Novel Inhibitors of Indoleamine 2,3-Dioxygenase (IDO), a Target for Anti-Cancer Immunotherapy

Eduard Dolusic, Sébastien Blanc, Pierre Larrieu, Laurence Moineaux, Delphine Colette, Graeme Fraser, Vincent Stroobant, Luc Pilotte, Didier Colau, Johan Wouters, Bernard Masereel, Benoît Van den Eynde, Raphaël Frédérick

Résultats de recherche: Contribution à un événement scientifique (non publié)Poster

78 Téléchargements (Pure)

Résumé

Anti-cancer vaccination has so far shown a limited efficacy because cancer cells develop mechanisms of resisting or escaping immune rejection. The enzyme indoleamine 2,3-dioxygenase (IDO), which catalyzes the oxidative degradation of tryptophan, has been identified as an important actor in this process. It has been demonstrated that many human tumors express IDO in a constitutive manner. [1] The recent elucidation of the three-dimensional structure of IDO [2] provides a basis for the structure-based drug discovery and design of IDO inhibitors. In the present work, [3] we applied virtual screening to discover new IDO inhibitors. The potency of the most promising candidate (1) was confirmed in vitro (IC50 = 65 µM) and could be improved 5-fold by pharmacomodulations. A number of analogs were also active in a cellular test. A modeling study was undertaken in order to explain the SAR.
langue originaleAnglais
PagesBook of Abstracts, XVIIIème Journée Jeunes Chercheurs, 04/02/11, Paris, France
Nombre de pages1
Etat de la publicationPublié - 2011
EvénementXVIIIeme JOURNEE JEUNES CHERCHEURS - Paris, Faculte de Pharmacie, France
Durée: 4 févr. 2011 → …

Une conférence

Une conférenceXVIIIeme JOURNEE JEUNES CHERCHEURS
La villeParis, Faculte de Pharmacie, France
période4/02/11 → …

    Empreinte digitale

Contient cette citation

Dolusic, E., Blanc, S., Larrieu, P., Moineaux, L., Colette, D., Fraser, G., Stroobant, V., Pilotte, L., Colau, D., Wouters, J., Masereel, B., Van den Eynde, B., & Frédérick, R. (2011). Novel Inhibitors of Indoleamine 2,3-Dioxygenase (IDO), a Target for Anti-Cancer Immunotherapy. Book of Abstracts, XVIIIème Journée Jeunes Chercheurs, 04/02/11, Paris, France. Poster présenté � XVIIIeme JOURNEE JEUNES CHERCHEURS, Paris, Faculte de Pharmacie, France, .