Simple β-lactones are potent irreversible antagonists for strigolactone receptors

Strigolactones (SLs) are a class of plant hormones that play vital roles not only in the control of plant branching and early seedling growth, but also in mediating rhizospheric communication with root parasitic plants and symbiotic fungi¹. SL receptors in host and parasitic plants have recently been identified to be a group of α/β hydrolases^2,3,4,5,6,7, but not in arbuscular mycorrhizal fungi, which form symbiosis with more than 80% of land plants⁸.

Small-molecule inhibitors of SL signaling could be valuable research tools as well as lead compounds for agrochemical development to eradicate root parasitic plants. In this regard, a triazole-containing small molecule has been reported to inhibit the biosynthesis of SLs⁹. Recently, McCourt and co-workers¹⁰ have reported non-covalent antagonists of SL receptors with micromolar IC₅₀s by using small-molecule high-throughput screening. Based on the mechanistic understanding of SL perception^2,3, here we developed a group of β-lactones as potent covalent antagonists for strigolactone receptors with nanomolar IC₅₀s.

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