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| | ==Crystal Structure of DAD2 in complex with tolfenamic acid== | | ==Crystal Structure of DAD2 in complex with tolfenamic acid== |
| - | <StructureSection load='6ap6' size='340' side='right' caption='[[6ap6]], [[Resolution|resolution]] 1.65Å' scene=''> | + | <StructureSection load='6ap6' size='340' side='right'caption='[[6ap6]], [[Resolution|resolution]] 1.65Å' scene=''> |
| | == Structural highlights == | | == Structural highlights == |
| - | <table><tr><td colspan='2'>[[6ap6]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Pethy Pethy]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6AP6 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6AP6 FirstGlance]. <br> | + | <table><tr><td colspan='2'>[[6ap6]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Petunia_x_hybrida Petunia x hybrida]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6AP6 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=6AP6 FirstGlance]. <br> |
| - | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=TLF:2-[(3-CHLORO-2-METHYLPHENYL)AMINO]BENZOIC+ACID'>TLF</scene></td></tr> | + | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.65Å</td></tr> |
| - | <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[4dnp|4dnp]]</td></tr> | + | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=TLF:2-[(3-CHLORO-2-METHYLPHENYL)AMINO]BENZOIC+ACID'>TLF</scene></td></tr> |
| - | <tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">DAD2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=4102 PETHY])</td></tr>
| + | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=6ap6 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6ap6 OCA], [https://pdbe.org/6ap6 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=6ap6 RCSB], [https://www.ebi.ac.uk/pdbsum/6ap6 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=6ap6 ProSAT]</span></td></tr> |
| - | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6ap6 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6ap6 OCA], [http://pdbe.org/6ap6 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6ap6 RCSB], [http://www.ebi.ac.uk/pdbsum/6ap6 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6ap6 ProSAT]</span></td></tr> | + | |
| | </table> | | </table> |
| | + | == Function == |
| | + | [https://www.uniprot.org/uniprot/DAD2_PETHY DAD2_PETHY] |
| | <div style="background-color:#fffaf0;"> | | <div style="background-color:#fffaf0;"> |
| | == Publication Abstract from PubMed == | | == Publication Abstract from PubMed == |
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| | __TOC__ | | __TOC__ |
| | </StructureSection> | | </StructureSection> |
| - | [[Category: Pethy]] | + | [[Category: Large Structures]] |
| - | [[Category: Hamiaux, C]] | + | [[Category: Petunia x hybrida]] |
| - | [[Category: Alpha/beta hydrolase]] | + | [[Category: Hamiaux C]] |
| - | [[Category: Plant protein]]
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| Structural highlights
Function
DAD2_PETHY
Publication Abstract from PubMed
The strigolactone (SL) family of plant hormones regulates a broad range of physiological processes affecting plant growth and development and also plays essential roles in controlling interactions with parasitic weeds and symbiotic fungi. Recent progress elucidating details of SL biosynthesis, signalling, and transport offer many opportunities for discovering new plant growth regulators via chemical interference. Here, using high throughput screening and downstream biochemical assays, we identified N-phenylanthranilic acid derivatives as potent inhibitors of the SL receptors from petunia (DAD2), rice (OsD14) and Arabidopsis (AtD14). Crystal structures of DAD2 and OsD14 in complex with inhibitors further provided detailed insights into the inhibition mechanism, and in silico modeling of 19 other plant strigolactone receptors suggested that these compounds are active across a large range of plant species. Altogether, these results provide chemical tools for investigating SL signaling and further define a framework for structure-based approaches to design and validate optimized inhibitors of SL receptors for specific plant targets.
Inhibition of strigolactone receptors by N-phenylanthranilic acid derivatives: structural and functional insights.,Hamiaux C, Drummond RSM, Luo Z, Lee HW, Sharma P, Janssen BJ, Perry NB, Denny WA, Snowden KC J Biol Chem. 2018 Mar 9. pii: RA117.001154. doi: 10.1074/jbc.RA117.001154. PMID:29523686[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
References
- ↑ Hamiaux C, Drummond RSM, Luo Z, Lee HW, Sharma P, Janssen BJ, Perry NB, Denny WA, Snowden KC. Inhibition of strigolactone receptors by N-phenylanthranilic acid derivatives: structural and functional insights. J Biol Chem. 2018 Mar 9. pii: RA117.001154. doi: 10.1074/jbc.RA117.001154. PMID:29523686 doi:http://dx.doi.org/10.1074/jbc.RA117.001154
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