Auxin molecular field maps define AUX1 selectivity: many auxin herbicides are not substrates
Jazyk angličtina Země Velká Británie, Anglie Médium print-electronic
Typ dokumentu časopisecké články, práce podpořená grantem
Grantová podpora
BB/G023972/1
Biotechnology and Biological Sciences Research Council - United Kingdom
BB/L001489/1
Biotechnology and Biological Sciences Research Council - United Kingdom
PubMed
29265374
DOI
10.1111/nph.14950
Knihovny.cz E-zdroje
- Klíčová slova
- auxin transport, cheminformatics, herbicide, herbicide resistance, molecular field maps, pharmacophore, structure-activity relationship, uptake carrier,
- MeSH
- Arabidopsis metabolismus MeSH
- biologické modely MeSH
- biotest MeSH
- herbicidy metabolismus MeSH
- indoly metabolismus MeSH
- inhibiční koncentrace 50 MeSH
- kořeny rostlin růst a vývoj MeSH
- kyselina 2,4-dichlorfenoxyoctová metabolismus MeSH
- kyseliny indoloctové metabolismus MeSH
- mutace genetika MeSH
- proteiny huseníčku metabolismus MeSH
- semenáček růst a vývoj MeSH
- substrátová specifita MeSH
- tabák cytologie MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Názvy látek
- AUX1 protein, Arabidopsis MeSH Prohlížeč
- herbicidy MeSH
- indoly MeSH
- kyselina 2,4-dichlorfenoxyoctová MeSH
- kyseliny indoloctové MeSH
- proteiny huseníčku MeSH
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.
Rothamsted Research Harpenden AL5 2JQ UK
School of Life Sciences University of Warwick Gibbet Hill Road Coventry CV4 7AL UK
Citace poskytuje Crossref.org
Advances in Understanding the Mechanism of Action of the Auxin Permease AUX1
