3wg8

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<StructureSection load='3wg8' size='340' side='right' caption='[[3wg8]], [[Resolution|resolution]] 2.30&Aring;' scene=''>
<StructureSection load='3wg8' size='340' side='right' caption='[[3wg8]], [[Resolution|resolution]] 2.30&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>[[3wg8]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3WG8 OCA]. <br>
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<table><tr><td colspan='2'>[[3wg8]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3WG8 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3WG8 FirstGlance]. <br>
</td></tr><tr><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=6AS:(2Z,4E)-5-[(1S)-3-(HEXYLSULFANYL)-1-HYDROXY-2,6,6-TRIMETHYL-4-OXOCYCLOHEX-2-EN-1-YL]-3-METHYLPENTA-2,4-DIENOIC+ACID'>6AS</scene><br>
</td></tr><tr><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=6AS:(2Z,4E)-5-[(1S)-3-(HEXYLSULFANYL)-1-HYDROXY-2,6,6-TRIMETHYL-4-OXOCYCLOHEX-2-EN-1-YL]-3-METHYLPENTA-2,4-DIENOIC+ACID'>6AS</scene><br>
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<tr><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Glucokinase Glucokinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.1.2 2.7.1.2] </span></td></tr>
 
<tr><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3wg8 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3wg8 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3wg8 RCSB], [http://www.ebi.ac.uk/pdbsum/3wg8 PDBsum]</span></td></tr>
<tr><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3wg8 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3wg8 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3wg8 RCSB], [http://www.ebi.ac.uk/pdbsum/3wg8 PDBsum]</span></td></tr>
<table>
<table>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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The plant stress hormone abscisic acid (ABA) is critical for several abiotic stress responses. ABA signaling is normally repressed by group-A protein phosphatases 2C (PP2Cs), but stress-induced ABA binds Arabidopsis PYR/PYL/RCAR (PYL) receptors, which then bind and inhibit PP2Cs. X-ray structures of several receptor-ABA complexes revealed a tunnel above ABA's 3' ring CH that opens at the PP2C binding interface. Here, ABA analogs with sufficiently long 3' alkyl chains were predicted to traverse this tunnel and block PYL-PP2C interactions. To test this, a series of 3'-alkylsulfanyl ABAs were synthesized with different alkyl chain lengths. Physiological, biochemical and structural analyses revealed that a six-carbon alkyl substitution produced a potent ABA antagonist that was sufficiently active to block multiple stress-induced ABA responses in vivo. This study provides a new approach for the design of ABA analogs, and the results validated structure-based design for this target class.
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Designed abscisic acid analogs as antagonists of PYL-PP2C receptor interactions.,Takeuchi J, Okamoto M, Akiyama T, Muto T, Yajima S, Sue M, Seo M, Kanno Y, Kamo T, Endo A, Nambara E, Hirai N, Ohnishi T, Cutler SR, Todoroki Y Nat Chem Biol. 2014 Jun;10(6):477-82. doi: 10.1038/nchembio.1524. Epub 2014 May, 4. PMID:24792952<ref>PMID:24792952</ref>
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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</div>
== References ==
== References ==
<references/>
<references/>

Revision as of 07:00, 11 June 2014

Crystal structure of the abscisic acid receptor PYR1 in complex with an antagonist AS6

3wg8, resolution 2.30Å

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