the potent oxo-β-lactam class [14]. In the present work, a coumarin-based oxo
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Materials and methods Cell culture and
2019-11-01
Materials and methods Cell culture and receptor gene transfection. PC12 Pamidronate Disodium were purchased from the Institute of Cell Biology, Chinese Academy of Sciences, Shanghai, China. The cDNA for mouse CysLT1 or CysLT2 receptor (mCysLT1 and mCysLT2, subcloned into pcDNA3.0) was kindly gifte
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Cariprazine One common method to replace the wet
2019-11-01
One common method to replace the wet limestone process is the use of an amine-based solution as an absorbent to capture SO2. However, almost all of the common amine-based absorbents are highly volatile compounds, whose emissions are air pollutants themselves. Therefore, it is desirable to either use
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Furthermore haplotypes formed by rs rs rs and
2019-11-01
Furthermore, haplotypes formed by rs6269, rs4633, rs4818, and rs4680 of the COMT gene constitute a central COMT locus haploblock that is associated with the enzymatic activity of COMT [8]. The SNPs rs6269 and rs4818, which are located in the central COMT locus haploblock, have been observed to be as
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Conventional assays rely on a comparable transformation of t
2019-11-01
Conventional assays rely on a comparable transformation of the target analytes and the structurally similar (but not identical) proxy substrates and are commonly used to measure individual enzyme activities in (pre-treated) intact sludge flocs (Burgess and Pletschke, 2008a, Gessesse et al., 2003, Yu
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The cytoplasmic domain of classical cadherins is highly cons
2019-11-01
The cytoplasmic domain of classical cadherins is highly conserved and can interact with different cytosolic proteins. Typically this domain is associated with catenin family members, including p120 catenin, β-catenin, and α-catenin, which form a cadherin-catenin complex (Fig. 1). The catenin family
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