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Biological Chemistry

Editor-in-Chief: Brüne, Bernhard

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

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IMPACT FACTOR 2017: 3.022

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1437-4315
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Volume 393, Issue 10

Issues

Structural origins of AGC protein kinase inhibitor selectivities: PKA as a drug discovery tool

Espen Åberg
  • Norwegian Structural Biology Center, Department of Chemistry, University of Tromsø, N-9012 Tromsø, Norway
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/ Bjarte Lund
  • Norwegian Structural Biology Center, Department of Chemistry, University of Tromsø, N-9012 Tromsø, Norway
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/ Alexander Pflug
  • Norwegian Structural Biology Center, Department of Chemistry, University of Tromsø, N-9012 Tromsø, Norway
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/ Osman A.B.S.M. Gani
  • Norwegian Structural Biology Center, Department of Chemistry, University of Tromsø, N-9012 Tromsø, Norway
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/ Ulli Rothweiler
  • Norwegian Structural Biology Center, Department of Chemistry, University of Tromsø, N-9012 Tromsø, Norway
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/ Taianà M. de Oliveira
  • Norwegian Structural Biology Center, Department of Chemistry, University of Tromsø, N-9012 Tromsø, Norway
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/ Richard A. Engh
  • Corresponding author
  • Norwegian Structural Biology Center, Department of Chemistry, University of Tromsø, N-9012 Tromsø, Norway
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Published Online: 2012-09-08 | DOI: https://doi.org/10.1515/hsz-2012-0248

Abstract

The era of structure-based protein kinase inhibitor design began in the early 1990s with the determination of crystal structures of protein kinase A (PKA, or cyclic AMP-dependent kinase). Although many other protein kinases have since been extensively characterized, PKA remains a prototype for studies of protein kinase active conformations. It serves well as a model for the structural properties of AGC subfamily protein kinases, clarifying inhibitor selectivity profiles. Its reliable expression, constitutive activity, simple domain structure, and reproducible crystallizability have also made it a useful surrogate for the discovery of inhibitors of both established and emerging AGC kinase targets.

Keywords: anticancer; crystallography; drug design; phosphotransferase; surrogate

About the article

Corresponding author: Richard A. Engh, Norwegian Structural Biology Center, Department of Chemistry, University of Tromsø, N-9012 Tromsø, Norway


Received: 2012-07-09

Accepted: 2012-08-22

Published Online: 2012-09-08

Published in Print: 2012-10-01


Citation Information: , Volume 393, Issue 10, Pages 1121–1129, ISSN (Online) 1437-4315, ISSN (Print) 1431-6730, DOI: https://doi.org/10.1515/hsz-2012-0248.

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