Synthesis, crystal and electronic properties of isomers of chloro-pyridinylvinyl-1H-indoles

Laurence Moineaux, Caroline Charlier, Eduard Dolusic, Pierre Larrieu, Luc Pilotte, Didier Colau, Vincent Stroobant, Moreno Galleni, Bernard Masereel, Benoît Van den Eynde, Johan Wouters, Raphaël Frédérick

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

Résumé

Immunotherapy is a promising novel strategy for cancer therapy. It consists of the therapeutic vaccination of cancer patients to stimulate their (natural) immune system against cancer cells. This approach, however, showed limited efficacy in vivo. Cancer cells are actually able to develop enzymatic mechanisms allowing tumours to resist or escape the immune rejection. Among the enzymes involved, the indoleamine 2,3-dioxygenases IDO and TDO represents potential actors.[1-3] These enzymes catalyse the rapid degradation of tryptophan (Trp) through the kynurenine (KYN) pathway to form quinolinic acid (QA). This results in a local Trp depletion that severely affects the proliferation of T lymphocytes and is thereby profoundly immunosuppressive. This project was funded in part by Télévie (FNRS grant 7.4.543.07) and led in collaboration with the team of Pr Benoit Van Den Eynde (LICR, UCL) and Pr Moreno Galeni (CIP, ULG) aims at developing novel TDO inhibitors using a rational approach. These inhibitors will allow a better understanding of the role of TDO in the phenomenon of immunosuppression, especially in cancerous tumors. From a certain synthesized inhibitors, crystallographic structure was obtained and linking with a docking study of these inhibitors in a model of TDO Ralstonia metallidurans (rmTDO) humanized. Furthermore, in parallel with this study, these compounds have been tested on the enzyme overexpressed and purified previously in order to better understand how to interact with inhibitors TDO. This process is presented on this poster.
langue originaleAnglais
PagesAbstracts, The sixth Belgian Crystallography Symposium (BCS-6), 13 October 2010, Brussels, Belgium
Nombre de pages1
Etat de la publicationPublié - 2010
EvénementThe sixth Belgian Crystallography Symposium (BCS-6) - Brussels, Belgique
Durée: 13 oct. 2010 → …

Colloque

ColloqueThe sixth Belgian Crystallography Symposium (BCS-6)
PaysBelgique
La villeBrussels
période13/10/10 → …

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