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
étatPublié - 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 → …

Empreinte digitale

Indoles
Neoplasms
Tryptophan
Ralstonia
Enzymes
Indoleamine-Pyrrole 2,3,-Dioxygenase
Quinolinic Acid
Kynurenine
Posters
Organized Financing
Immunosuppressive Agents
Immunotherapy
Immunosuppression
Immune System
Vaccination
T-Lymphocytes
Therapeutics

Citer ceci

Moineaux, L., Charlier, C., Dolusic, E., Larrieu, P., Pilotte, L., Colau, D., ... Frédérick, R. (2010). Synthesis, crystal and electronic properties of isomers of chloro-pyridinylvinyl-1H-indoles. Abstracts, The sixth Belgian Crystallography Symposium (BCS-6), 13 October 2010, Brussels, Belgium. Poster présenté � The sixth Belgian Crystallography Symposium (BCS-6), Brussels, Belgique.
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. / Synthesis, crystal and electronic properties of isomers of chloro-pyridinylvinyl-1H-indoles. Poster présenté � The sixth Belgian Crystallography Symposium (BCS-6), Brussels, Belgique.1 p.
@conference{7e0f8c1164df4816819c48b1b8f466da,
title = "Synthesis, crystal and electronic properties of isomers of chloro-pyridinylvinyl-1H-indoles",
abstract = "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 T{\'e}l{\'e}vie (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.",
author = "Laurence Moineaux and Caroline Charlier and Eduard Dolusic and Pierre Larrieu and Luc Pilotte and Didier Colau and Vincent Stroobant and Moreno Galleni and Bernard Masereel and {Van den Eynde}, Beno{\^i}t and Johan Wouters and Rapha{\"e}l Fr{\'e}d{\'e}rick",
year = "2010",
language = "English",
pages = "Abstracts, The sixth Belgian Crystallography Symposium (BCS--6), 13 October 2010, Brussels, Belgium",
note = "The sixth Belgian Crystallography Symposium (BCS-6) ; Conference date: 13-10-2010",

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Moineaux, L, Charlier, C, Dolusic, E, Larrieu, P, Pilotte, L, Colau, D, Stroobant, V, Galleni, M, Masereel, B, Van den Eynde, B, Wouters, J & Frédérick, R 2010, 'Synthesis, crystal and electronic properties of isomers of chloro-pyridinylvinyl-1H-indoles' The sixth Belgian Crystallography Symposium (BCS-6), Brussels, Belgique, 13/10/10, p. Abstracts, The sixth Belgian Crystallography Symposium (BCS-6), 13 October 2010, Brussels, Belgium.

Synthesis, crystal and electronic properties of isomers of chloro-pyridinylvinyl-1H-indoles. / 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, The sixth Belgian Crystallography Symposium (BCS-6), 13 October 2010, Brussels, Belgium Poster présenté � The sixth Belgian Crystallography Symposium (BCS-6), Brussels, Belgique.

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

TY - CONF

T1 - Synthesis, crystal and electronic properties of isomers of chloro-pyridinylvinyl-1H-indoles

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. 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.

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. 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.

M3 - Poster

SP - Abstracts, The sixth Belgian Crystallography Symposium (BCS-6), 13 October 2010, Brussels, Belgium

ER -

Moineaux L, Charlier C, Dolusic E, Larrieu P, Pilotte L, Colau D et al.. Synthesis, crystal and electronic properties of isomers of chloro-pyridinylvinyl-1H-indoles. 2010. Poster présenté � The sixth Belgian Crystallography Symposium (BCS-6), Brussels, Belgique.