| http://purl.uniprot.org/citations/18391211 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
| http://purl.uniprot.org/citations/18391211 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
| http://purl.uniprot.org/citations/18391211 | http://www.w3.org/2000/01/rdf-schema#comment | "The regulation of gene expression by the hormone auxin is a crucial mechanism in plant development. We have shown that the Arabidopsis F-box protein TIR1 is a receptor for auxin, and our recent structural work has revealed the molecular mechanism of auxin perception. TIR1 is the substrate receptor of the ubiquitin-ligase complex SCF(TIR1). Auxin binding enhances the interaction between TIR1 and its substrates, the Aux/IAA repressors, thereby promoting the ubiquitination and degradation of Aux/IAAs, altering the expression of hundreds of genes. TIR1 is the prototype of a new class of hormone receptor and the first example of an SCF ubiquitin-ligase modulated by a small molecule. Here, we describe the design, synthesis, and characterization of a series of auxin agonists and antagonists. We show these molecules are specific to TIR1-mediated events in Arabidopsis, and their mode of action in binding to TIR1 is confirmed by x-ray crystallographic analysis. Further, we demonstrate the utility of these probes for the analysis of TIR1-mediated auxin signaling in the moss Physcomitrella patens. Our work not only provides a useful tool for plant chemical biology but also demonstrates an example of a specific small-molecule inhibitor of F-box protein-substrate recruitment. Substrate recognition and subsequent ubiquitination by SCF-type ubiquitin ligases are central to many cellular processes in eukaryotes, and ubiquitin-ligase function is affected in several human diseases. Our work supports the idea that it may be possible to design small-molecule agents to modulate ubiquitin-ligase function therapeutically."xsd:string |
| http://purl.uniprot.org/citations/18391211 | http://purl.org/dc/terms/identifier | "doi:10.1073/pnas.0711146105"xsd:string |
| http://purl.uniprot.org/citations/18391211 | http://purl.org/dc/terms/identifier | "doi:10.1073/pnas.0711146105"xsd:string |
| http://purl.uniprot.org/citations/18391211 | http://purl.uniprot.org/core/author | "Nozaki H."xsd:string |
| http://purl.uniprot.org/citations/18391211 | http://purl.uniprot.org/core/author | "Nozaki H."xsd:string |
| http://purl.uniprot.org/citations/18391211 | http://purl.uniprot.org/core/author | "Hayashi K."xsd:string |
| http://purl.uniprot.org/citations/18391211 | http://purl.uniprot.org/core/author | "Hayashi K."xsd:string |
| http://purl.uniprot.org/citations/18391211 | http://purl.uniprot.org/core/author | "Kimura Y."xsd:string |
| http://purl.uniprot.org/citations/18391211 | http://purl.uniprot.org/core/author | "Kimura Y."xsd:string |
| http://purl.uniprot.org/citations/18391211 | http://purl.uniprot.org/core/author | "Tan X."xsd:string |
| http://purl.uniprot.org/citations/18391211 | http://purl.uniprot.org/core/author | "Tan X."xsd:string |
| http://purl.uniprot.org/citations/18391211 | http://purl.uniprot.org/core/author | "Zheng N."xsd:string |
| http://purl.uniprot.org/citations/18391211 | http://purl.uniprot.org/core/author | "Zheng N."xsd:string |
| http://purl.uniprot.org/citations/18391211 | http://purl.uniprot.org/core/author | "Kepinski S."xsd:string |
| http://purl.uniprot.org/citations/18391211 | http://purl.uniprot.org/core/author | "Kepinski S."xsd:string |
| http://purl.uniprot.org/citations/18391211 | http://purl.uniprot.org/core/author | "Hatate T."xsd:string |
| http://purl.uniprot.org/citations/18391211 | http://purl.uniprot.org/core/author | "Hatate T."xsd:string |
| http://purl.uniprot.org/citations/18391211 | http://purl.uniprot.org/core/date | "2008"xsd:gYear |
| http://purl.uniprot.org/citations/18391211 | http://purl.uniprot.org/core/date | "2008"xsd:gYear |
| http://purl.uniprot.org/citations/18391211 | http://purl.uniprot.org/core/name | "Proc. Natl. Acad. Sci. U.S.A."xsd:string |
| http://purl.uniprot.org/citations/18391211 | http://purl.uniprot.org/core/name | "Proc. Natl. Acad. Sci. U.S.A."xsd:string |
| http://purl.uniprot.org/citations/18391211 | http://purl.uniprot.org/core/pages | "5632-5637"xsd:string |
| http://purl.uniprot.org/citations/18391211 | http://purl.uniprot.org/core/pages | "5632-5637"xsd:string |