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

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

Namur Research Institute for Life Sciences

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 originale	Anglais
Pages	PC.281, 21st ISMC, Brussels, Belgium, September 5-9, 2010, Drugs of the Future, volume 35, issue suppl. A, pp. 181-182
Nombre de pages	2
Etat de la publication	Publié - 2010
Evénement	EFMC-ISMC 2010 XXIst INTERNATIONAL SYMPOSIUM ON MEDICINAL CHEMISTRY - Bruxelles, Belgique Durée: 5 sept. 2010 → …

Une conférence

Une conférence	EFMC-ISMC 2010 XXIst INTERNATIONAL SYMPOSIUM ON MEDICINAL CHEMISTRY
Pays/Territoire	Belgique
La ville	Bruxelles
période	5/09/10 → …

SDG des Nations Unies

Ce résultat contribue à ou aux Objectifs de développement durable suivants

4 Poster
3 Article
3 Revue de documentation
1 Article dans les actes d'une conférence/un colloque

Indoleamine 2,3-dioxygenase inhibitors: a patent review (2008-2012)
Dolušić, E. & Frédérick, R., 1 oct. 2013, Dans: Expert opinion on therapeutic targets. 23, 10, p. 1367-1381 15 p.
Résultats de recherche: Contribution à un journal/une revue › Revue de documentation › Revue par des pairs
Indoleamine 2,3-Dioxygenase Inhibitory Activity of Derivatives of Marine Alkaloid Tsitsikammamine A
Dolušić, E., Larrieu, P., Meinguet, C., Colette, D., Rives, A., Blanc, S., Ferain, T., Pilotte, L., Stroobant, V., Wouters, J., Van Den Eynde, B., Masereel, B., Delfourne, E. & Frédérick, R., 1 janv. 2013, Dans: Bioorganic and medicinal chemistry letters. 23, 1, p. 47-54 8 p.
Résultats de recherche: Contribution à un journal/une revue › Article › Revue par des pairs
3 Téléchargements (Pure)
Discovery and preliminary SARs of keto-indoles as novel indoleamine 2,3-dioxygenase (IDO) inhibitors
Dolušić, E., Larrieu, P., Blanc, S., Sapunaric, F., Pouyez, J., Moineaux, L., Colette, D., Stroobant, V., Pilotte, L., Colau, D., Ferain, T., Fraser, G., Galleni, M., Frère, J-M., Masereel, B., Van Den Eynde, B., Wouters, J. & Frédérick, R., 2011, Dans: European Journal of Medicinal Chemistry. 46, 7, p. 3058-3065 8 p.
Résultats de recherche: Contribution à un journal/une revue › Article › Revue par des pairs

1 Terminé

CANTOL: Conception et synthèse d'inhibiteurs de l'indolaminedioxygénase (IDO) pour le traitement du cancer
MASEREEL, B., Wouters, J., Dolušić, E., FREDERICK, R., POUYEZ, J., Van den Eynde, B. J., Frère, J., Moser, M., Jean-Marie, B., Combalbert, J. & Stephenne, J.
1/04/08 → 31/03/12
Projet: Recherche

Physico-chimie et caractérisation (PC2)
Johan Wouters (!!Manager) & Carmela Aprile (!!Manager)
Plateforme technologique Caracterisation physico-chimiques
Equipement/installations: Plateforme technolgique

3 Participation à une conférence, un congrès

47th RICT: Drug Discovery and Selection.
Eduard Dolusic (Poster)
6 juil. 2011 → 8 juil. 2011
Activité: Participation ou organisation d'un événement › Participation à une conférence, un congrès
XVIIIeme JOURNEE JEUNES CHERCHEURS
Eduard Dolusic (Poster)
4 févr. 2011
Activité: Participation ou organisation d'un événement › Participation à une conférence, un congrès
EFMC-ISMC 2010 XXIst INTERNATIONAL SYMPOSIUM ON MEDICINAL CHEMISTRY
Eduard Dolusic (Poster)
5 sept. 2010 → 9 sept. 2010
Activité: Participation ou organisation d'un événement › Participation à une conférence, un congrès

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.

@conference{08dbfdaba4fb4dada4204ba695b2859f,

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

abstract = "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 cells1The 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.2,3This 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",

author = "Rapha{\"e}l Fr{\'e}d{\'e}rick and S{\'e}bastien Blanc and Pierre Larrieu and Laurence Moineaux and Delphine Colette and Graeme Fraser and Vincent Stroobant and Luc Pilotte and Didier Colau and Johan Wouters and Bernard Masereel and {Van den Eynde}, Beno{\^i}t and Eduard Dolusic",

year = "2010",

language = "English",

pages = "PC.281, 21st ISMC, Brussels, Belgium, September 5--9, 2010, Drugs of the Future, volume 35, issue suppl. A, pp. 181--182",

note = "EFMC-ISMC 2010 XXIst INTERNATIONAL SYMPOSIUM ON MEDICINAL CHEMISTRY ; Conference date: 05-09-2010",

}

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', EFMC-ISMC 2010 XXIst INTERNATIONAL SYMPOSIUM ON MEDICINAL CHEMISTRY, Bruxelles, Belgique, 5/09/10 p. PC.281, 21st ISMC, Brussels, Belgium, September 5-9, 2010, Drugs of the Future, volume 35, issue suppl. A, pp. 181-182.

Discovery and Optimization Of Indole-pyridinyl-ethanones as Novel Inhibitors of Indoleamine-2,3-Dioxygenase (IDO), a Promising Target for Anti-Cancer Immunotherapy. / Frédérick, Raphaël; Blanc, Sébastien; Larrieu, Pierre et al.
2010. 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.

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

TY - CONF

T1 - Discovery and Optimization Of Indole-pyridinyl-ethanones as Novel Inhibitors of Indoleamine-2,3-Dioxygenase (IDO), a Promising Target for Anti-Cancer Immunotherapy

AU - Frédérick, Raphaël

AU - Blanc, Sébastien

AU - Larrieu, Pierre

AU - Moineaux, Laurence

AU - Colette, Delphine

AU - Fraser, Graeme

AU - Stroobant, Vincent

AU - Pilotte, Luc

AU - Colau, Didier

AU - Wouters, Johan

AU - Masereel, Bernard

AU - Van den Eynde, Benoît

AU - Dolusic, Eduard

PY - 2010

Y1 - 2010

N2 - 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 cells1The 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.2,3This 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

AB - 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 cells1The 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.2,3This 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

M3 - Poster

SP - PC.281, 21st ISMC, Brussels, Belgium, September 5-9, 2010, Drugs of the Future, volume 35, issue suppl. A, pp. 181-182

T2 - EFMC-ISMC 2010 XXIst INTERNATIONAL SYMPOSIUM ON MEDICINAL CHEMISTRY

Y2 - 5 September 2010

ER -

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

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