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Journal Articles

Pan-KRAS inhibitors BI-2493 and BI-2865 display potent anti-tumor activity in tumors with KRAS wild-type allele amplification

Antonio Tedeschi, Fiorella Schischlik, Francesca Rocchetti, Johannes Popow, Florian Ebner, Daniel Gerlach, Antonia Geyer, Valeria Santoro, Andrew S. Boghossian, Matthew G. Rees, Melissa M. Ronan, Jennifer A. Roth, Jesse Lipp, Matthias Samwer, Michael Gmachl, Norbert Kraut, Mark Pearson, Dorothea Rudolph
Journal: Molecular Cancer Therapeutics
Mol Cancer Ther (2024)
https://doi.org/10.1158/1535-7163.MCT-24-0386
Published: 23 December 2024
View article titled, Pan-KRAS inhibitors BI-2493 and BI-2865 display potent anti-tumor activity in tumors with KRAS wild-type allele amplification
Open the PDF for Pan-KRAS inhibitors BI-2493 and BI-2865 display potent anti-tumor activity in tumors with KRAS wild-type allele amplification in another window
Includes: Supplementary data
Journal Articles

Abstract C140: BI 1810631 is a novel EGFR wild-type sparing, HER2-selective small molecule inhibitor that efficiently blocks HER2 mutant-driven lung cancer

Ralph A. Neumüller, Birgit Wilding, Dirk Scharn, Anke Baum, Martin Augsten, Irene Waizenegger, Shinji Kohsaka, Valeria Santoro, Paolo Chetta, Lydia Woelflingseder, Johannes Popow, Daniel Gerlach, Peter Ettmayer, Thomas Gerstberger, Julian Fuchs, Matthias Treu, Stephan Zahn, Mark Pearson, Mark Petronczki, Darryl B. McConnell, Norbert Kraut, Flavio Solca
Journal: Molecular Cancer Therapeutics
Mol Cancer Ther (2023) 22 (12_Supplement): C140.
https://doi.org/10.1158/1535-7163.TARG-23-C140
Published: 01 December 2023
View article titled, Abstract C140: BI 1810631 is a novel EGFR wild-type sparing, HER2-selective small molecule inhibitor that efficiently blocks HER2 mutant-driven lung cancer
Journal Articles

Abstract A085: BI KRASmulti, a first-in-class, orally bioavailable and direct inhibitor of diverse oncogenic KRAS variants drives tumor regression in preclinical models and validates wild-type amplified KRAS as a therapeutic target

Antonio Tedeschi, Lorenz Herdeis, Valeria Santoro, Fabio Savarese, Birgit Wilding, Matthias Treu, Julian Fuchs, Joachim Bröker, Tobias Wunberg, Michael Gmachl, Rumpel Klaus, Fiorella Schischlik, Jesse Lipp, David H. Peng, Mariah Williams, Charles Deckard, Vandhana Ramamoorthy, Joseph R. Daniele, Jaffer A. Ajani, Funda Meric-Bernstam, Christopher P. Vellano, Joseph R. Marszalek, Timothy P. Heffernan, Darryl McConnell, Mark Pearson, Norbert Kraut, Dorothea Rudolph
Journal: Molecular Cancer Therapeutics
Mol Cancer Ther (2023) 22 (12_Supplement): A085.
https://doi.org/10.1158/1535-7163.TARG-23-A085
Published: 01 December 2023
View article titled, Abstract A085: BI KRAS<sup>multi</sup>, a first-in-class, orally bioavailable and direct inhibitor of diverse oncogenic KRAS variants drives tumor regression in preclinical models and validates wild-type amplified KRAS as a therapeutic target
Journal Articles

Abstract A087: BI KRASmulti, a first-in-class, orally bioavailable and direct inhibitor of diverse oncogenic KRAS variants drives tumor regression in KRAS G12V-driven preclinical models

David H Peng, Antonio Tedeschi, Lorenz Herdeis, Fabio Savarese, Francesca Rocchetti, Popow Johannes, Heinrich J Huber, Nicola Melillo, Jake Dickinson, Hitesh B Mistry, Birgit Wilding, Matthias Treu, Julian Fuchs, Joachim Broker, Tobias Wunberg, Fiorella Schischlik, Jesse Lipp, Vandhana Ramamoorthy, Joseph R Daniele, Scott Kopetz, Michael Kim, Don L Gibbons, Christopher P Vellano, Joseph R Marszalek, Timothy P Heffernan, Darryl McConnell, Mark Pearson, Norbert Kraut, Dorothea Rudolph
Journal: Molecular Cancer Therapeutics
Mol Cancer Ther (2023) 22 (12_Supplement): A087.
https://doi.org/10.1158/1535-7163.TARG-23-A087
Published: 01 December 2023
View article titled, Abstract A087: BI KRAS<sup>multi</sup>, a first-in-class, orally bioavailable and direct inhibitor of diverse oncogenic KRAS variants drives tumor regression in KRAS G12V-driven preclinical models
Journal Articles

Abstract A092: Determinants of sensitivity to BI KRASmulti inhibitor using high-throughput in-vitro drug screens

Fiorella Schischlik, Antonio Tedeschi, Dorothea Rudolph, Daniel Gerlach, Birgit Wilding, Matthias Treu, Julian Fuchs, Lorenz Herdeis, Joachim Broeker, Tobias Wunberg, Andrew S. Boghossian, Matthew G. Rees, Melissa M. Ronan, Jennifer A. Roth, Darryl McConnell, Mark Pearson, Norbert Kraut, Christian Haslinger, Jesse Lipp
Journal: Molecular Cancer Therapeutics
Mol Cancer Ther (2023) 22 (12_Supplement): A092.
https://doi.org/10.1158/1535-7163.TARG-23-A092
Published: 01 December 2023
View article titled, Abstract A092: Determinants of sensitivity to BI KRAS<sup>multi</sup> inhibitor using high-throughput <em>in-vitro</em> drug screens
Journal Articles

Selective Tumor Cell Apoptosis and Tumor Regression in CDH17-Positive Colorectal Cancer Models using BI 905711, a Novel Liver-Sparing TRAILR2 Agonist

Juan Manuel García-Martínez, Shirley Wang, Cordula Weishaeupl, Andreas Wernitznig, Paolo Chetta, Catarina Pinto, Jason Ho, Darrin Dutcher, Philip N. Gorman, Rachel Kroe-Barrett, Joerg Rinnenthal, Craig Giragossian, Maria Antonietta Impagnatiello, Iñigo Tirapu, Frank Hilberg, Norbert Kraut, Mark Pearson, Klaus Peter Kuenkele
Journal: Molecular Cancer Therapeutics
Series: Author Choice
Mol Cancer Ther (2021) 20 (1): 96–108.
https://doi.org/10.1158/1535-7163.MCT-20-0253
Published: 05 January 2021
View article titled, Selective Tumor Cell Apoptosis and Tumor Regression in CDH17-Positive Colorectal Cancer Models using BI 905711, a Novel Liver-Sparing TRAILR2 Agonist
Open the PDF for Selective Tumor Cell Apoptosis and Tumor Regression in CDH17-Positive Colorectal Cancer Models using BI 905711, a Novel Liver-Sparing TRAILR2 Agonist in another window
Includes: Supplementary data
Journal Articles

Selective and Potent CDK8/19 Inhibitors Enhance NK-Cell Activity and Promote Tumor Surveillance

Marco H. Hofmann, Rajeswaran Mani, Harald Engelhardt, Maria A. Impagnatiello, Sebastian Carotta, Marc Kerenyi, Seila Lorenzo-Herrero, Jark Böttcher, Dirk Scharn, Heribert Arnhof, Andreas Zoephel, Renate Schnitzer, Thomas Gerstberger, Michael P. Sanderson, Girish Rajgolikar, Swagata Goswami, Sumithira Vasu, Peter Ettmayer, Segundo Gonzalez, Mark Pearson, Darryl B. McConnell, Norbert Kraut, Natarajan Muthusamy, Jürgen Moll
Journal: Molecular Cancer Therapeutics
Mol Cancer Ther (2020) 19 (4): 1018–1030.
https://doi.org/10.1158/1535-7163.MCT-19-0789
Published: 02 April 2020
View article titled, Selective and Potent CDK8/19 Inhibitors Enhance NK-Cell Activity and Promote Tumor Surveillance
Open the PDF for Selective and Potent CDK8/19 Inhibitors Enhance NK-Cell Activity and Promote Tumor Surveillance in another window
Includes: Supplementary data
Journal Articles

Abstract C133: Effective targeting of KRAS-driven tumors by the first-in-class, orally bioavailable SOS1::KRAS inhibitor BI-3406

Marco H Hofmann, Michael Gmachl, Jürgen Ramharter, Fabio Savarese, Michael P Sanderson, Daniel Gerlach, Francesca Trapani, Dana-Adriana Botesteanu, Dirk Kessler, Peter Ettmayer, Heribert Arnhof, Thomas Gerstberger, Renate Schnitzer, Christiane Kofink, Heinz Stadtmueller, Tobias Wunberg, Jonathan C. O’Connell, Rachel L Mendes, David Richard, Adrian S Saldanha, Juergen Moll, Mark Pearson, Darryl B McConnell, Norbert Kraut
Journal: Molecular Cancer Therapeutics
Mol Cancer Ther (2019) 18 (12_Supplement): C133.
https://doi.org/10.1158/1535-7163.TARG-19-C133
Published: 01 December 2019
View article titled, Abstract C133: Effective targeting of KRAS-driven tumors by the first-in-class, orally bioavailable SOS1::KRAS inhibitor BI-3406
Journal Articles

Abstract PL06-01: Discovery of BI-3406: A potent and selective SOS1::KRAS inhibitor opens a new approach for treating KRAS-driven tumors

Marco H Hofmann, Michael Gmachl, Jürgen Ramharter, Fabio Savarese, Daniel Gerlach, Joseph R Marszalek, Michael P Sanderson, Francesca Trapani, Dirk Kessler, Klaus Rumpel, Dana-Adriana Botesteanu, Peter Ettmayer, Heribert Arnhof, Thomas Gerstberger, Christiane Kofink, Tobias Wunberg, Szu-Chin Fu, Jessica Teh, Christopher P. Vellano, Jonathan C. O’Connell, Rachel L Mendes, Juergen Moll, Timothy P. Heffernan, Mark Pearson, Darryl B McConnell, Norbert Kraut
Journal: Molecular Cancer Therapeutics
Mol Cancer Ther (2019) 18 (12_Supplement): PL06-01.
https://doi.org/10.1158/1535-7163.TARG-19-PL06-01
Published: 01 December 2019
View article titled, Abstract PL06-01: Discovery of BI-3406: A potent and selective SOS1::KRAS inhibitor opens a new approach for treating KRAS-driven tumors
Journal Articles

Delayed tissue fixation interferes with detection of phospho-activated, but not total proteins of the mTOR pathway

Maja Walker, Noelle Hanoteau, Caroline Fux, Mark Pearson, Michael Stumm
Journal: Molecular Cancer Therapeutics
Mol Cancer Ther (2007) 6 (11_Supplement): A161.
Published: 01 November 2007
View article titled, Delayed tissue fixation interferes with detection of phospho-activated, but not total proteins of the mTOR pathway