3-ALKENYL INDOLES AS TRYPTOPHAN 2,3-DIOXYGENASE INHIBITORS FOR THE ENHANCEMENT OF CANCER IMMUNOTHERAPY

Eduard Dolušić, Luc Pilotte, Laurence Moineaux, Pierre Larrieu, Vincent Stroobant, Didier Colau, Lionel Pochet, Etienne De Plaen, Catherine Uyttenhove, Benoît Van den Eynde, Johan Wouters, Bernard Masereel, Steve Lanners, Raphaël Frédérick

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3 Article
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2012
Reversal of tumoral immune resistance by inhibition of tryptophan 2,3-dioxygenase
Pilotte, L., Larrieu, P., Stroobant, V., Colau, D., Dolušić, E., Frédérick, R., De Plaen, E., Uyttenhove, C., Wouters, J., Masereel, B. & Van Den Eynde, B. J., 14 Feb 2012, In: Proceedings of the National Academy of Sciences of the United States of America. 109, 7, p. 2497-2502 6 p.
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Reversal of Tumoral Immune Resistance by Inhibition of Tryptophan 2,3-Dioxygenase (TDO): Design, Synthesis and Preclinical Evaluation of a Novel TDO Inhibitor.
Dolušić, E., Larrieu, P., Moineaux, L., Stroobant, V., Pilotte, L., Colaux, D., Van den Eynde, B., Masereel, B., Wouters, J. & Frédérick, R., 2012, In: ChemMedChem. p. 371 1 p.
Research output: Contribution to journal › Literature review › peer-review
Synthesis, crystal structures and electronic properties of isomers of chloro-pyridinylvinyl-1H-indoles
Moineaux, L., Laurent, S., Reniers, J., Dolusic, E., Galleni, M., Frère, J.-M., Masereel, B., Frédérick, R. & Wouters, J., 1 Aug 2012, In: European Journal of Medicinal Chemistry. 54, p. 95-102 8 p.
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Tryptophan 2,3-Dioxygenase (TDO) Inhibitors as Anticancer Immunomodulators
Dolusic, E., Larrieu, P., Moineaux, L., Strobant, V., Pilotte, L., Colau, D., Pochet, L., De Plaen, E., Uyttenhove, C., Van den Eynde, B., Wouters, J., Masereel, B. & Frédérick, R., 15 Jul 2012, p. Programme & Book of Abstracts, BOSS XIII, KU Leuven, Belgium, 15 - 20 July 2012, P292, p. 339. 1 p.
Research output: Contribution to conference › Poster

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2011
coauthor on lecture: Reversal of tumoral immune resistance by inhibition of tryptophan 2,3-dioxygenase (TDO): discovery of an orally active TDO inhibitor.
Dolusic, E., Larrieu, P., Moineaux, L., Stroobant, V., Pilotte, L., Colau, D., Van den Eynde, B., Masereel, B., Wouters, J. & Frédérick, R., 2011, Book of Abstracts, Emerging Targets and Treatments: Opportunities and Challenges for Drug Design, Ghent, 25 November 2011: Annual One-Day Meeting on Medicinal Chemistry of SRC & KVCV (MedChem 2011). Vol. OC01. p. OC01
Research output: Contribution in Book/Catalog/Report/Conference proceeding › Conference contribution
SYNTHESIS, ACTIVITY, CRYSTAL AND ELECTRONIC PROPERTIES OF ISOMERS OF CHLORO-PYRIDINYLVINYL-1H-INDOLES
Moineaux, L., Laurent, S., Dolusic, E., Reniers, J., Norberg, B., Frère, J.-M., Galleni, M., Van den Eynde, B., Masereel, B., Frédérick, R. & Wouters, J., 2011, p. Book of Abstracts, 25èmes Journées Franco-belges de Pharmacochimie, 19-20/05/11, Liège, P20, p. 45. 1 p.
Research output: Contribution to conference › Poster
Synthesis, structural, enzymatic and cellular studies of vinyl-1H-indole analogues as potential inhibitors of tryptophan 2,3-dioxygenase (TDO), an attractive target in cancer immunotherapy.
Moineaux, L., Charlier, C., Dolusic, E., Larrieu, P., Pilotte, L., Colau, D., Stroobant, V., Charlier, P., Laurent, S., Galleni, M., Masereel, B., Van den Eynde, B., Wouters, J. & Frédérick, R., 2011, p. Book of Abstracts, Annual One-Day Meeting on Medicinal Chemistry of SRC & KVCV (MedChem 2011), Ghent, 25 November 2011, p. 22. 1 p.
Research output: Contribution to conference › Poster
Tryptophan 2,3-dioxygenase (TDO) inhibitors : Identification of new scaffolds using virtual screening
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., 2011, p. Book of Abstracts, 25èmes Journées Franco-belges de Pharmacochimie, 19-20/05/11, Liège, p. 19. 1 p.
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Tryptophan 2,3-dioxygenase (TDO) inhibitors. 3-(2-(pyridyl)ethenyl)indoles as potential anticancer immunomodulators
Dolušić, E., Larrieu, P., Moineaux, L., Stroobant, V., Pilotte, L., Colau, D., Pochet, L., Van Den Eynde, B., Masereel, B., Wouters, J. & Frédérick, R., 11 Aug 2011, In: Journal of Medicinal Chemistry. 54, 15, p. 5320-5334 15 p.
Research output: Contribution to journal › Article › peer-review
2010

Conception, synthèse et étude d'inhibiteurs de la tryptophane 2,3-dioxygénase (TDO), une cible prometteuse pour le traitement du cancer
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, p. Abstracts, Séminaire des jeunes chercheurs Télévie 2011, Brussels, Belgium, 7 December 2010. 1 p.
Research output: Contribution to conference › Poster

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Design, synthesis and study of inhibitors of tryptophan 2,3-dioxygenase (TDO), a promising target for cancer therapy
Moineaux, L., Charlier, C., Dolusic, E., Larrieu, P., Pilotte, L., Colau, D., Stroobant, V., Galleni, M., Masereel, B., Van den Eynde, B., Wouters, J. (Supervisor) & Frédérick, R., 2010, p. Abstracts, école doctorale SFMBBM, Liège, Belgium, 10 December 2010. 1 p.
Research output: Contribution to conference › Poster
Structural and enzymatic study of tryptophan 2,3-dioxgenase (TDO), a potential target in anticancer immunotherapy.
Moineaux, L., Charlier, C., Dolušić, E., Larrieu, P., Pilotte, L., Colaux, D., Stroobant, V., Galleni, M., Masereel, B., Van den Eynde, B., Wouters, J. & Frédérick, R., 2010, In: Drugs of the future. 35, suppl A, p. 189
Research output: Contribution to journal › Literature review › peer-review
Structural and enzymatic study of tryptophan 2.3-dioxygenase (TDO), a potential target in anticancer immunotherapy
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, p. PC.355, 21st ISMC, Brussels, Belgium, September 5-9, 2010, Drugs of the Future, volume 35, issue suppl. A, pp. 217-218. 2 p.
Research output: Contribution to conference › Paper
Synthesis, crystal and electronic properties of isomers of chloro-pyridinylvinyl-1H-indoles
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, p. Abstracts, The sixth Belgian Crystallography Symposium (BCS-6), 13 October 2010, Brussels, Belgium. 1 p.
Research output: Contribution to conference › Poster
Tryptophan 2,3-dioxygenase (TDO) inhibitors : Identification of new scaffolds using virtual screening
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, p. Abstracts, Journée scientifique de la Société royale de chimie (SRC), Gembloux, Belgium, 14 October 2010.
Research output: Contribution to conference › Poster

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3-ALKENYL INDOLES AS TRYPTOPHAN 2,3-DIOXYGENASE INHIBITORS FOR THE ENHANCEMENT OF CANCER IMMUNOTHERAPY

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