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

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Abstract

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.
Original languageEnglish
PagesBook of Abstracts, XVIIIème Journée Jeunes Chercheurs, 04/02/11, Paris, France
Number of pages1
Publication statusPublished - 2011
EventXVIIIeme JOURNEE JEUNES CHERCHEURS - Paris, Faculte de Pharmacie, France
Duration: 4 Feb 2011 → …

Conference

ConferenceXVIIIeme JOURNEE JEUNES CHERCHEURS
CityParis, Faculte de Pharmacie, France
Period4/02/11 → …

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Dolusic, E., Blanc, S., Larrieu, P., Moineaux, L., Colette, D., Fraser, G., ... 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 session presented at XVIIIeme JOURNEE JEUNES CHERCHEURS, Paris, Faculte de Pharmacie, France, .