Bactericidal bissulfone B7 targets bacterial pyruvate kinase to impair bacterial biology and pathogenicity in plants  

作　　者：Awei Zhang Haizhen Zhang Ronghua Wang Hongfu He Baoan Song Runjiang Song 

机构地区：[1]National Key Laboratory of Green Pesticide,Key Laboratory of Green Pesticide and Agricultural Bioengineering,Ministry of Education,Center for R&D of Fine Chemicals of Guizhou University,Guiyang 550025,China

出　　处：《Science China(Life Sciences)》2024年第2期391-402,共12页中国科学（生命科学英文版）

基　　金：supported by the National Key Research and Development Program of China(2022YFD1700300);Program of Introducing Talents of Discipline to Universities of China(111Program,D20023);the Key Technologies R&D Program of Guizhou Province in China(2017-5788-1)。

摘　　要：The prevention and control of rice bacterial leaf blight(BLB)disease has not yet been achieved due to the lack of effective agrochemicals and available targets.Herein,we develop a series of novel bissulfones and a novel target with a unique mechanism to address this challenge.The developed bissulfones can control Xanthomonas oryzae pv.oryzae(Xoo),and 2-(bis(methylsulfonyl)methylene)-N-(4-chlorophenyl)hydrazine-1-carboxamide(B_(7))is more effective than the commercial drugs thiodiazole copper(TC)and bismerthiazol(BT).Pyruvate kinase(PYK)in Xoo has been identified for the first time as the target protein of our bissulfone B_(7).PYK modulates bacterial virulence via a CRP-like protein(Clp)/two-component system regulatory protein(reg R)axis.The elucidation of this pathway facilitates the use of B_(7)to reduce PYK expression at the transcriptional level,block PYK activity at the protein level,and impair the interaction within the PYK-Clp-reg R complex via competitive inhibition,thereby attenuating bacterial biology and pathogenicity.This study offers insights into the molecular and mechanistic aspects underlying anti-Xoo strategies that target PYK.We believe that these valuable discoveries will be used for bacterial disease control in the future.

关 键 词：2-bissulfone-N-phenylhydrazine-1-carboxamide derivatives XOO antibacterial activities pyruvate kinase regulatory mechanism 

分 类 号：S482.2[农业科学—农药学]