Structures and mechanisms of the Arabidopsis auxin transporter PIN3

Su, Nannan; Zhu, Aiqin; Tao, Xin; Ding, Ziqian; Chang, Shenghai; Ye, Fan; Zhang, Yan; Zhao, Cheng; Chen, Qian; Wang, Jiangqin; Zhou, Chen; Guo, Yirong; Jiao, Shasha; Zhang, Sufen; Wen, Han; Ma, Lixin; Ye, Sheng; Zheng, Shao Jian; Yang, Fan; Wu, Shan; Guo, Jiangtao

doi:10.1038/s41586-022-05142-w

Cited by 56 publications

(40 citation statements)

References 59 publications

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“…Recently, crystal structure analysis of the PIN protein showed that NPA inhibits auxin transport by binding to PIN auxin efflux carrier proteins 8,9 . NPA induces auxin accumulation in root tips by inhibiting auxin transport, resulting in the accumulation of DR5:GFP signal in the root tips of NPA-treated roots (Fig.…”

Section: Resultsmentioning

confidence: 99%

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Design and synthesis of strong root gravitropism inhibitors with no concomitant growth inhibition

Nishimura

Makigawa

Sun

et al. 2023

Sci Rep

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Herein, we describe a highly potent gravitropic bending inhibitor with no concomitant growth inhibition. Previously, we reported that (2Z,4E)-5-phenylpenta-2,4-dienoic acid (ku-76) selectively inhibits root gravitropic bending of lettuce radicles at 5 μM. Based on the structure–activity relationship study of ku-76 as a lead compound, we designed and synthesized various C4-substituted analogs of ku-76. Among the analogs, 4-phenylethynyl analog exhibited the highest potency for gravitropic bending inhibition, which was effective at only 0.01 μM. Remarkably, 4-phenylethynyl analog is much more potent than the known inhibitor, NPA. Substitution in the para position on the aromatic ring of 4-phenylethynyl group was tolerated without diminished activity. In addition, evaluation using Arabidopsis indicated that 4-phenylethynyl analog inhibits gravitropism by affecting auxin distribution in the root tips. Based on the effects on Arabidopsis phenotypes, 4-phenylethynyl analog may be a novel inhibitor that differs in action from the previously reported auxin transport inhibitors.

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Section: Resultsmentioning

confidence: 99%

“…Recently, following the determination of the structure of PIN proteins, NPA was shown to inhibit auxin transport by binding directly to PIN proteins 8,9 . This indicates that compounds that universally inhibit the auxin efflux activity of PIN interfere not only with gravitropism but also with tissue growth.…”

Section: Discussionmentioning

confidence: 99%

Design and synthesis of strong root gravitropism inhibitors with no concomitant growth inhibition

Nishimura

Makigawa

Sun

et al. 2023

Sci Rep

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show abstract

“…Additionally, multiple PIN family members like PIN1, PIN2 and PIN3 are localized on the same plasma membrane and they form homo- or heterodimers in vivo, and their stability and polar auxin transport activity can be further regulated by endogenous flavonols (Teale et al ., 2021), phosphorylation (Huang et al ., 2010) and inhibited by 1-naphthylphthalamic acid (NPA) which binds to the same pocket as natural auxin IAA but with much higher affinity (Abas et al ., 2021, Su et al ., 2022, Yang et al ., 2022). However, not much is known on how molecular chaperones are associated with these proteins during their folding and targeting processes to the dedicated membranes.…”

Section: Discussionmentioning

confidence: 99%

Knockout of endoplasmic reticulum localized molecular chaperone HSP90.7 impairs seeding development and cellular auxin homeostasis in Arabidopsis

Noureddine

Hamidzada

et al. 2023

Preprint

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The Arabidopsis endoplasmic reticulum localized heat shock protein HSP90.7 modulates tissue differentiation and stress responses; however, complete knockout lines have not been previously reported. In this study, we identified and analyzed a mutant allele, hsp90.7-1, which did not express any protein and showed seedling lethality. Microscopic analyses revealed its essential role in male and female fertility, trichomes and root hairs development, proper chloroplast function, and in apical meristem maintenance and differentiation. Comparative transcriptome and proteome analyses also revealed a role of the protein in a multitude of cellular processes. Particularly, the auxin responsive pathway was specifically down-regulated in the hsp90.7-1 mutant seedlings. We measured a much-reduced auxin content in both root and shoot tissues. Through comprehensive histological and molecular analyses, we demonstrated PIN1 and PIN5 expressions were dramatically reduced in the mutant, and the TAA-YUCCA primary auxin biosynthesis pathway was also down-regulated, thus revealing a critical new role of HSP90.7 in the regulation of auxin responses. This study therefore not only fulfilled a gap in understanding the essential role of HSP90 paralogs in eukaryotes, but also provided a mechanistic insight on this molecular chaperone in regulating plant growth and development via modulating cellular auxin homeostasis.

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“…In African clawed frog oocyte heterologous expression system, quantitative measurement of auxin transportation confirmed the direct blockage of PIN‐mediated auxin efflux by NPA (Abas et al, 2021). Last year, three cryogenic electron microscopy (cryo‐EM) investigations on PIN8 (Ung et al, 2022), PIN1 (Yang et al, 2022), and PIN3 (Su et al, 2022) showed that NPA competes with IAA inside the PIN auxin efflux carriers. Updated reviews highlight these findings and point out questions for future research (Joshi and Napier, 2023; Ung et al, 2023).…”

Section: Introductionmentioning

confidence: 99%

A unique mutation in PIN‐FORMED1 and a genetic pathway for reduced sensitivity of Arabidopsis roots to N‐1‐naphthylphthalamic acid

Huang,

Chen,

Yang

et al. 2023

Physiologia Plantarum

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The small chemical N‐1‐naphthylphthalamic acid (NPA) has long been used as a polar auxin transport inhibitor. Recent biochemical and structural investigations have revealed that this molecule competes with the auxin IAA (indole‐3‐acetic acid) inside the PIN‐FORMED auxin efflux carriers. However, the existence of any mutations in PIN family proteins capable of uncoupling the docking of IAA from NPA remains unclear. We report that Arabidopsis thaliana seedlings overexpressing SMALL AUXIN UP RNA 41 were hypersensitive to NPA‐induced root elongation inhibition. We mutagenized this line to improve the genetic screening efficiency for NPA hyposensitivity mutants. Using bulked segregation analysis and mapping‐by‐sequencing assessment of these mutants, we identified a core genetic pathway for NPA‐induced root elongation inhibition, including genes required for auxin biosynthesis, transportation, and signaling. To evaluate specific changes of auxin signaling activity in mutant roots before and after NPA treatment, the DR5::GFP/DR5::YFP markers were introduced and observed. Most importantly, we discovered a unique mutation in the PIN1 protein, substituting a proline residue with leucine at position 584, leading to a loss of NPA sensitivity while keeping the auxin efflux capacity. Transforming the null mutant pin1‐201 with the PIN1::PIN1P584L‐GFP fusion construct rescued the PIN1 function and provided NPA hyposensitivity. The proline residue is predicted to be adjacent to a hinge in the middle region of the ninth transmembrane helix of PIN1 and is conserved from moss to higher plants. Our work may bring new insights into the engineering of NPA‐resistant PINs for auxin biology studies.

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Structures and mechanisms of the Arabidopsis auxin transporter PIN3

Cited by 56 publications

References 59 publications

Design and synthesis of strong root gravitropism inhibitors with no concomitant growth inhibition

Design and synthesis of strong root gravitropism inhibitors with no concomitant growth inhibition

Knockout of endoplasmic reticulum localized molecular chaperone HSP90.7 impairs seeding development and cellular auxin homeostasis in Arabidopsis

A unique mutation in PIN‐FORMED1 and a genetic pathway for reduced sensitivity of Arabidopsis roots to N‐1‐naphthylphthalamic acid

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