Supplemental Figure 1 from Discovery and Pharmacological Characterization of JNJ-42756493 (Erdafitinib), a Functionally Selective Small-Molecule FGFR Family Inhibitor

Autor: Matthew V. Lorenzi, Sylvie Laquerre, Patrick Angibaud, Christopher Moy, Jayaprakash D. Karkera, Suso J. Platero, Jennifer Yang, Liang Xie, Na Cheng, David R. Newell, Neil T. Thompson, George Ward, Ron Gilissen, Christopher W. Murray, Martin Page, Gordon Saxty, Matthew Squires, David C. Rees, Eddy Freyne, Peter King, Kelly Van De Ven, Caroline Paulussen, Tinne Verhulst, Desiree De Lange, Jorge Vialard, Laurence Mevellec, Eleonora Jovcheva, Timothy P.S. Perera

A) Structure of JNJ-42541707, a structurally related compound to JNJ-42756493. B) 72h growth inhibition (IC50) of JNJ-42541707 against 236 cancer cell lines from multiple origins color coded based on FGFR1,2,4 mRNA overexpression and FGFR WT.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::014876daf0ea3141cec8e46d4cd3afe8
https://doi.org/10.1158/1535-7163.22503741

Supplemental Table 1 from Discovery and Pharmacological Characterization of JNJ-42756493 (Erdafitinib), a Functionally Selective Small-Molecule FGFR Family Inhibitor

Autor: Matthew V. Lorenzi, Sylvie Laquerre, Patrick Angibaud, Christopher Moy, Jayaprakash D. Karkera, Suso J. Platero, Jennifer Yang, Liang Xie, Na Cheng, David R. Newell, Neil T. Thompson, George Ward, Ron Gilissen, Christopher W. Murray, Martin Page, Gordon Saxty, Matthew Squires, David C. Rees, Eddy Freyne, Peter King, Kelly Van De Ven, Caroline Paulussen, Tinne Verhulst, Desiree De Lange, Jorge Vialard, Laurence Mevellec, Eleonora Jovcheva, Timothy P.S. Perera

In vitro kinase inhibition by DiscoverX KinomeScan assay. For details see (19)

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::707b5abacc5ec387fe47990836d03d73
https://doi.org/10.1158/1535-7163.22503738

Supplemental Table 3 from Discovery and Pharmacological Characterization of JNJ-42756493 (Erdafitinib), a Functionally Selective Small-Molecule FGFR Family Inhibitor

Autor: Matthew V. Lorenzi, Sylvie Laquerre, Patrick Angibaud, Christopher Moy, Jayaprakash D. Karkera, Suso J. Platero, Jennifer Yang, Liang Xie, Na Cheng, David R. Newell, Neil T. Thompson, George Ward, Ron Gilissen, Christopher W. Murray, Martin Page, Gordon Saxty, Matthew Squires, David C. Rees, Eddy Freyne, Peter King, Kelly Van De Ven, Caroline Paulussen, Tinne Verhulst, Desiree De Lange, Jorge Vialard, Laurence Mevellec, Eleonora Jovcheva, Timothy P.S. Perera

JNJ-42756493 anti-proliferative activity against cancer cells lines from multiple origins.. Detailed data supporting Figure 2.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::59bca756040d98715cf3d679230a312d
https://doi.org/10.1158/1535-7163.22503732.v1

Data from JNJ-26481585, a Novel Second-Generation Oral Histone Deacetylase Inhibitor, Shows Broad-Spectrum Preclinical Antitumoral Activity

Autor: Patrick Angibaud, Kristof van Emelen, Martin Page, Michel Janicot, Marc Du Jardin, Luc Andries, Ilse Goris, Willem Talloen, Kees Bol, Eugene Cox, Veronique Vreys, Ian Hickson, Ron Gilissen, Laurence Decrane, Bruno Roux, Isabelle Pilatte, Lut Janssen, Ann Belin, Wim Floren, Ann Marin, Peter King, Janine Arts

Purpose: Histone deacetylase (HDAC) inhibitors have shown promising clinical activity in the treatment of hematologic malignancies, but their activity in solid tumor indications has been limited. Most HDAC inhibitors in clinical development only tran

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2434ea75f5b9b9c5f4fbdf2a8833ab91
https://doi.org/10.1158/1078-0432.c.6517927

Pd(0)-Catalyzed Direct Inter- and Intramolecular C–H Functionalization of 4-Carboxyimidazoles

Autor: Virginie Sophie Poncelet, Christophe Hoarau, Antoine Peresson, Thibaut Perse, Steven Frippiat, Christine Baudequin, Olivier Querolle, Cédric Schneider, Vincent Levacher, Patrick Angibaud, Lieven Meerpoel, Yvan Ramondenc, Laurent Bischoff

Publikováno v: SYNLETT
SYNLETT, Georg Thieme Verlag, 2020, 31 (10), pp.1015-2021. ⟨10.1055/s-0040-1708003⟩
SYNLETT, Georg Thieme Verlag, 2020, 31 (10), pp.1015-1021. ⟨10.1055/s-0040-1708003⟩

International audience; The palladium-catalyzed arylation and alkenylation of N-substituted methyl imidazole-4-carboxylates are described through inter- and intramolecular pathways. Both direct C2–H and C5–H arylation and alkenylation proceed und

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c9434a083cc8e00032950a76fb30e594
https://hal-normandie-univ.archives-ouvertes.fr/hal-02548986