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Insect contains diverse forms of chitin to constitute unique physical barriers including exoskeleton and peritrophic matrix.Chitin-remodeling enzymes that play key roles during insect metamorphosis attract much attention in view of entomology and plant protection.We previously reported that OfHexl, the evolved β-N-acetyl-D-hexosaminidase (EC 3.2.1.52) from the insect Ostrinia furnacalis (one of the most destructive pests), was an insect-evolved enzyme to function in chitin degradation.The crystal structure of Of Hexl gives structural details of the difference between insect and human enzymes.Based on structural difference, we designed and synthesized highly specific and efficient inhibitors against OfHex1.In this presentation,we focus on the discovery process of how to explore insect-specific inhibitors.