3wg8
From Proteopedia
Crystal structure of the abscisic acid receptor PYR1 in complex with an antagonist AS6
Structural highlights
Function[PYR1_ARATH] Receptor for abscisic acid (ABA) required for ABA-mediated responses such as stomatal closure and germination inhibition. Inhibits the activity of group-A protein phosphatases type 2C (PP2Cs) when activated by ABA.[1] [2] [3] Publication Abstract from PubMedThe 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. 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[4] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See AlsoReferences
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Categories: Arath | Akiyama, T | Cutler, S R | Endo, A | Hirai, N | Muto, T | Nambara, E | Ohnishi, T | Okamoto, M | Sue, M | Takeuchi, J | Todoroki, Y | Yajima, S | Abscisic acid | Hormone receptor
