OSU-T315 as an Interesting Lead Molecule for Novel B Cell-Specific Therapeutics

Autor: Kristien Van Belle, Jean Herman, Mark Waer, Ben Sprangers, Thierry Louat

Publikováno v: Journal of Immunology Research, Vol 2018 (2018)

B cells are pathogenic in various disease processes and therefore represent an interesting target for the development of novel immunosuppressants. In the search for new therapeutic molecules, we utilized an in vitro B cell activation assay with ODN20

Externí odkaz: https://doaj.org/article/ad3f02dda00c44c9b25a0a7f0fd6418a

Structure-based drug repositioning explains ibrutinib as VEGFR2 inhibitor

Autor: Daniele Parisi, Jörg-Christian Heinrich, V. Joachim Haupt, Melissa F. Adasme, Michael Schroeder, Kristien Van Belle, Thierry Louat, Gary Jennings, Yves Moreau, Jean Herman, Ben Sprangers, Sebastian Salentin

Publikováno v: PLoS ONE
PLoS ONE, Vol 15, Iss 5, p e0233089 (2020)

Many drugs are promiscuous and bind to multiple targets. On the one hand, these targets may be linked to unwanted side effects, but on the other, they may achieve a combined desired effect (polypharmacology) or represent multiple diseases (drug repos

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f65599f42f8b22eca2d778b555662a38
http://europepmc.org/articles/PMC7252619

Synthesis and Evaluation of 6-Aza-2′-deoxyuridine Monophosphate Analogs as Inhibitors of Thymidylate Synthases, and as Substrates or Inhibitors of Thymidine Monophosphate Kinase in Mycobacterium tuberculosis

Autor: Jef Rozenski, Piet Herdewijn, Martin Kögler, Kristien Van Belle, Thierry Louat, Roger Busson, Steven De Jonghe, Hélène Munier-Lehmann

Publikováno v: Chemistry and Biodiversity
Chemistry and Biodiversity, Wiley, 2012, 9 (3), pp.536-56. ⟨10.1002/cbdv.201100285⟩
Chemistry and Biodiversity, 2012, 9 (3), pp.536-56. ⟨10.1002/cbdv.201100285⟩

A series of 5-substituted analogs of 6-aza-2'-deoxyuridine 5'-monophosphate, 6-aza-dUMP, has been synthesized and evaluated as potential inhibitors of the two mycobacterial thymidylate synthases (i.e., a flavin-dependent thymidylate synthase, ThyX, a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f3eea1948b7741eb2ab4333050f32a33
https://doi.org/10.1002/cbdv.201100285

Discovery of 7-N-Piperazinylthiazolo[5,4-d]pyrimidine Analogues as a Novel Class of Immunosuppressive Agents with in Vivo Biological Activity

Autor: Bart Vanderhoydonck, Kristien Van Belle, Jean Herman, Mathy Froeyen, Mi-Yeon Jang, Jef Rozenski, Mark Waer, Piet Herdewijn, Ling-Jie Gao, Yuan Lin, Thierry Louat, Steven De Jonghe

Publikováno v: Journal of Medicinal Chemistry. 54:655-668

Herein we describe the synthesis and in vitro and in vivo activity of thiazolo[5,4-d]pyrimidines as a novel class of immunosuppressive agents, useful for preventing graft rejection after organ transplantation. This research resulted in the discovery

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2f79d147db10b4272a8eff4984b623fb
https://doi.org/10.1021/jm101254z

Synthesis, immunosuppressive activity and structure–activity relationship study of a new series of 4-N-piperazinyl-thieno[2,3-d]pyrimidine analogues

Autor: Mark Waer, Mi-Yeon Jang, Steven De Jonghe, Piet Herdewijn, Thierry Louat, Kristien Van Belle

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 20:844-847

The synthesis of a new series of 4-N-piperazinyl-thieno[2,3-d]pyrimidines is described. The synthetic route allows introducing structural variety at positions 2, 4 and 6 of the scaffold. Evaluation of their immunosuppressive activity in a Mixed Lymph

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e0d4085cbbf020871fdf78b938690608
https://doi.org/10.1016/j.bmcl.2009.12.098