Jump to ContentJump to Main Navigation
Show Summary Details
More options …

Biological Chemistry

Editor-in-Chief: Brüne, Bernhard

Editorial Board: Buchner, Johannes / Lei, Ming / Ludwig, Stephan / Sies, Helmut / Thomas, Douglas D. / Turk, Boris / Wittinghofer, Alfred

12 Issues per year

IMPACT FACTOR 2017: 3.022

CiteScore 2017: 2.81

SCImago Journal Rank (SJR) 2017: 1.562
Source Normalized Impact per Paper (SNIP) 2017: 0.705

See all formats and pricing
More options …
Volume 383, Issue 7-8


Trypsin Mutants for Structure-Based Drug Design: Expression, Refolding and Crystallisation

D. Rauh / S. Reyda / G. Klebe / M.T. Stubbs
Published Online: 2005-06-01 | DOI: https://doi.org/10.1515/BC.2002.148


New techniques in drug discovery are essential for the fast and efficient development of novel innovative drugs to deal with the challenges of the future. Structure determinations of various members of serine proteinases have provided a basis for computerbased drug design within this class of enzymes. In many proteins of interest, however, this course is blocked through a lack of suitable crystals. As a strategy for circumventing such problems, we have investigated the use of surrogate proteins for studying protein ligand interactions. To test the feasibility of this approach, we have chosen bovine trypsin as a scaffold to reconstruct the ligand binding site of factor Xa. The simple modular design of trypsin, its readiness to crystallise and straightforward handling lends itself to such drug design by proxy. The expression, folding, purification, crystallographic and kinetic characterisation of bovine trypsin forms with factor Xa phenotype are presented.

About the article

Published Online: 2005-06-01

Published in Print: 2002-08-27

Citation Information: Biological Chemistry, Volume 383, Issue 7-8, Pages 1309–1314, ISSN (Print) 1431-6730, DOI: https://doi.org/10.1515/BC.2002.148.

Export Citation

Citing Articles

Here you can find all Crossref-listed publications in which this article is cited. If you would like to receive automatic email messages as soon as this article is cited in other publications, simply activate the “Citation Alert” on the top of this page.

Janet Newman, Vincent J. Fazio, Tom T. Caradoc-Davies, Kim Branson, and Thomas S. Peat
Journal of Biomolecular Screening, 2009, Volume 14, Number 10, Page 1245
Stefan Grüner, Manuel Neeb, Luzi Jakob Barandun, Frank Sielaff, Christoph Hohn, Shun Kojima, Torsten Steinmetzer, François Diederich, and Gerhard Klebe
Biochimica et Biophysica Acta (BBA) - General Subjects, 2014, Volume 1840, Number 9, Page 2843
Ömür Çelikbıçak, Mehmet Atakay, Ülkü Güler, and Bekir Salih
Analytical Letters, 2014, Volume 47, Number 4, Page 707
Daniel Rauh, Gerhard Klebe, and Milton T. Stubbs
Journal of Molecular Biology, 2004, Volume 335, Number 5, Page 1325
Bernhard Stengl, Emmanuel A. Meyer, Andreas Heine, Ruth Brenk, François Diederich, and Gerhard Klebe
Journal of Molecular Biology, 2007, Volume 370, Number 3, Page 492
Michael J. Page, Christopher J. Carrell, and Enrico Di Cera
Journal of Molecular Biology, 2008, Volume 378, Number 3, Page 666
Daniel Rauh, Gerhard Klebe, Jörg Stürzebecher, and Milton T. Stubbs
Journal of Molecular Biology, 2003, Volume 330, Number 4, Page 761
Janet Newman, Olan Dolezal, Vincent Fazio, Tom Caradoc-Davies, and Thomas S. Peat
Journal of Computer-Aided Molecular Design, 2012, Volume 26, Number 5, Page 497
Michael Schöpfel, Anastasia Tziridis, Ulrich Arnold, and Milton T. Stubbs
ChemBioChem, 2011, Volume 12, Number 10, Page 1523
Armida Di Fenza, Andreas Heine, Ulrich Koert, and Gerhard Klebe
ChemMedChem, 2007, Volume 2, Number 3, Page 297

Comments (0)

Please log in or register to comment.
Log in