Rational design of inhibitors of VirA–VirG two-component signal transduction

J Maresh, J Zhang, YL Tzeng, NA Goodman…

Index: Maresh, Justin; Zhang, Jin; Tzeng, Yih-Ling; Goodman, Nora A.; Lynn, David G. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 12 p. 3281 - 3286

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Citation Number: 10

Abstract

VirA–VirG two-component system regulates the vir (virulence) operon in response to specific host factors (xenognosins) in the plant pathogen Agrobacterium tumefaciens. Using whole cell assays, stable inhibitors inspired by the labile natural benzoxazinone inhibitor HDMBOA are developed. It is found that aromatic aldehydes represent a minimal structural unit for activity. In particular, 3-hydroxy-4, 6-dimethoxy-3H-isobenzofuran-1-one (HDI) was found ...