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https://hdl.handle.net/2440/92371
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dc.contributor.author | Chua, K. | - |
dc.contributor.author | Pietsch, M. | - |
dc.contributor.author | Zhang, X. | - |
dc.contributor.author | Hautmann, S. | - |
dc.contributor.author | Chan, H. | - |
dc.contributor.author | Bruning, J. | - |
dc.contributor.author | Gütschow, M. | - |
dc.contributor.author | Abell, A. | - |
dc.date.issued | 2014 | - |
dc.identifier.citation | Angewandte Chemie International Edition, 2014; 53(30):7828-7831 | - |
dc.identifier.issn | 1433-7851 | - |
dc.identifier.issn | 1521-3773 | - |
dc.identifier.uri | http://hdl.handle.net/2440/92371 | - |
dc.description.abstract | There is a real need for simple structures that define a β-strand conformation, a secondary structure that is central to peptide-protein interactions. For example, protease substrates and inhibitors almost universally adopt this geometry on active site binding. A planar pyrrole is used to replace two amino acids of a peptide backbone to generate a simple macrocycle that retains the required geometry for active site binding. The resulting β-strand templates have reduced peptide character and provide potent protease inhibitors with the attachment of an appropriate amino aldehyde to the C-terminus. Picomolar inhibitors of cathepsin L and S are reported and the mode of binding of one example to the model protease chymotrypsin is defined by X-ray crystallography. | - |
dc.description.statementofresponsibility | Krystle C. H. Chua, Markus Pietsch, Xiaozhou Zhang, Stephanie Hautmann, Hon Y. Chan, John B. Bruning, Michael Gütschow, and Andrew D. Abell | - |
dc.language.iso | en | - |
dc.publisher | Wiley | - |
dc.rights | © 2014 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim | - |
dc.source.uri | http://dx.doi.org/10.1002/anie.201404301 | - |
dc.subject | inhibitors; macrocycles; peptidomimetics; proteases; β-strands | - |
dc.title | Macrocyclic protease inhibitors with reduced peptide character | - |
dc.type | Journal article | - |
dc.identifier.doi | 10.1002/anie.201404301 | - |
pubs.publication-status | Published | - |
dc.identifier.orcid | Bruning, J. [0000-0002-6919-1824] | - |
dc.identifier.orcid | Abell, A. [0000-0002-0604-2629] | - |
Appears in Collections: | Aurora harvest 2 IPAS publications |
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