Auxin molecular field maps define AUX1 selectivity : many auxin herbicides are not substrates

Bibliographische Detailangaben
Veröffentlicht in:	The New phytologist. - 1979. - 217(2018), 4 vom: 20. März, Seite 1625-1639
1. Verfasser:	Hoyerova, Klara (VerfasserIn)
Weitere Verfasser:	Hosek, Petr, Quareshy, Mussa, Li, Jun, Klima, Petr, Kubes, Martin, Yemm, Antony A, Neve, Paul, Tripathi, Ashutosh, Bennett, Malcolm J, Napier, Richard M
Format:	Online-Aufsatz
Sprache:	English
Veröffentlicht:	2018
Zugriff auf das übergeordnete Werk:	The New phytologist
Schlagworte:	Journal Article Research Support, Non-U.S. Gov't auxin transport cheminformatics herbicide herbicide resistance molecular field maps pharmacophore structure-activity relationship uptake carrier mehr... AUX1 protein, Arabidopsis Arabidopsis Proteins Herbicides Indoleacetic Acids Indoles 2,4-Dichlorophenoxyacetic Acid 2577AQ9262

Beschreibung
Zusammenfassung:	© 2017 The Authors. New Phytologist © 2017 New Phytologist Trust. 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 IC50 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
Beschreibung:	Date Completed 13.09.2019 Date Revised 13.12.2023 published: Print-Electronic Citation Status MEDLINE
ISSN:	1469-8137
DOI:	10.1111/nph.14950