Discovery and Optimization Of Indole-pyridinyl-ethanones as Novel Inhibitors of Indoleamine-2,3-Dioxygenase (IDO), a Promising Target for Anti-Cancer Immunotherapy

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

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

Résumé

Cancers and tumors regularly evade the immune surveillance system of the host employing several mechanisms. It was found previously that one mechanism resulting in tumoral immune resistance stems from the constitutive expression of indoleamine 2,3-dioxygenase (IDO) by tumor cells1
The present work is based on the recent discovery that a second enzyme in tryptophan catabolism, tryptophan 2,3-dioxygenase (TDO), is also unexpectedly expressed in many tumor cells.2,3
This work4 describes the design, synthesis, X-ray structure determination, enzyme inhibition, cellular assays, docking and solubility tests of indole-based TDO inhibitors of the general structure 1. This strategy is based on similar compounds reported as dual TDO/5-HT reuptake inhibitors.5
langue originaleAnglais
PagesPC.281, 21st ISMC, Brussels, Belgium, September 5-9, 2010, Drugs of the Future, volume 35, issue suppl. A, pp. 181-182
Nombre de pages2
Etat de la publicationPublié - 2010
EvénementEFMC-ISMC 2010 XXIst INTERNATIONAL SYMPOSIUM ON MEDICINAL CHEMISTRY - Bruxelles, Belgique
Durée: 5 sept. 2010 → …

Une conférence

Une conférenceEFMC-ISMC 2010 XXIst INTERNATIONAL SYMPOSIUM ON MEDICINAL CHEMISTRY
PaysBelgique
La villeBruxelles
période5/09/10 → …

    Empreinte digitale

Contient cette citation

Frédérick, R., Blanc, S., Larrieu, P., Moineaux, L., Colette, D., Fraser, G., Stroobant, V., Pilotte, L., Colau, D., Wouters, J., Masereel, B., Van den Eynde, B., & Dolusic, E. (2010). Discovery and Optimization Of Indole-pyridinyl-ethanones as Novel Inhibitors of Indoleamine-2,3-Dioxygenase (IDO), a Promising Target for Anti-Cancer Immunotherapy. PC.281, 21st ISMC, Brussels, Belgium, September 5-9, 2010, Drugs of the Future, volume 35, issue suppl. A, pp. 181-182. Poster présenté � EFMC-ISMC 2010 XXIst INTERNATIONAL SYMPOSIUM ON MEDICINAL CHEMISTRY, Bruxelles, Belgique.