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Vintonyak V.V.,Max Planck Institute For Molekulare Physiologie | Warburg K.,Max Planck Institute For Molekulare Physiologie | Warburg K.,TU Dortmund | Kruse H.,University of Munster | And 5 more authors.
Angewandte Chemie - International Edition | Year: 2010

(Figure Presented) The best of 40000: Detailed structureactivity- relationship studies revealed key structural elements of indolin-2-on-3- spirothiazolidinones (see example) and their appropriate configuration for strong inhibitory activity against the pathophysiologically relevant title protein. © 2010 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim. Source


Krahn D.,University of Duisburg - Essen | Ottmann C.,Chemical Genomics Center der Max Planck Gesellschaft | Kaiser M.,University of Duisburg - Essen
Natural Product Reports | Year: 2011

Covering: up to March 2011 Syrbactin is a subordinate term for the syringolin, glidobactin and cepafungin natural product families. Their grouping is based on their related molecular frameworks, similar biosynthesis pathways and, most importantly, identical modes-of-action, being irreversible proteasome inhibition. With this report, we aim to review their chemical biology, describing their common, but also differential characteristics. © 2011 The Royal Society of Chemistry. Source


Clerc J.,Chemical Genomics Center der Max Planck Gesellschaft | Schellenberg B.,University of Zurich | Groll M.,TU Munich | Bachmann A.S.,University of Hawaii at Manoa | And 5 more authors.
European Journal of Organic Chemistry | Year: 2010

A convergent synthesis of SylA was developed and consists of the synthesis of a fully functionalized macrocycle, which is subsequently coupled with a urea moiety. For cyclization, ring-closing metathesis of a conformationally preorganized precursor was employed. The established synthetic route was then applied to the synthesis of SylA derivatives by using various peptidic side chains for decoration of the SylA macrocycle. The resulting collection of SylA analogues was tested for proteasome inhibition, revealing PEGylated SylA derivatives as the most potent proteasome inhibitors. © 2010 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim. Source


Kaschani F.,University of Duisburg - Essen | Clerc J.,University of Gottingen | Krahn D.,University of Duisburg - Essen | Bier D.,Chemical Genomics Center der Max Planck Gesellschaft | And 6 more authors.
Angewandte Chemie - International Edition | Year: 2012

Exceptionally specific: The natural-product-like structural complexity of a bicyclic hydantoin was exploited to generate the novel, highly specific activity-based profiling probe (ABPP) Mrl-Rh (Rh=rhodamine; see picture) for glyceraldehyde 3-phosphate dehydrogenases. This probe can be used to investigate activity changes of this enzyme class during plant-pathogen interactions. Copyright © 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim. Source


Stolze S.C.,Chemical Genomics Center der Max Planck Gesellschaft | Stolze S.C.,University of Duisburg - Essen | Meltzer M.,University of Duisburg - Essen | Ehrmann M.,University of Duisburg - Essen | And 2 more authors.
Chemical Communications | Year: 2010

The solid phase total synthesis of the marine cyanobacterial Ahp-cyclodepsipeptide Symplocamide A is reported as a model for a general route for the synthesis of tailor-made non-covalent serine protease inhibitors. © The Royal Society of Chemistry 2010. Source

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