Structural highlights
FunctionPublication Abstract from PubMedThe authors previously reported that 2-methylbenzimidazole derivatives (MBIs) exhibit insect growth-regulating activity against the silkworm, Bombyx mori. However, despite their unique effects on juvenile hormone (JH)-related endocrine pathways, the precise mode of action of MBIs remained unclear. In the present study, the interactions between MBIs and the lepidopteran hemolymph JH-binding protein (JHBP), a key regulator of JH transport and activity, were investigated using multiple approaches, including in vitro binding affinity assays, X-ray crystallography, and molecular docking simulations. A series of MBIs bearing a 1-(4-alkoxybenzyl) group, which exhibited potent insect growth-regulating activity, showed high binding affinity and structural compatibility with the JH-binding pocket of JHBP. In contrast, 1-(4-alkylbenzyl) MBIs, which displayed weak or negligible insect growth-regulating activity, exhibited low affinity for JHBP. These findings suggest that the insect growth-regulating activity of MBIs is mediated through inhibition of JHBP function, likely by disrupting the precise regulation of JH concentration in the hemolymph during larval development and pupal metamorphosis. Structural Characteristics for the Interaction of 1-Benzyl-2-Methylbenzimidazoles as Insect Growth Regulators and Juvenile Hormone Binding Protein.,Gunasekara UKDSS, Inoue K, Fujimoto Z, Henmi S, Tsuchiya W, Suzuki R, Kutsuwada K, Ikeda I, Yamazaki T, Shiotsuki T Insects. 2026 Jun 22;17(6):657. doi: 10.3390/insects17060657. PMID:42355390[1] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. References
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