Abstract
| Original language | English |
|---|---|
| Pages | Abstracts, Journée scientifique de la Société royale de chimie (SRC), Gembloux, Belgium, 14 October 2010 |
| Publication status | Published - 2010 |
| Event | Journée scientifique de la Société royale de chimie (SRC) - Gembloux, Belgium Duration: 14 Oct 2010 → … |
Symposium
| Symposium | Journée scientifique de la Société royale de chimie (SRC) |
|---|---|
| Country | Belgium |
| City | Gembloux |
| Period | 14/10/10 → … |
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Tryptophan 2,3-dioxygenase (TDO) inhibitors : Identification of new scaffolds using virtual screening. / Moineaux, Laurence; Charlier, Caroline; Dolusic, Eduard; Larrieu, Pierre; Pilotte, Luc; Colau, Didier; Stroobant, Vincent; Galleni, Moreno; Masereel, Bernard; Van den Eynde, Benoît; Wouters, Johan; Frédérick, Raphaël.
2010. Abstracts, Journée scientifique de la Société royale de chimie (SRC), Gembloux, Belgium, 14 October 2010 Poster session presented at Journée scientifique de la Société royale de chimie (SRC), Gembloux, Belgium.Research output: Contribution to conference › Poster
TY - CONF
T1 - Tryptophan 2,3-dioxygenase (TDO) inhibitors : Identification of new scaffolds using virtual screening
AU - Moineaux, Laurence
AU - Charlier, Caroline
AU - Dolusic, Eduard
AU - Larrieu, Pierre
AU - Pilotte, Luc
AU - Colau, Didier
AU - Stroobant, Vincent
AU - Galleni, Moreno
AU - Masereel, Bernard
AU - Van den Eynde, Benoît
AU - Wouters, Johan
AU - Frédérick, Raphaël
PY - 2010
Y1 - 2010
N2 - 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. A series of vinyl-1H-indoles has been synthesized and their inhibitory potential has been evaluated on TDO of Ralstonia metallidurans (rmTDO) overexpressed in E.coli and purified by affinity chromatography. Crystallographic structure of some analogues was obtained and used as starting point for a docking study of these inhibitors in a model of humanized rmTDO. These data allowbetter understanding of how this family of inhibitors interact with TDO. This process is presented on this poster.
AB - 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. A series of vinyl-1H-indoles has been synthesized and their inhibitory potential has been evaluated on TDO of Ralstonia metallidurans (rmTDO) overexpressed in E.coli and purified by affinity chromatography. Crystallographic structure of some analogues was obtained and used as starting point for a docking study of these inhibitors in a model of humanized rmTDO. These data allowbetter understanding of how this family of inhibitors interact with TDO. This process is presented on this poster.
M3 - Poster
SP - Abstracts, Journée scientifique de la Société royale de chimie (SRC), Gembloux, Belgium, 14 October 2010
ER -