Literature DB >> 23517565

N-methyldihydroquinazolinone derivatives of Retro-2 with enhanced efficacy against Shiga toxin.

Romain Noel1, Neetu Gupta, Valérie Pons, Amélie Goudet, Maria Daniela Garcia-Castillo, Aurélien Michau, Jennifer Martinez, David-Alexandre Buisson, Ludger Johannes, Daniel Gillet, Julien Barbier, Jean-Christophe Cintrat.   

Abstract

The Retro-2 molecule protects cells against Shiga toxins by specifically blocking retrograde transport from early endosomes to the trans-Golgi network. A SAR study has been carried out to identify more potent compounds. Cyclization and modifications of Retro-2 led to a compound with roughly 100-fold improvement of the EC50 against Shiga toxin cytotoxicity measured in a cell protein synthesis assay. We also demonstrated that only one enantiomer of the dihydroquinazolinone reported herein is bioactive.

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Year:  2013        PMID： 23517565     DOI： 10.1021/jm4002346

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  25 in total

Review 1.  Retrograde transport of protein toxins through the Golgi apparatus.

Authors:  Kirsten Sandvig; Tore Skotland; Bo van Deurs; Tove Irene Klokk
Journal:  Histochem Cell Biol       Date:  2013-06-14       Impact factor: 4.304

2.  Antisecretory factor peptide AF-16 inhibits the secreted autotransporter toxin-stimulated transcellular and paracellular passages of fluid in cultured human enterocyte-like cells.

Authors:  Valérie Nicolas; Vanessa Liévin-Le Moal
Journal:  Infect Immun       Date:  2014-12-22       Impact factor: 3.441

3.  Inhibition of diverse opportunistic viruses by structurally optimized retrograde trafficking inhibitors.

Authors:  Dhimant Desai; Matthew Lauver; Alexandria Ostman; Linda Cruz; Kevin Ferguson; Ge Jin; Brianne Roper; Daniel Brosius; Aron Lukacher; Shantu Amin; Nick Buchkovich
Journal:  Bioorg Med Chem       Date:  2019-03-13       Impact factor: 3.641

4.  (S)-N-Methyldihydroquinazolinones are the Active Enantiomers of Retro-2 Derived Compounds against Toxins.

Authors:  Neetu Gupta; Valérie Pons; Romain Noël; David-Alexandre Buisson; Aurélien Michau; Ludger Johannes; Daniel Gillet; Julien Barbier; Jean-Christophe Cintrat
Journal:  ACS Med Chem Lett       Date:  2013-12-04       Impact factor: 4.345

5.  Retrograde Transport from Early Endosomes to the trans-Golgi Network Enables Membrane Wrapping and Egress of Vaccinia Virus Virions.

Authors:  Gilad Sivan; Andrea S Weisberg; Jeffrey L Americo; Bernard Moss
Journal:  J Virol       Date:  2016-09-12       Impact factor: 5.103

6.  Potent Inhibition of Human Cytomegalovirus by Modulation of Cellular SNARE Syntaxin 5.

Authors:  Linda Cruz; Nicholas T Streck; Kevin Ferguson; Trisha Desai; Dhimant H Desai; Shantu G Amin; Nicholas J Buchkovich
Journal:  J Virol       Date:  2016-12-16       Impact factor: 5.103

7.  Syntaxin 5-dependent retrograde transport to the trans-Golgi network is required for adeno-associated virus transduction.

Authors:  Mathieu E Nonnenmacher; Jean-Christophe Cintrat; Daniel Gillet; Thomas Weber
Journal:  J Virol       Date:  2014-11-19       Impact factor: 5.103

8.  Structural optimization of a retrograde trafficking inhibitor that protects cells from infections by human polyoma- and papillomaviruses.

Authors:  Daniel W Carney; Christian D S Nelson; Bennett D Ferris; Julia P Stevens; Alex Lipovsky; Teymur Kazakov; Daniel DiMaio; Walter J Atwood; Jason K Sello
Journal:  Bioorg Med Chem       Date:  2014-07-10       Impact factor: 3.641

Review 9.  Retrograde trafficking of AB₅ toxins: mechanisms to therapeutics.

Authors:  Somshuvra Mukhopadhyay; Adam D Linstedt
Journal:  J Mol Med (Berl)       Date:  2013-05-12       Impact factor: 4.599

Review 10.  JC polyomavirus attachment, entry, and trafficking: unlocking the keys to a fatal infection.

Authors:  Melissa S Maginnis; Christian D S Nelson; Walter J Atwood
Journal:  J Neurovirol       Date:  2014-07-31       Impact factor: 2.643
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