Retro-2

Retro-2 is a selective inhibitor of retrograde protein trafficking mediated by syntaxin-5 at the interface between the endosome and trans-Golgi network, with no discernable effects on other intracellular trafficking pathways.^1,2 Retro-2 inhibits ebolavirus infection with an EC₅₀ value of 12.2 µM and reduces ricin-induced toxicity by 2.7-fold when used at a concentration of 20 µM in HeLa cells.^2,3 Retro-2 also blocks JC polyomavirus, BK polyomavirus, and SV40 infectivity in Vero green monkey kidney epithelial cells in vitro (EC₅₀s = 28.4, 61.2, and 58.6 µM, respectively).⁴ In mouse models, Retro-2 improves survival and reduces symptoms following infection with Shiga toxin-producing E. coli when administered at a dose of 100 mg/kg and protects against ricin challenge when administered prophylactically at a dose of 2 mg/kg.^2,5

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1. Nonnenmacher, M.E., Cintrat, J.C., Gillet, D., et al. Syntaxin 5-dependent retrograde transport to the trans-Golgi network is required for adeno-associated virus transduction. J. Virol. 89(3), 1673-1687 (2015).

2. Stechmann, B., Bai, S.K., Gobbo, E., et al. Inhibition of retrograde transport protects mice from lethal ricin challenge. Cell 141(2), 231-242 (2010).

3. Shtanko, O., Sakurai, Y., Reyes, A.N., et al. Retro-2 and its dihydroquinazolinone derivatives inhibit filovirus infection. Antiviral Res. 149, 154-163 (2018).

4. Nelson, C.D., Carney, D.W., Derdowski, A., et al. A retrograde trafficking inhibitor of ricin and Shiga-like toxins inhibits infection of cells by human and monkey polyomaviruses. MBio 4(6), e00729-00713 (2013).

5. Secher, T., Shima, A., Hinsinger, K., et al. Retrograde trafficking inhibitor of Shiga toxins reduces morbidity and mortality of mice infected with enterohemorrhagic Escherichia coli. Antimicrob. Agents Chemother. 59(8), 5010-5013 (2015).