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Zhaolin Wang Cara Fraley Adam R. Mezo 《Bioorganic & medicinal chemistry letters》2013,23(5):1253-1256
The neonatal Fc receptor, FcRn, prolongs the half-life of IgG in the serum and represents a potential therapeutic target for the treatment of autoimmune disease. Small molecules that block the protein–protein interactions of human IgG–human FcRn may lower pathogenic autoantibodies and provide effective treatment. A novel class of quinoxalines has been discovered as antagonists of the IgG:FcRn protein–protein interaction through optimization of a hit derived from a virtual ligand-based screen. 相似文献
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Plant and Soil - Cracks and biopores in compacted soil such as plough pans could aid deep rooting, mitigating constraints to seasonal upland use of paddy fields for rice production. This research... 相似文献
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Perspective texture synthesis has great significance in many fields like video editing, scene capturing etc., due to its ability to read and control global feature information. In this paper, we present a novel example-based, specifically energy optimization-based algorithm, to synthesize perspective textures. Energy optimization technique is a pixel-based approach, so it’s time-consuming. We improve it from two aspects with the purpose of achieving faster synthesis and high quality. Firstly, we change this pixel-based technique by replacing the pixel computation with a little patch. Secondly, we present a novel technique to accelerate searching nearest neighborhoods in energy optimization. Using k- means clustering technique to build a search tree to accelerate the search. Hence, we make use of principal component analysis (PCA) technique to reduce dimensions of input vectors. The high quality results prove that our approach is feasible. Besides, our proposed algorithm needs shorter time relative to other similar methods. 相似文献
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One novel approach for the biological delivery of peptide drugs is to incorporate the sequence of the peptide into the structure of a natural transport protein such as human serum transferrin (HST). However, a potential drawback is that the HST may increase the immunoreactivity of the peptide, in the same way that carrier proteins can be used to generate highly immunogenic peptide hapten conjugates. In this study we have generated a recombinant HST carrier protein that contains a peptide substrate of HIV-1 protease (VSQNYPIVL). The protein retained native HST function, and the peptide was surface exposed since it was immunoreactive in native dot blots, and was cleaved by HIV-1 protease. Immunisation of rabbits with the recombinant protein elicited only a very poor anti-peptide immune response. In contrast, strong anti-peptide immune responses were raised against both the peptide alone, and a chemical conjugate of the peptide with HST. These data demonstrate that it is possible to attenuate the immune response normally directed against an immunogenic peptide sequence by engineering into a surface exposed loop of HST. These findings may have an important impact on the future design of peptide delivery systems. 相似文献
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