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M48U1 CD4 mimetic has a sustained inhibitory effect on cell-associated HIV-1 by attenuating virion infectivity through gp120 shedding

Philippe Selhorst1, Katrijn Grupping1, Tommy Tong2, Ema T Crooks2, Loïc Martin3, Guido Vanham14, James M Binley2 and Kevin K Ariën1*

  • * Corresponding author: Kevin K Ariën

  • † Equal contributors

Author Affiliations

1 Department of Biomedical Sciences, Unit of Virology, Institute of Tropical Medicine, Antwerp, B-2000, Belgium

2 Torrey Pines Institute for Molecular Studies, San Diego, CA 92121, USA

3 Commissariat à l'énergie atomique et aux énergies alternatives, iBiTecS, SIMOPRO, Gif sur Yvette, F-91191, France

4 Faculty of Pharmaceutical, Biomedical and Veterinary Sciences, University of Antwerp, Antwerp, B-2000, Belgium

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Retrovirology 2013, 10:12  doi:10.1186/1742-4690-10-12

Published: 1 February 2013



HIV-1 infected cells can establish new infections by crossing the vaginal epithelia and subsequently producing virus in a milieu that avoids the high microbicide concentrations of the vaginal lumen.


To address this problem, here, we report that pretreatment of HIV-infected peripheral blood mononuclear cells (PBMCs) with a 27 amino acid CD4-mimetic, M48U1, causes dramatic and prolonged reduction of infectious virus output, due to its induction of gp120 shedding.


M48U1 may, therefore, be valuable for prophylaxis of mucosal HIV-1 transmission.

HIV; Entry; CD4 binding site; gp120; Shedding; Inhibition