Virstatin Explained

Virstatin is a small molecule that inhibits the activity of the cholera protein, ToxT.^[1]

Its activity in cholera was first published in 2005 in a paper that described the screening of a chemical library in a phenotypic screen and subsequent testing of one of the hits in infected mice.^{[1] [2]}

The compound is an isoquinoline alkaloid^[3] and can be synthesized by a simple two-step synthesis^[4]

Notes and References

1. Anthouard R, DiRita VJ . Chemical biology applied to the study of bacterial pathogens . Infection and Immunity . 83 . 2 . 456–69 . February 2015 . 25404026 . 4294262 . 10.1128/IAI.02021-14 .
2. Hung DT, Shakhnovich EA, Pierson E, Mekalanos JJ . Small-molecule inhibitor of Vibrio cholerae virulence and intestinal colonization . Science . 310 . 5748 . 670–4 . October 2005 . 16223984 . 10.1126/science.1116739 . 2005Sci...310..670H . 30557147 . free .
3. Cushnie TP, Cushnie B, Lamb AJ . Alkaloids: an overview of their antibacterial, antibiotic-enhancing and antivirulence activities . International Journal of Antimicrobial Agents . 44 . 5 . 377–86 . November 2014 . 25130096 . 10.1016/j.ijantimicag.2014.06.001 . 205171789 .
4. McDonald CE . 2009 . A Two-Step Synthesis of Virstatin, A Virulence Inhibitor of Vibrio cholerae. J. Chem. Educ. . 86 . 4. 482 . 10.1021/ed086p482 . 2009JChEd..86..482M .