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Auxin molecular field maps define AUX1 selectivity: many auxin herbicides are not substrates
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SYSNO ASEP 0488687 Document Type J - Journal Article R&D Document Type Journal Article Subsidiary J Článek ve WOS Title Auxin molecular field maps define AUX1 selectivity: many auxin herbicides are not substrates Author(s) Hoyerová, Klára (UEB-Q) RID, ORCID
Hošek, Petr (UEB-Q) ORCID
Quareshy, M. (GB)
Li, J. (CN)
Klíma, Petr (UEB-Q) RID, ORCID
Kubeš, Martin (UEB-Q) RID, ORCID
Yemm, A. A. (GB)
Neve, P. (GB)
Tripathi, A. (GB)
Bennett, M.J. (GB)
Napier, R. M. (GB)Number of authors 11 Source Title New Phytologist - ISSN 0028-646X
Roč. 217, č. 4 (2018), s. 1625-1639Number of pages 15 s. Language eng - English Country GB - United Kingdom Keywords auxin transport ; cheminformatics ; herbicide ; herbicide resistance ; molecular field maps ; pharmacophore ; structure–activity relationship ; uptake carrier Subject RIV ED - Physiology OECD category Cell biology R&D Projects GA16-19557S GA ČR - Czech Science Foundation (CSF) LD15137 GA MŠMT - Ministry of Education, Youth and Sports (MEYS) Institutional support UEB-Q - RVO:61389030 UT WOS 000424284400022 EID SCOPUS 85041613393 DOI 10.1111/nph.14950 Annotation Developmental responses to auxin are regulated by facilitated uptake and efflux, but detailed molecular understanding of the carrier proteins is incomplete. We have used pharmacological tools to explore the chemical space that defines substrate preferences for the auxin uptake carrier AUX1. Total and partial loss-of-function aux1 mutants were assessed against wild-type for dose-dependent resistance to a range of auxins and analogues. We then developed an auxin accumulation assay with associated mathematical modelling to enumerate accurate IC 50 values for a small library of auxin analogues. The structure activity relationship data were analysed using molecular field analyses to create a pharmacophoric atlas of AUX1 substrates. The uptake carrier exhibits a very high level of selectivity towards small substrates including the natural indole-3-acetic acid, and the synthetic auxin 2,4-dichlorophenoxyacetic acid. No AUX1 activity was observed for herbicides based on benzoic acid (dicamba), pyridinyloxyacetic acid (triclopyr) or the 6-arylpicolinates (halauxifen), and very low affinity was found for picolinic acid-based auxins (picloram) and quinolinecarboxylic acids (quinclorac). The atlas demonstrates why some widely used auxin herbicides are not, or are very poor substrates. We list molecular descriptors for AUX1 substrates and discuss our findings in terms of herbicide resistance management. Workplace Institute of Experimental Botany Contact David Klier, knihovna@ueb.cas.cz, Tel.: 220 390 469 Year of Publishing 2019
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