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Journal Articles

Abstract LB319: IAG933, a selective and orally efficacious YAP1/WWTR1(TAZ)-panTEAD protein-protein interaction inhibitor with pre-clinical activity in monotherapy and combinations

Tobias Schmelzle, Emilie Chapeau, Daniel Bauer, Patrick Chene, Jason Faris, Cesar Fernandez, Pascal Furet, Giorgio Galli, Jiachang Gong, Stephanie Harlfinger, Francesco Hofmann, Eloisa Jimenez Nunez, Joerg Kallen, Thanos Mourikis, Laurent Sansregret, Paulo Santos, Clemens Scheufler, Holger Sellner, Markus Voegtle, Markus Wartmann, Peter Wessels, Frederic Zecri, Nicolas Soldermann
Journal: Cancer Research
Cancer Res (2023) 83 (8_Supplement): LB319.
https://doi.org/10.1158/1538-7445.AM2023-LB319
Published: 14 April 2023
View article titled, Abstract LB319: IAG933, a selective and orally efficacious YAP1/WWTR1(TAZ)-panTEAD protein-protein interaction inhibitor with pre-clinical activity in monotherapy and combinations
Journal Articles

Abstract 4026: JDQ443, a covalent inhibitor of KRASG12C with a novel binding mode, shows broad antitumor activity in KRASG12C preclinical models as a single agent and in combination with inhibitors of SHP2, MEK or CDK4/6

Andreas Weiss, Hans Voshol, Diana Graus Porta, Carmine Fedele, Dario Sterker, Ruben De Kanter, Rowan Stringer, Toni Widmer, Alice Loo, Daniel A. Guthy, Kim S. Beyer, Nils Ostermann, Catherine LeBlanc, Marc Gerspacher, Andrea Vaupel, Richard Sedrani, Frederic Zecri, Saveur-Michel Maria, Francesco Hofmann, Peter Hammerman, Jeff Engelman, Edwige Lorthiois, Simona Cotesta, Saskia M. Brachmann
Journal: Cancer Research
Cancer Res (2022) 82 (12_Supplement): 4026.
https://doi.org/10.1158/1538-7445.AM2022-4026
Published: 15 June 2022
View article titled, Abstract 4026: JDQ443, a covalent inhibitor of KRAS<sup>G12C</sup> with a novel binding mode, shows broad antitumor activity in KRAS<sup>G12C</sup> preclinical models as a single agent and in combination with inhibitors of SHP2, MEK or CDK4/6
Journal Articles

Abstract 1276: Identification of S65487/VOB560 as a potent and selective intravenous 2nd-generation BCL-2 inhibitor active in wild-type and clinical mutants resistant to Venetoclax

Arnaud Le Tiran, Audrey Claperon, James Davidson, Jérôme-Benoit Starck, Thierry Le Diguarher, Maïa Chanrion, Prakash Mistry, Youzhen Wang, Elodie Monceau, Fabienne Bernhardt, Francesca Rocchetti, Gaelle Lysiak-Auvity, Ijen Chen, Zoe Daniels, Chris Pedder, Mandy Fallowfield, Jean-Michel Henlin, Imre Fejes, Janos Tatai, Miklos Nyerges, Didier Durand, Marion Zarka, Sneha Sanghavi, Anne-Marie Girard, Marie Schoumacher, Laurence Kraus-Berthier, Rick Newcombe, Ensar Halilovic, Sébastien Banquet, Alain Rupin, Heiko Maacke, James Murray, Erick Morris, Francesco Hofmann, Frédéric Colland, Olivier Geneste
Journal: Cancer Research
Cancer Res (2021) 81 (13_Supplement): 1276.
https://doi.org/10.1158/1538-7445.AM2021-1276
Published: 01 July 2021
View article titled, Abstract 1276: Identification of S65487/VOB560 as a potent and selective intravenous 2<sup>nd-</sup>generation BCL-2 inhibitor active in wild-type and clinical mutants resistant to Venetoclax
Journal Articles

Abstract 1770: A new DOT1L inhibitor with in vivo activity in mouse models of MLL-translocated leukemia

Andreas Weiss, Frederic Stauffer, Clemens Clemens, Henrik Möbitz, Christian Ragot, Kim S. Beyer, Keith Calkins, Claudio Thoma, Daniel Guthy, Michael Kiffe, Bernard Van Eerdenbrugh, William R. Sellers, Francesco Hofmann, Ralph Tiedt, Christoph Gaul
Journal: Cancer Research
Cancer Res (2020) 80 (16_Supplement): 1770.
https://doi.org/10.1158/1538-7445.AM2020-1770
Published: 15 August 2020
View article titled, Abstract 1770: A new DOT1L inhibitor with <em>in vivo</em> activity in mouse models of MLL-translocated leukemia
Journal Articles

Dose and Schedule Determine Distinct Molecular Mechanisms Underlying the Efficacy of the p53–MDM2 Inhibitor HDM201

Sébastien Jeay, Stéphane Ferretti, Philipp Holzer, Jeanette Fuchs, Emilie A. Chapeau, Markus Wartmann, Dario Sterker, Vincent Romanet, Masato Murakami, Grainne Kerr, Eric Y. Durand, Swann Gaulis, Marta Cortes-Cros, Stephan Ruetz, Therese-Marie Stachyra, Joerg Kallen, Pascal Furet, Jens Würthner, Nelson Guerreiro, Ensar Halilovic, Astrid Jullion, Audrey Kauffmann, Emil Kuriakose, Marion Wiesmann, Michael R. Jensen, Francesco Hofmann, William R. Sellers
Journal: Cancer Research
Series: Author Choice
Cancer Res (2018) 78 (21): 6257–6267.
https://doi.org/10.1158/0008-5472.CAN-18-0338
Published: 01 November 2018
View article titled, Dose and Schedule Determine Distinct Molecular Mechanisms Underlying the Efficacy of the p53–MDM2 Inhibitor HDM201
Open the PDF for Dose and Schedule Determine Distinct Molecular Mechanisms Underlying the Efficacy of the p53–MDM2 Inhibitor HDM201 in another window
Includes: Supplementary data
Journal Articles

Abstract 1879: Pyrazolopyrimidines as novel selective allosteric MALT1 inhibitors with in vivo activity in ABC-DLBCL

Andreas Weiss, Thomas Radimerski, Daniel Wyss, Rita Andraos, Alexandra Buhles, Dario Sterker, Jean Quancard, Carole Pissot, Oliver Simic, Marc Bigaud, Frederic Bornancin, Achim Schlapbach, Catherine Regnier, Paul McSheehy, Elisabeth Buchdunger, Markus Wartmann, Martin Renatus, Ralf Endres, William Sellers, Francesco Hofmann
Journal: Cancer Research
Cancer Res (2018) 78 (13_Supplement): 1879.
https://doi.org/10.1158/1538-7445.AM2018-1879
Published: 01 July 2018
View article titled, Abstract 1879: Pyrazolopyrimidines as novel selective allosteric MALT1 inhibitors with in vivo activity in ABC-DLBCL
Journal Articles

Abstract 3934: Determination of the PI3Kα selective inhibitor alpelisib mechanism of action and efficacy in ER+/ PIK3CA mutant breast cancer preclinical models

Christine Fritsch, Estelle Pfister, Nicolas Ebel, Daniel Guthy, Christian Schnell, Francesco Hofmann
Journal: Cancer Research
Cancer Res (2018) 78 (13_Supplement): 3934.
https://doi.org/10.1158/1538-7445.AM2018-3934
Published: 01 July 2018
View article titled, Abstract 3934: Determination of the PI3Kα selective inhibitor alpelisib mechanism of action and efficacy in ER+/ PIK3CA mutant breast cancer preclinical models
Journal Articles

Abstract 5560: PD-1/PD-L1 blockade enhances MDM2 inhibitor activity in p53 wild-type cancers

Hui Qin Wang, Jinsheng Liang, Iain Mulford, Fiona Sharp, Swann Gaulis, Yan Chen, Gina Trabucco, David Quinn, Joseph D. Growney, Matthew J. Meyer, Juliet Williams, Peter Hammerman, Francesco Hofmann, Glenn Dranoff, Jeffrey Engelman, Jennifer Mataraza, Ensar Halilovic
Journal: Cancer Research
Cancer Res (2018) 78 (13_Supplement): 5560.
https://doi.org/10.1158/1538-7445.AM2018-5560
Published: 01 July 2018
View article titled, Abstract 5560: PD-1/PD-L1 blockade enhances MDM2 inhibitor activity in p53 wild-type cancers
Journal Articles

Abstract 2098: NVP-FGF401, a first-in-class highly selective and potent FGFR4 inhibitor for the treatment of HCC

Diana Graus Porta, Andreas Weiss, Robin A. Fairhurst, Markus Wartmann, Christelle Stamm, Flavia Reimann, Alexandra Buhles, Jaqueline Kinyamu-Akunda, Dario Sterker, Masato Murakami, Youzhen Wang, Jeffrey Engelman, Francesco Hofmann, William R. Sellers
Journal: Cancer Research
Cancer Res (2017) 77 (13_Supplement): 2098.
https://doi.org/10.1158/1538-7445.AM2017-2098
Published: 01 July 2017
View article titled, Abstract 2098: NVP-FGF401, a first-in-class highly selective and potent FGFR4 inhibitor for the treatment of HCC
Journal Articles

Abstract 2103: NVP-FGF401: Cellular and in vivo profile of a novel highly potent and selective FGFR4 inhibitor for the treatment of FGF19/FGFR4/KLB+ tumors

Andreas Weiss, Diana Graus Porta, Flavia Reimann, Alexandra Buhles, Christelle Stamm, Robin A. Fairhurst, Jacqueline Kinyamu-Akunda, Dario Sterker, Masato Murakami, Markus Wartmann, Youzhen Wang, Jeffrey A. Engelman, Francesco Hofmann, Wiliam R. Sellers
Journal: Cancer Research
Cancer Res (2017) 77 (13_Supplement): 2103.
https://doi.org/10.1158/1538-7445.AM2017-2103
Published: 01 July 2017
View article titled, Abstract 2103: NVP-FGF401: Cellular and in vivo profile of a novel highly potent and selective FGFR4 inhibitor for the treatment of FGF19/FGFR4/KLB+ tumors
Journal Articles

Abstract 1225: NVP-HDM201: cellular and in vivo profile of a novel highly potent and selective PPI inhibitor of p53-Mdm2

Sébastien Jeay, Patrick Chène, Stéphane Ferretti, Pascal Furet, Bjoern Gruenenfelder, Vito Guagnano, Nelson Guerreiro, Ensar Halilovic, Francesco Hofmann, Joerg Kallen, Michelle Léonard, Robert Mah, Keiichi Masuya, Rita Ramos, Caroline Rynn, Stephan Ruetz, Thérèse Stachyra-Valat, Stefan Stutz, Andrea Vaupel, Jens Wuerthner, Philipp Holzer
Journal: Cancer Research
Cancer Res (2016) 76 (14_Supplement): 1225.
https://doi.org/10.1158/1538-7445.AM2016-1225
Published: 15 July 2016
View article titled, Abstract 1225: NVP-HDM201: cellular and in vivo profile of a novel highly potent and selective PPI inhibitor of p53-Mdm2
Journal Articles

Abstract 1224: Insights into the mechanism of action of NVP-HDM201, a differentiated and versatile Next-Generation small-molecule inhibitor of Mdm2, under evaluation in phase I clinical trials

Stéphane Ferretti, Ramona Rebmann, Marjorie Berger, Francesca Santacroce, Geneviève Albrecht, Kerstin Pollehn, Dario Sterker, Markus Wartmann, Andreas Hueber, Marion Wiesmann, Michael R. Jensen, Francesco Hofmann, William R. Sellers, Philipp Holzer, Sébastien Jeay
Journal: Cancer Research
Cancer Res (2016) 76 (14_Supplement): 1224.
https://doi.org/10.1158/1538-7445.AM2016-1224
Published: 15 July 2016
View article titled, Abstract 1224: Insights into the mechanism of action of NVP-HDM201, a differentiated and versatile Next-Generation small-molecule inhibitor of Mdm2, under evaluation in phase I clinical trials
Journal Articles

Abstract 1239: NVP-HDM201: Biochemical and biophysical profile of a novel highly potent and selective PPI inhibitor of p53-Mdm2

Thérèse Stachyra-Valat, Frédéric Baysang, Anne-Cécile D’Alessandro, Erdmann Dirk, Pascal Furet, Vito Guagnano, Joerg Kallen, Lukas Leder, Robert Mah, Keiichi Masuya, Stefan Stutz, Andrea Vaupel, Francesco Hofmann, Patrick Chène, Sébastien Jeay, Philipp Holzer
Journal: Cancer Research
Cancer Res (2016) 76 (14_Supplement): 1239.
https://doi.org/10.1158/1538-7445.AM2016-1239
Published: 15 July 2016
View article titled, Abstract 1239: NVP-HDM201: Biochemical and biophysical profile of a novel highly potent and selective PPI inhibitor of p53-Mdm2
Journal Articles

Abstract LB-017: Disordered methionine metabolism in MTAP/CDKN2A-deleted cancers leads to marked dependence on PRMT5

Konstantinos Mavrakis, E Robert McDonald, III, Michael R. Schlabach, Eric Billy, Gregory R. Hoffman, Antoine deWeck, David A. Ruddy, Kavitha Venkatesan, Greg McAllister, Rosalie deBeaumont, Samuel Ho, Yue Liu, Yan Yan-Neale, Guizhi Yang, Fallon Lin, Hong Yin, Hui Gao, David Randal Kipp, Songping Zhao, Joshua T. McNamara, Elizabeth R. Sprague, Young Shin Cho, Justin Gu, Ken Crawford, Vladimir Capka, Kristen Hurov, Jeffrey A. Porter, John Tallarico, Craig Mickanin, Emma Lees, Raymond Pagliarini, Nicholas Keen, Tobias Schmelzle, Francesco Hofmann, Frank Stegmeier, William R. Sellers
Journal: Cancer Research
Cancer Res (2016) 76 (14_Supplement): LB-017.
https://doi.org/10.1158/1538-7445.AM2016-LB-017
Published: 15 July 2016
View article titled, Abstract LB-017: Disordered methionine metabolism in MTAP/CDKN2A-deleted cancers leads to marked dependence on PRMT5
Journal Articles

Abstract 4855: Discovery of NVP-HDM201 - First disclosure of a Next-Generation Mdm2 inhibitor with superior characteristics

Philipp Holzer, Patrick Chène, Stéphane Ferretti, Pascal Furet, Tobias Gabriel, Bjoern Gruenenfelder, Vito Guagnano, Francesco Hofmann, Joerg Kallen, Robert Mah, Keiichi Masuya, Rita Ramos, Stephan Ruetz, Caroline Rynn, Thérèse Stachyra-Valat, Stefan Stutz, Andrea Vaupel, Sébastien Jeay.
Journal: Cancer Research
Cancer Res (2016) 76 (14_Supplement): 4855.
https://doi.org/10.1158/1538-7445.AM2016-4855
Published: 15 July 2016
View article titled, Abstract 4855: Discovery of NVP-HDM201 - First disclosure of a Next-Generation Mdm2 inhibitor with superior characteristics
Journal Articles

Maximizing the Efficacy of MAPK-Targeted Treatment in PTENLOF/BRAFMUT Melanoma through PI3K and IGF1R Inhibition

Barbara Herkert, Audrey Kauffmann, Sandra Mollé, Christian Schnell, Thomas Ferrat, Hans Voshol, Janina Juengert, Hélène Erasimus, Grégory Marszalek, Malika Kazic-Legueux, Eric Billy, David Ruddy, Mark Stump, Daniel Guthy, Mitko Ristov, Keith Calkins, Sauveur-Michel Maira, William R. Sellers, Francesco Hofmann, Michael N. Hall, Saskia M. Brachmann
Journal: Cancer Research
Cancer Res (2016) 76 (2): 390–402.
https://doi.org/10.1158/0008-5472.CAN-14-3358
Published: 14 January 2016
View article titled, Maximizing the Efficacy of MAPK-Targeted Treatment in <em>PTEN</em><sup>LOF</sup><em>/BRAF</em><sup>MUT</sup> Melanoma through PI3K and IGF1R Inhibition
Open the PDF for Maximizing the Efficacy of MAPK-Targeted Treatment in <em>PTEN</em><sup>LOF</sup><em>/BRAF</em><sup>MUT</sup> Melanoma through PI3K and IGF1R Inhibition in another window
Includes: Supplementary data
Journal Articles

Abstract DDT01-01: Discovery of CGM097 as a novel Mdm2 inhibitor

Keiichi Masuya, Pascal Furet, Stefan Stutz, Philipp Holzer, Carole Pissot-Soldmann, Nicole Buschmann, Thérèse Valat, Stéphane Ferretti, Stephan Ruetz, Caroline Rynn, Joerg Berghausen, Edgar Jacoby, Marc Lang, Tobias Gabriel, Francesco Hofmann, Joerg Kallen, Sébastien Jeay, Francois Gessier
Journal: Cancer Research
Cancer Res (2014) 74 (19_Supplement): DDT01-01.
https://doi.org/10.1158/1538-7445.AM2014-DDT01-01
Published: 01 October 2014
View article titled, Abstract DDT01-01: Discovery of CGM097 as a novel Mdm2 inhibitor
Journal Articles

Abstract 1798: Mechanistic study of NVP-CGM097: a potent, selective and species specific inhibitor of p53-Mdm2

Thérèse Valat, Keiichi Masuya, Frédéric Baysang, Geneviève Albrecht, Nicole Buschmann, Dirk Erdmann, Pascal Furet, Tobias Gabriel, François Gessier, Francesco Hofmann, Philipp Holzer, Joerg Kallen, Carole Pissot-Solderman, Stefan Stutz, Patrick Chène, Sébastien Jeay
Journal: Cancer Research
Cancer Res (2014) 74 (19_Supplement): 1798.
https://doi.org/10.1158/1538-7445.AM2014-1798
Published: 01 October 2014
View article titled, Abstract 1798: Mechanistic study of NVP-CGM097: a potent, selective and species specific inhibitor of p53-Mdm2
Journal Articles

Abstract 1797: Discovery of NVP-CGM097, a highly potent and optimized small molecule inhibitor of Mdm2 under evaluation in a Phase I clinical trial

Sebastien Jeay, Joerg Berghausen, Nicole Buschmann, Patrick Chène, Robert Cozens, Dirk Erdmann, Stéphane Ferretti, Pascal Furet, Tobias Gabriel, François Gessier, Diana Graus-Porta, Francesco Hofmann, Philipp Holzer, Moriko Ito, Edgar Jacoby, Michael Jensen, Joerg Kallen, Marc Lang, Joanna Lisztwan, Masato Murakami, Carole Pissot-Soldermann, Stephan Ruetz, Caroline Rynn, Dario Sterker, Stefan Stutz, Thérèse Valat, Marion Wiesmann, Keiichi Masuya
Journal: Cancer Research
Cancer Res (2014) 74 (19_Supplement): 1797.
https://doi.org/10.1158/1538-7445.AM2014-1797
Published: 01 October 2014
View article titled, Abstract 1797: Discovery of NVP-CGM097, a highly potent and optimized small molecule inhibitor of Mdm2 under evaluation in a Phase I clinical trial
Journal Articles

Abstract 3743: NVP-BYL719, a selective inhibitor of the class Ia PI3K isoform alpha impairs angiogenesis and microvascular permeability.

Christian R. Schnell, Stephanie Barbe, Giorgio Caravatti, Saskia Brachmann, Daniel Guthy, Sauveur Michel Maira, Robert Cozens, Francesco Hofmann, Christine Fritsch
Journal: Cancer Research
Cancer Res (2012) 72 (8_Supplement): 3743.
https://doi.org/10.1158/1538-7445.AM2012-3743
Published: 15 April 2012
View article titled, Abstract 3743: NVP-BYL719, a selective inhibitor of the class Ia PI3K isoform alpha impairs angiogenesis and microvascular permeability.