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Andreas Reif Sebastian Siebenhaar Andrea Tröster Marina Schmälzlein Carolin Lechner Phanindra Velisetty Karen Gottwald Claudia Pöhner Irene Boos Volker Schubert Prof. Stefan Rose‐John Prof. Carlo Unverzagt 《Angewandte Chemie (International ed. in English)》2014,53(45):12125-12131
Human interleukin 6 (IL‐6) is a potent cytokine with immunomodulatory properties. As the influence of N‐glycosylation on the in vivo activities of IL‐6 could not be elucidated so far, a semisynthesis of homogeneous glycoforms of IL‐6 was established by sequential native chemical ligation. The four cysteines of IL‐6 are convenient for ligations and require only the short synthetic glycopeptide 43–48. The Cys‐peptide 49–183 could be obtained recombinantly by cleavage of a SUMO tag. The fragment 1–42 was accessible by the simultaneous cleavage of two inteins, leading to the 1–42 thioester with the native N‐terminus. Ligation and refolding studies showed that the inherently labile Asp? Pro bond 139–140 was detrimental for the sequential C‐ to N‐terminal ligation. A reversed ligation sequence using glycopeptide hydrazides gave full‐length IL‐6 glycoproteins, which showed full bioactivity after efficient refolding and purification. 相似文献
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Ulf Prüsse Luca Bilancetti Marek Bučko Branko Bugarski Jozef Bukowski Peter Gemeiner Dorota Lewińska Verica Manojlovic Benjamin Massart Claudio Nastruzzi Viktor Nedovic Denis Poncelet Swen Siebenhaar Lucien Tobler Azzurra Tosi Alica Vikartovská Klaus-Dieter Vorlop 《Chemical Papers》2008,62(4):364-374
This paper describes the results of the round robin experiment “Bead production technologies” carried out during the COST
840 action “Bioencapsulation Innovation and Technologies” within the 5th Framework Program of the European Community. In this
round robin experiment, calcium alginate hydrogel beads with the diameter of (800 ± 100) μm were produced by the most common
bead production technologies using 0.5–4 mass % sodium alginate solutions as starting material. Dynamic viscosity of the alginate
solutions ranged from less than 50 mPa s up to more than 10000 mPa s. With the coaxial air-flow and electrostatic enhanced
dropping technologies as well as with the JetCutter technology in the soft-landing mode, beads were produced from all alginate
solutions, whereas the vibration technology was not capable to process the high-viscosity 3 % and 4 % alginate solutions.
Spherical beads were generated by the electrostatic and the JetCutter technologies. Slightly deformed beads were obtained
from high-viscosity alginate solutions using the coaxial airflow and from the 0.5 % and 2 % alginate solutions using the vibration
technology. The rate of bead production using the JetCutter was about 10 times higher than with the vibration technology and
more than 10000 times higher than with the coaxial air-flow and electrostatic technology.
In memory of our colleague Stefan Rosinski 相似文献
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Polymorphism - integrated approach from high-throughput screening to crystallization optimization 总被引:3,自引:0,他引:3
Hilfiker R. Berghausen J. Blatter F. Burkhard A. De Paul S. M. Freiermuth B. Geoffroy A. Hofmeier U. Marcolli C. Siebenhaar B. Szelagiewicz M. Vit A. von Raumer M. 《Journal of Thermal Analysis and Calorimetry》2003,73(2):429-440
Crystal structure (polymorphism) as well as crystal shape (morphology) and size have a huge practical and commercial impact
on active substances all the way from research to manufacture of the final product. For an optimal development process, it
is important to have an integrated approach to these issues ranging from a systematic polymorphism screening to a controlled
scale-up of the crystallization process. The polymorphism program has to be tailored according to the development stage. Particularly
suitable for an early development stage is a high-throughput polymorphism screening, which is the basis for a more thorough
investigation if the product proceeds further in development. Such a comprehensive polymorphism investigation involves further
crystallization experiments and extensive physicochemical characterization of the various forms. In this article the high-throughput
polymorphism screening method that we have developed is described. Using carbamazepine as an example, the power of this high-throughput
polymorphism screening system is demonstrated. Not only were all published forms found, but also new forms were identified.
In the second part of the article, important considerations for crystallization optimization are discussed, again using the
example of carbamazepine.
This revised version was published online in July 2006 with corrections to the Cover Date. 相似文献
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