Zobrazeno 1 - 10
of 19
pro vyhledávání: '"Bart Vanderhoydonck"'
Autor:
Lei Chen, Paula Milani de Marval, Kendall Powell, Mark Johnson, Greg Falls, Brian Lawhorn, Aurélie Candi, Amuri Kilonda, Bart Vanderhoydonck, Arnaud Marchand, Matthias Versele, Georg Halder, Stephen L. Gwaltney, Adeela Kamal
Publikováno v:
Cancer Research. 83:4964-4964
Many cancers harbor mutations in the Hippo pathway that lead to constitutive activation of the transcriptional co-activators YAP/TAZ that then bind the transcription factor TEAD and drive aberrant transcription of target genes involved in cell prolif
Autor:
Adeela Kamal, Aurélie Candi, Matthias Versele, Bart Vanderhoydonck, Arnaud Marchand, Ron de Jong, Thuy Hoang, Georg Halder, Patrick Chaltin, Stephen L. Gwaltney, Mike Burgess
Publikováno v:
Cancer Research. 82:3945-3945
Background: The Hippo pathway is an evolutionarily conserved signaling cascade whose deregulation can promote excessive cell proliferation and tumor development. Pathway output is mediated by the YAP and TAZ transcriptional co-activators, which bind
Autor:
Leticia Sansores, Matthias Versele, Bart Vanderhoydonck, Wim Smets, Aurélie Candi, Arnaud Marchand, Wanda Haeck, Marnik Nijs, Patrick Chaltin, Georg Halder, Stéphane Spieser, Hugo Klaassen
Publikováno v:
Cancer Research. 80:5229-5229
The Hippo pathway is a highly conserved signaling pathway across higher-order vertebrates and a key modulator of developmental biology. Both genetic aberrations as well as non-genetic dysregulation of the pathway lead to constitutive nuclear localiza
Autor:
Adnan Khan, Farnaz Fallah-Arani, Bart Vanderhoydonck, Judi Charlotte Neuss, Sarah Malcolm, Alfred Lammens, Richard J. Franklin, Lindsay K. Shuttleworth, Qiuya Huang, Jamie Henshall, Daniel James Ford, Mi-Yeon Jang, Shengqiao Li, Helen Tracey Horsley, Daniel Christopher Brookings, Mark Waer, Rodger A. Allen, Payne Andrew Charles, Yuan Lin, Eleanor Ward, Tom Ceska, Piet Herdewijn, Mark Jairaj, James Thomas Reuberson, Stefan Steinbacher, Mark Daniel Calmiano, Carl Brendan Doyle, Ling-Jie Gao, William R. Pitt, Jean Herman, Martin Augustin, Thierry Louat, Anant Ramrao Ghawalkar
Publikováno v:
Journal of medicinal chemistry. 61(15)
The primary target of a novel series of immunosuppressive 7-piperazin-1-ylthiazolo[5,4- d]pyrimidin-5-amines was identified as the lipid kinase, PI4KIIIβ. Evaluation of the series highlighted their poor solubility and unwanted off-target activities.
Autor:
Kristien Van Belle, Eveline Lescrinier, Jean Herman, Bart Vanderhoydonck, Jef Rozenski, Piet Herdewijn, Carol Hopkins Sibley, Thierry Louat, Steven De Jonghe, Martin Kögler, Anastasia Parchina
Publikováno v:
Journal of Medicinal Chemistry. 54:4847-4862
A series of 5-substituted 2'-deoxyuridine monophosphate analogues has been synthesized and evaluated as potential inhibitors of mycobacterial ThyX, a novel flavin-dependent thymidylate synthase in Mycobacterium tuberculosis. A systematic SAR study le
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
Publikováno v:
Tetrahedron. 63:7679-7689
Syntheses of 5-phosphono-2-oxazolidinones and 5-phosphono-2-imidazolidinones were achieved from the corresponding 1-vinyl-2-phosphonoaziridines. Regioselective aziridine ring opening employing methyl chloroformate affords 1-amido-2-chloroethylphospho
Publikováno v:
The Journal of Organic Chemistry. 70:191-198
Several 1-phosphono-2-aza-1,3-butadienes, 1 and 13-20, were evaluated in the reaction with different enolate-type nucleophiles to induce addition at the 1- or the 4-position of the azadiene. 1-Phosphono-2-azadienes 1 react with sodium malonate at the
Publikováno v:
Tetrahedron. 57:4793-4800
α-Chloro acylphosphonates and α,α′-dichloro bisacylphosphonates were prepared in situ by chlorination of acylphosphonates and bisacylphosphonates, respectively, using sulfuryl chloride. Subsequently, they were cleaved to the corresponding α-chl
Autor:
Kenneth Segers, Jozef Anné, Bart Vanderhoydonck, Piet Herdewijn, Steven De Jonghe, Alessandro Stella, Jef Rozenski
Publikováno v:
Chemistrybiodiversity. 8(2)
The 2-(1,2-dihydro-3-oxo-3H-pyrazol-2-yl)benzothiazole scaffold was selected as a central core structure for the discovery of novel antibacterial compounds. A systematic variation of the substituents on the oxo-pyrazole moiety, as well as on the benz