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

Research output: Contribution to conferencePoster

108 Downloads (Pure)


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 → …


CityParis, Faculte de Pharmacie, France
Period4/02/11 → …


Dive into the research topics of 'Novel Inhibitors of Indoleamine 2,3-Dioxygenase (IDO), a Target for Anti-Cancer Immunotherapy'. Together they form a unique fingerprint.

Cite this