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Journal Articles

Abstract 2081: Robust activity of BLU-285, a potent and highly selective inhibitor of mutant KIT and PDGFRα, in patient-derived xenograft (PDX) models of gastrointestinal stromal tumor (GIST)

Yemarshet K. Gebreyohannes, Agnieszka Wozniak, Madelina-Elena Zhai, Jasmien Wellens, Jasmien Cornillie, Erica Evans, Alexandra K Gardino, Christoph Lengauer, Maria Debiec-Rychter, Raf Sciot, Patrick Schöffski

Cancer Res (2017) 77 (13_Supplement): 2081.

https://doi.org/10.1158/1538-7445.AM2017-2081

Published: 01 July 2017

View article titled, Abstract 2081: Robust activity of BLU-285, a potent and highly selective inhibitor of mutant KIT and PDGFRα, in patient-derived xenograft (PDX) models of gastrointestinal stromal tumor (GIST)

Journal Articles

Abstract 2641: The development of potent, selective RET inhibitors that target both wild-type RET and prospectively identified resistance mutations to multi-kinase inhibitors

Rami Rahal, Erica K. Evans, Wei Hu, Michelle Maynard, Paul Fleming, Lucian DiPietro, Joseph L. Kim, Michael P. Sheets, Doug P. Wilson, Kevin J. Wilson, Nicolas Stransky, Jason D. Brubaker, Timothy Guzi, Nancy E. Kohl, Christoph Lengauer

Cancer Res (2016) 76 (14_Supplement): 2641.

https://doi.org/10.1158/1538-7445.AM2016-2641

Published: 15 July 2016

View article titled, Abstract 2641: The development of potent, selective RET inhibitors that target both wild-type RET and prospectively identified resistance mutations to multi-kinase inhibitors

Journal Articles

Abstract 791: BLU-285, the first selective inhibitor of PDGFRα D842V and KIT Exon 17 mutants

Erica K. Evans, Brian L. Hodous, Alexandra K. Gardino, Alison Davis, Julia Zhu, Adam Shutes, Joseph L. Kim, Kevin J. Wilson, Doug Wilson, Yulian Zhang, Tat Chu, Nancy E. Kohl, Vivek Kadambi, Timothy Guzi, Christoph Lengauer

Cancer Res (2015) 75 (15_Supplement): 791.

https://doi.org/10.1158/1538-7445.AM2015-791

Published: 01 August 2015

View article titled, Abstract 791: BLU-285, the first selective inhibitor of PDGFRα D842V and KIT Exon 17 mutants

Journal Articles

Abstract 954: The landscape of kinase fusions in cancer

Nicolas Stransky, Ethan Cerami, Stefanie Schalm, Joseph L. Kim, Klaus Hoeflich, Christoph Lengauer

Cancer Res (2015) 75 (15_Supplement): 954.

https://doi.org/10.1158/1538-7445.AM2015-954

Published: 01 August 2015

View article titled, Abstract 954: The landscape of kinase fusions in cancer

Journal Articles

Abstract LB-324: First isoform selective inhibitor of FGFR4 for the treatment of genomically defined patients with hepatocellular carcinoma

Margit Hagel, Chandra Miduturu, Mike Sheets, Weifan Weng, Nooreen Rubin, Neil Bifulco, Lucian DiPietro, Joseph Kim, Natasja Brooijmans, Nicolas Stransky, Christopher Winter, Christoph Lengauer, Timothy Guzi

Cancer Res (2014) 74 (19_Supplement): LB-324.

https://doi.org/10.1158/1538-7445.AM2014-LB-324

Published: 01 October 2014

View article titled, Abstract LB-324: First isoform selective inhibitor of FGFR4 for the treatment of genomically defined patients with hepatocellular carcinoma

Journal Articles

Abstract 2201: The molecular signature of tumor cells that are sensitives to a new tight binder NAMPT inhibitor.

Cancer Res (2013) 73 (8_Supplement): 2201.

https://doi.org/10.1158/1538-7445.AM2013-2201

Published: 15 April 2013

View article titled, Abstract 2201: The molecular signature of tumor cells that are sensitives to a new tight binder NAMPT inhibitor.

Journal Articles

Abstract 3258: Discovery and characterization of SAR260301, a novel PI3Kβ-selective inhibitor in clinical development for the treatment of PTEN-deficient tumors .

Angela Virone-Oddos, Hélène Bonnevaux, Olivier Lemaitre, Loic Vincent, Franck Halley, Brigitte Demers, Véronique Charrier, Olivier Courtin, Stéphane Guérif, Laurent Besret, Pierre-Yves Abecassis, Sylvaine Cartot-Cotton, Gary Emmons, Alan Roberts, David Compton, Bin Wu, Laurent Schio, Christoph Lengauer, Carlos Garcia-Echeverria

Cancer Res (2013) 73 (8_Supplement): 3258.

https://doi.org/10.1158/1538-7445.AM2013-3258

Published: 15 April 2013

View article titled, Abstract 3258: Discovery and characterization of SAR260301, a novel PI3Kβ-selective inhibitor in clinical development for the treatment of PTEN-deficient tumors .

Journal Articles

Abstract 3135: In vitro and in vivo synthetic lethal screens to identify novel targets in the context of PTEN deficiency.

Cancer Res (2013) 73 (8_Supplement): 3135.

https://doi.org/10.1158/1538-7445.AM2013-3135

Published: 15 April 2013

View article titled, Abstract 3135: In vitro and in vivo synthetic lethal screens to identify novel targets in the context of PTEN deficiency.

Journal Articles

Abstract 1135: Chemical Proteomics effort identifies PKN1 as a key player in the canonical NF-κB signaling pathway.

Katherine Tang, Michael Lampa, Tieu-Binh Le, Matthieu Barrague, Ronald Tomlinson, Brittain Scott, Tahir Majid, Marion Dorsch, Hong Cheng, Christoph Lengauer, Carlos Garcia-Echeverria, Francisco Adrian, Mikhail Levit, Balin Zhang, Kin Yu, Ivan Cornella-Taracido, Lakshmi Srinivasan

Cancer Res (2013) 73 (8_Supplement): 1135.

https://doi.org/10.1158/1538-7445.AM2013-1135

Published: 15 April 2013

View article titled, Abstract 1135: Chemical Proteomics effort identifies PKN1 as a key player in the canonical NF-κB signaling pathway.

Journal Articles

Abstract 4376: Evaluation of PRP4 kinase as a potential drug target in cancer.

Qiang Gao, Ingrid Mechin, Nayantara Kothari, Zhuyan Guo, Gejing Deng, Anlai Wang, Dmitri Wiederschain, Jennifer Rocnik, Werngard Czechtizky, Feng Liu, Tahir Majid, Vinod Patel, Christoph Lengauer, Carlos Garcia-Echeverria, Bailin Zhang, Hong Cheng, Marion Dorsch, Shih-Min A. Huang

Cancer Res (2013) 73 (8_Supplement): 4376.

https://doi.org/10.1158/1538-7445.AM2013-4376

Published: 15 April 2013

View article titled, Abstract 4376: Evaluation of PRP4 kinase as a potential drug target in cancer.

Journal Articles

Abstract 845: In vitro and in vivo pharmacology of SAR125844, a potent and selective intravenous MET kinase inhibitor undergoing Phase I clinical trial

Hélène Goulaouic, Mireille Kenigsberg, Christine Delaisi, Françoise Begassat, Véronique Do-Vale, Jessica Mestadier, Fabrice Bonche, Tsiala Bénard, Jean-Paul Nicolas, Loreley Calvet, Coumaran Egile, Conception Nemecek, Christoph Lengauer

Cancer Res (2012) 72 (8_Supplement): 845.

https://doi.org/10.1158/1538-7445.AM2012-845

Published: 15 April 2012

View article titled, Abstract 845: In vitro and in vivo pharmacology of SAR125844, a potent and selective intravenous MET kinase inhibitor undergoing Phase I clinical trial

Journal Articles

Abstract 4731: Cytotoxic versus cytostatic effects in tumor models by spiro-oxindole-based modulators of the MDM2-p53 interaction

Isabelle Meaux, Cédric Barrière, Donna McEachern, Stéphane Guerif, Laurent Besret, Odette Dos-Santos, Stéphane D'Agostino, Isabelle Sanchez, Dimitri Gorge-Bernat, Pascal Pannier, Nathalie Ratet, James Watters, Harry Miao, Jason Sager, Christoph Lengauer, Carlos Garcia-Echeverria, Shaomeng Wang, Lance Leopold, Laurent Debussche

Cancer Res (2012) 72 (8_Supplement): 4731.

https://doi.org/10.1158/1538-7445.AM2012-4731

Published: 15 April 2012

View article titled, Abstract 4731: Cytotoxic versus cytostatic effects in tumor models by spiro-oxindole-based modulators of the MDM2-p53 interaction

Journal Articles

Abstract 2911: SAR125844: a potent and selective ATP-competitive inhibitor of MET kinase

Laurent Schio, Conception Nemecek, Antonio Ugolini, Sylvie Wentzler, Sandrine Grapinet, Jean Khider, Eva Albert, Nathalie Dischamps, Frédéric Gay, Véronique Sonnefraud, Eric Bacqué, Mireille Kenigsberg, Hélène Goulaouic, Anne Dagallier, François Vallée, Fabrice Bonche, Christoph Lengauer

Cancer Res (2012) 72 (8_Supplement): 2911.

https://doi.org/10.1158/1538-7445.AM2012-2911

Published: 15 April 2012

View article titled, Abstract 2911: SAR125844: a potent and selective ATP-competitive inhibitor of MET kinase

Journal Articles

Abstract 4648: In vitro characterization of spiro-oxindole-based modulators of the MDM2-p53 interaction and their interspecies selectivity.

Cancer Res (2012) 72 (8_Supplement): 4648.

https://doi.org/10.1158/1538-7445.AM2012-4648

Published: 15 April 2012

View article titled, Abstract 4648: In vitro characterization of spiro-oxindole-based modulators of the MDM2-p53 interaction and their interspecies selectivity.

Journal Articles

Abstract 2338: Aflibercept (VEGF Trap) impairs tumor growth and perfusion, and restrains metastasis invasion in orthotopic models

Chantal Carrez, Erwan Jouannot, Stéphane Guerif, Christoph Lengauer, Donald Bergstrom, Marielle Chiron

Cancer Res (2012) 72 (8_Supplement): 2338.

https://doi.org/10.1158/1538-7445.AM2012-2338

Published: 15 April 2012

View article titled, Abstract 2338: Aflibercept (VEGF Trap) impairs tumor growth and perfusion, and restrains metastasis invasion in orthotopic models

Journal Articles

Abstract LB-295: Combination of PI3K (SAR245408 and SAR245409) and MEK (MSC1936369B) inhibitors induce tumor apoptosis in vivo: fluorescence molecular tomography study in a human colon carcinoma xenograft model

Stephane GUERIF, Sebastien D'heilly, Celine Lefranc, Coumaran Egile, Laurent Debusshe, Loïc Vincent, Chantal Carrez, Marielle Chiron, Jiango Ma, Janet A. Ogden, Joanne Lager, Carlos Garcia-Echeverria, Christoph Lengauer

Cancer Res (2011) 71 (8_Supplement): LB-295.

https://doi.org/10.1158/1538-7445.AM2011-LB-295

Published: 15 April 2011

View article titled, Abstract LB-295: Combination of PI3K (SAR245408 and SAR245409) and MEK (MSC1936369B) inhibitors induce tumor apoptosis in vivo: fluorescence molecular tomography study in a human colon carcinoma xenograft model

Journal Articles

The Polycomb Group Protein Bmi-1 Is Essential for the Growth of Multiple Myeloma Cells

Zainab Jagani, Dmitri Wiederschain, Alice Loo, Dan He, Rebecca Mosher, Paul Fordjour, John Monahan, Michael Morrissey, Yung-Mae Yao, Christoph Lengauer, Markus Warmuth, William R. Sellers, Marion Dorsch

Cancer Res (2010) 70 (13): 5528–5538.

https://doi.org/10.1158/0008-5472.CAN-09-4229

Published: 30 June 2010

View article titled, The Polycomb Group Protein Bmi-1 Is Essential for the Growth of Multiple Myeloma Cells

Includes: Supplementary data

Journal Articles

Abstract 4475: Discovery and characterization of PI3K isoform-selective inhibitors

Cancer Res (2010) 70 (8_Supplement): 4475.

https://doi.org/10.1158/1538-7445.AM10-4475

Published: 15 April 2010

View article titled, Abstract 4475: Discovery and characterization of PI3K isoform-selective inhibitors

Journal Articles

Abstract 1976: The discovery of mechanisms of resistance to SMO antagonists and the therapeutic implications

Cancer Res (2010) 70 (8_Supplement): 1976.

https://doi.org/10.1158/1538-7445.AM10-1976

Published: 15 April 2010

View article titled, Abstract 1976: The discovery of mechanisms of resistance to SMO antagonists and the therapeutic implications

Journal Articles

PI3K Pathway Activation Mediates Resistance to MEK Inhibitors in KRAS Mutant Cancers

Susan Wee, Zainab Jagani, Kay Xiaoqin Xiang, Alice Loo, Marion Dorsch, Yung-Mae Yao, William R. Sellers, Christoph Lengauer, Frank Stegmeier

Cancer Res (2009) 69 (10): 4286–4293.

https://doi.org/10.1158/0008-5472.CAN-08-4765

Published: 15 May 2009

View article titled, PI3K Pathway Activation Mediates Resistance to MEK Inhibitors in KRAS Mutant Cancers

Includes: Supplementary data

NARROW

Abstract 2081: Robust activity of BLU-285, a potent and highly selective inhibitor of mutant KIT and PDGFRα, in patient-derived xenograft (PDX) models of gastrointestinal stromal tumor (GIST)

Abstract 2641: The development of potent, selective RET inhibitors that target both wild-type RET and prospectively identified resistance mutations to multi-kinase inhibitors

Abstract 791: BLU-285, the first selective inhibitor of PDGFRα D842V and KIT Exon 17 mutants

Abstract 954: The landscape of kinase fusions in cancer

Abstract LB-324: First isoform selective inhibitor of FGFR4 for the treatment of genomically defined patients with hepatocellular carcinoma

Abstract 2201: The molecular signature of tumor cells that are sensitives to a new tight binder NAMPT inhibitor.

Abstract 3258: Discovery and characterization of SAR260301, a novel PI3Kβ-selective inhibitor in clinical development for the treatment of PTEN-deficient tumors .

Abstract 3135: In vitro and in vivo synthetic lethal screens to identify novel targets in the context of PTEN deficiency.

Abstract 1135: Chemical Proteomics effort identifies PKN1 as a key player in the canonical NF-κB signaling pathway.

Abstract 4376: Evaluation of PRP4 kinase as a potential drug target in cancer.

Abstract 845: In vitro and in vivo pharmacology of SAR125844, a potent and selective intravenous MET kinase inhibitor undergoing Phase I clinical trial

Abstract 4731: Cytotoxic versus cytostatic effects in tumor models by spiro-oxindole-based modulators of the MDM2-p53 interaction

Abstract 2911: SAR125844: a potent and selective ATP-competitive inhibitor of MET kinase

Abstract 4648: In vitro characterization of spiro-oxindole-based modulators of the MDM2-p53 interaction and their interspecies selectivity.

Abstract 2338: Aflibercept (VEGF Trap) impairs tumor growth and perfusion, and restrains metastasis invasion in orthotopic models

Abstract LB-295: Combination of PI3K (SAR245408 and SAR245409) and MEK (MSC1936369B) inhibitors induce tumor apoptosis in vivo: fluorescence molecular tomography study in a human colon carcinoma xenograft model

The Polycomb Group Protein Bmi-1 Is Essential for the Growth of Multiple Myeloma Cells

Abstract 4475: Discovery and characterization of PI3K isoform-selective inhibitors

Abstract 1976: The discovery of mechanisms of resistance to SMO antagonists and the therapeutic implications

PI3K Pathway Activation Mediates Resistance to MEK Inhibitors in KRAS Mutant Cancers

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