ArticleProceedings of the National Academy of Sciences of the United States of America2021
Click-to-lead design of a picomolar ABA receptor antagonist with potent activity in vivo.
Article in Proceedings of the National Academy of Sciences of the United States of America, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers.
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Who cites it
23 citing papers in PubMed.
- High-throughput screening and structure-guided design of small molecules enable modulation of SAL-PAP stress signaling.Journal of experimental botany · 2026Article
- Accelerate Your Science: Direct-to-Biology Strategies in Medicinal Chemistry.Journal of medicinal chemistry · 2026Review
- Nanoscale Direct-to-Biology Optimization of Cdk2 Inhibitors.Journal of medicinal chemistry · 2026Article
- Computational design of dynamic biosensors for emerging synthetic opioids.Nature communications · 2026Article
- Corepressor AtSDR4L and its paralog regulate hormonal and hypoxia responses in multiple Arabidopsis seed compartments.Plant physiology · 2025Article
- RACK1A positively regulates opening of the apical hook inProceedings of the National Academy of Sciences of the United States of America · 2025Article
- A PIF-SAUR module safeguards hypocotyl elongation from ABA inhibition in the dark.Science advances · 2025Article
- Computational design of dynamic biosensors for emerging synthetic opioids.bioRxiv : the preprint server for biology · 2025Article
- BioCurve Analyzer: a web-based shiny app for analyzing biological response curves.Plant methods · 2025Article
- Chemical application improves stress resilience in plants.Plant molecular biology · 2025Review
- From Regulation to Application: The Role of Abscisic Acid in Seed and Fruit Development and Agronomic Production Strategies.International journal of molecular sciences · 2024Review
- Small chemical molecules regulating the phytohormone signalling alter the plant's physiological processes to improve stress adaptation, growth and productivity.Physiology and molecular biology of plants : an international journal of functional plant biology · 2024Review
- Stabilization of dimeric PYR/PYL/RCAR family members relieves abscisic acid-induced inhibition of seed germination.Nature communications · 2024Article
- The Discovery of Highly Efficient and Promising ABA Receptor Antagonists for Agricultural Applications Based on APAn Modification.Molecules (Basel, Switzerland) · 2024Article
- Null mutants of a tomato Rho of plants exhibit enhanced water use efficiency without a penalty to yield.Proceedings of the National Academy of Sciences of the United States of America · 2024Article
- Unveiling the crucial roles of abscisic acid in plant physiology: implications for enhancing stress tolerance and productivity.Frontiers in plant science · 2024Review
- Chemical disruption of ABA signaling overcomes high-temperature inhibition of seed germination and enhances seed priming responses.PloS one · 2024Article
- Structure-guided engineering of a receptor-agonist pair for inducible activation of the ABA adaptive response to drought.Science advances · 2023Article
- Examining Heterodimerization by Aryl C-N Coupling in Dynemicin Biosynthesis.ACS chemical biology · 2023Article
- Abscisic acid mimic-fluorine derivative 4 alleviates water deficit stress by regulating ABA-responsive genes, proline accumulation, CO2 assimilation, water use efficiency and better nutrient uptake in tomato plants.Frontiers in plant science · 2023Article
Corrections and comments
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Authors and funding
15 authors.
Funding
Abstract
Abscisic acid (ABA) is a key plant hormone that mediates both plant biotic and abiotic stress responses and many other developmental processes. ABA receptor antagonists are useful for dissecting and manipulating ABA's physiological roles in vivo. We set out to design antagonists that block receptor-PP2C interactions by modifying the agonist opabactin (OP), a synthetically accessible, high-affinity scaffold. Click chemistry was used to create an ∼4,000-member library of C4-diversified opabactin derivatives that were screened for receptor antagonism in vitro. This revealed a peptidotriazole motif shared among hits, which we optimized to yield antabactin (ANT), a pan-receptor antagonist. An X-ray crystal structure of an ANT-PYL10 complex (1.86 Å) reveals that ANT's peptidotriazole headgroup is positioned to sterically block receptor-PP2C interactions in the 4' tunnel and stabilizes a noncanonical closed-gate receptor conformer that partially opens to accommodate ANT binding. To facilitate binding-affinity studies using fluorescence polarization, we synthesized TAMRA-ANT. Equilibrium dissociation constants for TAMRA-ANT binding to
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.