Aminopeptidases as relevant therapeutic targets in cancer, autoimmune diseases and tropical diseases

Aminopeptidases have been involved in metabolic disorders (angiogenesis, autoimmune diseases) and are essential for the development of pathogenic agents (Plasmodium, Toxoplasma…). Our research interests are focused on the design of potential inhibitors for the M1(alanyl) and M17(leucyl) aminopeptidase families. We have discovered a modular platform, based on aminobenzosuberone scaffold, inhibiting potently and selectively each aminopeptidase family. Several medicinal chemistry programs (recombinant enzymes, SAR studies, prodrugs) are currently in progress:

 

Aminopeptidase target Disease Collaboration
Aminopeptidase N/CD13 Angiogenesis, cancer Dr. D. Guenot (Unistra, Strasbourg, France)
PfA-M1 and PfA-M17 hemoglobin catabolism, malaria Prof. I. Florent (MNHN, Paris, France)
Endoplasmic Reticulum AminoPeptidase 1/2 antigen presentation, ankylosing spondylitis Dr E. Stratikos (CNRS, Athens, Greece)

To learn more about this research, feel free to contact :
Sébastien Albrecht, sebastien.albrecht@uha.fr
Céline Tarnus, celine.tarnus@uha.fr
Marjorie Schmitt, marjorie.schmitt@uha.fr
Emmanuel Salomon, emmanuel.salomon@uha.fr

Selected references:
C. Schmitt, M. Voegelin, A. Marin, M. Schmitt, F. Schegg, P. Hénon, D. Guenot, C. Tarnus, Bioorg. Med. Chem. 2013, 21, 2135-2144.
Link: http://www.sciencedirect.com/science/article/pii/S0968089612010115

M. Al-Lakkis-Wehbe, B. Chaillou, A. Defoin, S. Albrecht, C. Tarnus, Bioorg. Med. Chem. 2013, 21, 6447-6455.
Link: http://www.sciencedirect.com/science/article/pii/S0968089613007475

C. Maiereanu, C. Schmitt, N. Schifano-Faux, D. Le Nouën, A. Defoin, C. Tarnus, Bioorg. Med. Chem. 2011, 19, 5719-5733.
Link: http://www.sciencedirect.com/science/article/pii/S0968089611005463

 

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