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Timothy P. Heffernan
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Journal Articles

Abstract 3321: KRASmulti inhibitor BI 3706674, an orally bioavailable, direct inhibitor of diverse oncogenic KRAS variants drives tumor regression in KRASG12V-driven preclinical models

David Hwa Peng, Antonio Tedeschi, Lorenz Herdeis, Otmar Schaaf, Fabio Savarese, Francesca Rocchetti, Johannes Popow, Heinrich J. Huber, Birgit Wilding, Matthias Treu, Julian Fuchs, Joachim Bröeker, Tobias Wunberg, Firoella Schischlik, Jesse Lipp, Mariah Williams, Vaness Chandler, Charles E. Deckard, 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: Cancer Research
Cancer Res (2024) 84 (6_Supplement): 3321.
https://doi.org/10.1158/1538-7445.AM2024-3321
Published: 22 March 2024
View article titled, Abstract 3321: KRAS<sup>multi</sup> inhibitor BI 3706674, an orally bioavailable, direct inhibitor of diverse oncogenic KRAS variants drives tumor regression in KRAS<sup>G12V</sup>-driven preclinical models
Journal Articles

Abstract 1447: Development of advanced preclinical modeling for a comprehensive characterization of cardiac angiosarcoma biology

Rosalba Minelli, Luigi Perelli, Benjamin J. Bivona, Sanjana Srinivasan, Desiree Catania, Bianca E. Amador, Frederick S. Robinson, Johnathon L. Rose, Christopher T. Terranova, Alejandro Hernandez Martinez, Charles E. Deckard, Courtney N. Le, Kuo-Shun Hsu, Michael Peoples, Aparna Subramaniam, Hannah C. Beird, Ningping Feng, Joseph R. Daniele, Christopher Vellano, Joseph Marszalek, Vinod Ravi, Alexander J. Lazar, Andrew Futreal, Timothy P. Heffernan, Giannicola Genovese, Virginia Giuliani
Journal: Cancer Research
Cancer Res (2024) 84 (6_Supplement): 1447.
https://doi.org/10.1158/1538-7445.AM2024-1447
Published: 22 March 2024
View article titled, Abstract 1447: Development of advanced preclinical modeling for a comprehensive characterization of cardiac angiosarcoma biology
Journal Articles

Abstract 6506: SOS1 inhibition in combination with HER2 inhibition in models of HER2-driven cancer

Robyn L. Schenk, Kaja Kostyrko, Johannes Popow, Christina Gewinner, Anke Baum, Christoph Albrecht, Melanie Hinkel, Robin Jacob, Tom Madensky, Regina Ruzicka, Eva Strauss, Hengyu Lyu, Anastasia M. Lopez, Ningping Feng, Christopher P. Vellano, Joseph R. Marszalek, Timothy P. Heffernan, Mark Pearson, Marco H. Hofmann
Journal: Cancer Research
Cancer Res (2024) 84 (6_Supplement): 6506.
https://doi.org/10.1158/1538-7445.AM2024-6506
Published: 22 March 2024
View article titled, Abstract 6506: SOS1 inhibition in combination with HER2 inhibition in models of HER2-driven cancer
Journal Articles

Abstract 3317: KRASmulti inhibitor BI 3706674 shows efficacy in KRAS-driven preclinical models of cancer that supports clinical testing in patients with tumors harbouring KRASG12V mutations and KRAS wild-type amplifications

Antonio Tedeschi, David H. Peng, Fiorella Schischlik, Lorenz Herdeis, Otmar Schaaf, Valeria Santoro, Daniel Gerlach, Fabio Savarese, Jesse Lipp, Christian Haslinger, Francesca Rocchetti, Johannes Popow, Heinrich J. Huber, Birgit Wilding, Matthias Treu, Julian Fuchs, Joachim Broeker, Tobias Wunber, Michael Gmachl, Klaus Rumpel, Matthew Rees, Melissa Ron, Jennifer Roth, Mariah Williams, Charles Deckard, Vandhana Ramamoorthy, Joseph R. Daniele, Jaffer A. Ajani, Funda Meric-Bernstam, 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: Cancer Research
Cancer Res (2024) 84 (6_Supplement): 3317.
https://doi.org/10.1158/1538-7445.AM2024-3317
Published: 22 March 2024
View article titled, Abstract 3317: KRAS<sup>multi</sup> inhibitor BI 3706674 shows efficacy in KRAS-driven preclinical models of cancer that supports clinical testing in patients with tumors harbouring KRAS<sup>G12V</sup> mutations and KRAS wild-type amplifications
Journal Articles

Abstract B092: CDK8 and CXCL2 remodel the tumor microenvironment to contribute to KRASG12D small molecule inhibition resistance in pancreatic ductal adenocarcinoma

Kathleen M. McAndrews, Krishnan K. Mahadevan, Bingrui Li, Amari M. Sockwell, Sami J. Morse, Patience J. Kelly, Michelle L. Kirtley, Meagan R. Conner, Sarah I. Patel, Shreyasee V. Khumbar, Kent A. Arian, Yasaman Barekatain, Barbara A. Moreno Diaz, Hengyu Lyu, Hikaru Sugimoto, Lakshmi Kavitha Sthanam, Navid Sobhani, Francesca Paradiso, Vincent Bernard, Paola Guerrero, Haoqiang Ying, Anirban Maitra, Timothy P. Heffernan, Raghu Kalluri
Journal: Cancer Research
Cancer Res (2024) 84 (2_Supplement): B092.
https://doi.org/10.1158/1538-7445.PANCA2023-B092
Published: 16 January 2024
View article titled, Abstract B092: CDK8 and CXCL2 remodel the tumor microenvironment to contribute to KRAS<sup>G12D</sup> small molecule inhibition resistance in pancreatic ductal adenocarcinoma
Journal Articles

Abstract 4017: TAS2940 inhibits intracranial tumor growth and prolongs survival in HER2-aberrant and EGFR-amplified patient-derived xenograft models

Jing Han, Mikhila Mahendra, Poojabahen Gandhi, Joseph R. Daniele, Caroline C. Carrillo, Benjamin J. Bivona, Ningping Feng, John V. Heymach, Funda Meric-Bernstam, Kei Oguchi, Shinji Mizuarai, Timothy P. Heffernan, Christopher P. Vellano, Joseph R. Marszalek
Journal: Cancer Research
Cancer Res (2023) 83 (7_Supplement): 4017.
https://doi.org/10.1158/1538-7445.AM2023-4017
Published: 04 April 2023
View article titled, Abstract 4017: TAS2940 inhibits intracranial tumor growth and prolongs survival in HER2-aberrant and EGFR-amplified patient-derived xenograft models
Journal Articles

Abstract 2667: Trial in progress: Phase 1 study of BI 1823911, an irreversible KRASG12C inhibitor targeting KRAS in its GDP-loaded state, as monotherapy and in combination with the pan-KRAS SOS1 inhibitor BI 1701963 in solid tumors expressing KRASG12C mutation

Irene C. Waizenegger, Hengyu Lu, Claus Thamer, Fabio Savarese, Daniel Gerlach, Dorothea Rudolph, Christopher P. Vellano, Marcelo Marotti, John Heymach, Scott Kopetz, Timothy P. Heffernan, Joseph R. Marszalek, Mark P. Petronczki, Marco H. Hofmann, Norbert Kraut
Journal: Cancer Research
Cancer Res (2022) 82 (12_Supplement): 2667.
https://doi.org/10.1158/1538-7445.AM2022-2667
Published: 15 June 2022
View article titled, Abstract 2667: Trial in progress: Phase 1 study of BI 1823911, an irreversible KRAS<sup>G12C</sup> inhibitor targeting KRAS in its GDP-loaded state, as monotherapy and in combination with the pan-KRAS SOS1 inhibitor BI 1701963 in solid tumors expressing KRAS<sup>G12C</sup> mutation
Journal Articles

Abstract LB079: Pancreatic clonal replica tumors display functional heterogeneity in response to KRAS pharmacological inhibition and reveal unique epigenetic vulnerabilities to overcome resistance

Hengyu Lyu, Rosalba Minelli, Charles E. Deckard, Sahil Seth, Justin Huang, Hong Jiang, Michael D. Peoples, Meggie Lam, Christopher A. Bristow, Daniel Gerlach, Ulrike Tontsch-Grunt, Chieh-Yuan Li, I-Lin Ho, Christopher P. Vellano, Marco H. Hofmann, Timothy P. Heffernan, Joseph R. Marszalek, Andrea Viale, Alessandro Carugo
Journal: Cancer Research
Cancer Res (2022) 82 (12_Supplement): LB079.
https://doi.org/10.1158/1538-7445.AM2022-LB079
Published: 15 June 2022
View article titled, Abstract LB079: Pancreatic clonal replica tumors display functional heterogeneity in response to KRAS pharmacological inhibition and reveal unique epigenetic vulnerabilities to overcome resistance
Journal Articles

Oxidative Phosphorylation Is a Metabolic Vulnerability in Chemotherapy-Resistant Triple-Negative Breast Cancer

Kurt W. Evans, Erkan Yuca, Stephen S. Scott, Ming Zhao, Natalia Paez Arango, Christian X. Cruz Pico, Turcin Saridogan, Maryam Shariati, Caleb A. Class, Christopher A. Bristow, Christopher P. Vellano, Xiaofeng Zheng, Ana Maria Gonzalez-Angulo, Xiaoping Su, Coya Tapia, Ken Chen, Argun Akcakanat, Bora Lim, Debu Tripathy, Timothy A. Yap, Maria Emilia Di Francesco, Giulio F. Draetta, Philip Jones, Timothy P. Heffernan, Joseph R. Marszalek, Funda Meric-Bernstam
Journal: Cancer Research
Cancer Res (2021) 81 (21): 5572–5581.
https://doi.org/10.1158/0008-5472.CAN-20-3242
Published: 01 November 2021
View article titled, Oxidative Phosphorylation Is a Metabolic Vulnerability in Chemotherapy-Resistant Triple-Negative Breast Cancer
Open the PDF for Oxidative Phosphorylation Is a Metabolic Vulnerability in Chemotherapy-Resistant Triple-Negative Breast Cancer in another window
Includes: Supplementary data
Journal Articles

Targeting Glucose Metabolism Sensitizes Pancreatic Cancer to MEK Inhibition

Liang Yan, Bo Tu, Jun Yao, Jing Gong, Alessandro Carugo, Christopher A. Bristow, Qiuyun Wang, Cihui Zhu, Bingbing Dai, Ya'an Kang, Leng Han, Ningping Feng, Yanqing Jin, Jason Fleming, Timothy P. Heffernan, Wantong Yao, Haoqiang Ying
Journal: Cancer Research
Cancer Res (2021) 81 (15): 4054–4065.
https://doi.org/10.1158/0008-5472.CAN-20-3792
Published: 01 August 2021
View article titled, Targeting Glucose Metabolism Sensitizes Pancreatic Cancer to MEK Inhibition
Open the PDF for Targeting Glucose Metabolism Sensitizes Pancreatic Cancer to MEK Inhibition in another window
Includes: Supplementary data
Journal Articles

Abstract 87: Asparagine synthetase (ASNS) expression predicts response to the GLS1 inhibitor IPN60090 in ovarian cancer through selective modulation of redox homeostasis

Nakia D. Spencer, Christopher A. Bristow, Virginia Giulani, Meredith A. Miller, Alessandro Carugo, Angela L. Harris, Rosalba Minelli, Ningpeng Feng, Qing Chang, Michael J. Soth, Kang Le, John N. Weinstein, Philip L. Lorenzi, Jinsong Liu, Wei-Lien Wang, Timothy A. Yap, Giulio Draetta, Philip Jones, Timothy P. Heffernan, Jeffrey J. Kovacs
Journal: Cancer Research
Cancer Res (2021) 81 (13_Supplement): 87.
https://doi.org/10.1158/1538-7445.AM2021-87
Published: 01 July 2021
View article titled, Abstract 87: Asparagine synthetase (ASNS) expression predicts response to the GLS1 inhibitor IPN60090 in ovarian cancer through selective modulation of redox homeostasis
Journal Articles

Abstract 985: BI 905711 selectively induces apoptosis and anti-tumor response in TRAILR2/CDH17- expressing pancreatic cancer models

Jing Han, Annette A. Machado, Mikhila Mahendra, Joseph R. Daniele, Christopher A. Bristow, Justin Kwang-Lay Huang, Alessandro Carugo, Robert A. Mullinax, Benjamin J. Bivona, Ningping Feng, Poojabahen Gandhi, Norbert Schweifer, Paolo Maria Chetta, Juan Manuel Garcia-Martinez, Frank Hilberg, Christopher P. Vellano, Timothy P. Heffernan, Joseph R. Marszalek
Journal: Cancer Research
Cancer Res (2021) 81 (13_Supplement): 985.
https://doi.org/10.1158/1538-7445.AM2021-985
Published: 01 July 2021
View article titled, Abstract 985: BI 905711 selectively induces apoptosis and anti-tumor response in TRAILR2/CDH17- expressing pancreatic cancer models
Journal Articles

Abstract CT210: Trial in Process: Phase 1 studies of BI 1701963, a SOS1::KRAS Inhibitor, in combination with MEK inhibitors, irreversible KRASG12C inhibitors or irinotecan.

Marco H. Hofmann, Hengyu Lu, Ulrich Duenzinger, Daniel Gerlach, Francesca Trapani, Annette A. Machado, Joseph R. Daniele, Irene Waizenegger, Michael Gmachl, Dorothea Rudolph, Christopher P. Vellano, Marcelo Marotti, Vitomir Vucenovic, Timothy P. Heffernan, Joseph R. Marszalek, Mark P. Petronczki, Norbert Kraut
Journal: Cancer Research
Cancer Res (2021) 81 (13_Supplement): CT210.
https://doi.org/10.1158/1538-7445.AM2021-CT210
Published: 01 July 2021
View article titled, Abstract CT210: Trial in Process: Phase 1 studies of BI 1701963, a SOS1::KRAS Inhibitor, in combination with MEK inhibitors, irreversible KRASG12C inhibitors or irinotecan.
Journal Articles

Abstract 2338: The GLS1 inhibitor IPN60090 enhances antitumor immune response through metabolic reprogramming of T cells and impacts on the tumor microenvironment

Erika Suzuki, Jennifer Molina, Nakia D. Spencer, Christopher A. Bristow, Angela L. Harris, Ningping Feng, Mikhila Mahendra, Sonal Gera, Michael J. Soth, Kang Le, Timothy A. Yap, Giulio Draetta, Philip Jones, Timothy P. Heffernan, Jeffrey J. Kovacs
Journal: Cancer Research
Cancer Res (2021) 81 (13_Supplement): 2338.
https://doi.org/10.1158/1538-7445.AM2021-2338
Published: 01 July 2021
View article titled, Abstract 2338: The GLS1 inhibitor IPN60090 enhances antitumor immune response through metabolic reprogramming of T cells and impacts on the tumor microenvironment
Journal Articles

Abstract 2136: Diversity across the pancreatic ductal adenocarcinoma disease spectrum revealed by network-anchored functional genomics

Sanjana Srinivasan, Johnathon Rose, Wantong Yao, Sahil Seth, Michael Peoples, Annette Machado, Chieh-Yuan Li, I Lin Ho, Jaewon J. Lee, Paola A. Guerrera, Eiru Kim, Mustafa Syed, Joseph Daniele, Angela K. Deem, Michael Kim, Christopher A. Bristow, Eugene Koay, Giannicola Genovese, Andrea Viale, Timothy P. Heffernan, Anirban Maitra, Traver Hart, Alessandro Carugo, Giulio Draetta
Journal: Cancer Research
Cancer Res (2021) 81 (13_Supplement): 2136.
https://doi.org/10.1158/1538-7445.AM2021-2136
Published: 01 July 2021
View article titled, Abstract 2136: Diversity across the pancreatic ductal adenocarcinoma disease spectrum revealed by network-anchored functional genomics
Journal Articles

Abstract 1271: In vitro and in vivo characterization of BI 1823911 - a novel KRASG12C selective small molecule inhibitor

Fabio Savarese, Andreas Gollner, Dorothea Rudolph, Jesse Lipp, Johannes Popow, Marco H. Hofmann, Heribert Arnhof, Jörg Rinnenthal, Francesca Trapani, Michael Gmachl, Daniel Gerlach, Joachim Broeker, Peter Ettmayer, Andreas Mantoulidis, Jason Phan, Christian A. Smethurst, Matthias Treu, Alex G. Waterson, Hengyu Lu, Annette Machado, Joseph Daniele, Stephan W. Fesik, Christopher P. Vellano, Timothy P. Heffernan, Joseph R. Marszalek, Darryl B. McConnell, Mark Petronczki, Norbert Kraut, Irene C. Waizenegger
Journal: Cancer Research
Cancer Res (2021) 81 (13_Supplement): 1271.
https://doi.org/10.1158/1538-7445.AM2021-1271
Published: 01 July 2021
View article titled, Abstract 1271: <em>In vitro</em> and <em>in vivo</em> characterization of BI 1823911 - a novel KRAS<sup>G12C</sup> selective small molecule inhibitor
Journal Articles

Loss of ARID1A Promotes Epithelial–Mesenchymal Transition and Sensitizes Pancreatic Tumors to Proteotoxic Stress

Hideo Tomihara, Federica Carbone, Luigi Perelli, Justin K. Huang, Melinda Soeung, Johnathon L. Rose, Frederick S. Robinson, Yonathan Lissanu Deribe, Ningping Feng, Mitsunobu Takeda, Akira Inoue, Edoardo Del Poggetto, Angela K. Deem, Anirban Maitra, Pavlos Msaouel, Nizar M. Tannir, Giulio F. Draetta, Andrea Viale, Timothy P. Heffernan, Christopher A. Bristow, Alessandro Carugo, Giannicola Genovese
Journal: Cancer Research
Series: Author Choice
Cancer Res (2021) 81 (2): 332–343.
https://doi.org/10.1158/0008-5472.CAN-19-3922
Published: 15 January 2021
View article titled, Loss of ARID1A Promotes Epithelial–Mesenchymal Transition and Sensitizes Pancreatic Tumors to Proteotoxic Stress
Open the PDF for Loss of ARID1A Promotes Epithelial–Mesenchymal Transition and Sensitizes Pancreatic Tumors to Proteotoxic Stress in another window
Includes: Supplementary data
Journal Articles

Allosteric SHP2 Inhibitor, IACS-13909, Overcomes EGFR-Dependent and EGFR-Independent Resistance Mechanisms toward Osimertinib

Yuting Sun, Brooke A. Meyers, Barbara Czako, Paul Leonard, Faika Mseeh, Angela L. Harris, Qi Wu, Sarah Johnson, Connor A. Parker, Jason B. Cross, Maria Emilia Di Francesco, Benjamin J. Bivona, Christopher A. Bristow, Jason P. Burke, Caroline C. Carrillo, Christopher L. Carroll, Qing Chang, Ningping Feng, Guang Gao, Sonal Gera, Virginia Giuliani, Justin K. Huang, Yongying Jiang, Zhijun Kang, Jeffrey J. Kovacs, Chiu-Yi Liu, Anastasia M. Lopez, Xiaoyan Ma, Pijus K. Mandal, Timothy McAfoos, Meredith A. Miller, Robert A. Mullinax, Michael Peoples, Vandhana Ramamoorthy, Sahil Seth, Nakia D. Spencer, Erika Suzuki, Christopher C. Williams, Simon S. Yu, Andy M. Zuniga, Giulio F. Draetta, Joseph R. Marszalek, Timothy P. Heffernan, Nancy E. Kohl, Philip Jones
Journal: Cancer Research
Series: Author Choice
Cancer Res (2020) 80 (21): 4840–4853.
https://doi.org/10.1158/0008-5472.CAN-20-1634
Published: 03 November 2020
View article titled, Allosteric SHP2 Inhibitor, IACS-13909, Overcomes EGFR-Dependent and EGFR-Independent Resistance Mechanisms toward Osimertinib
Open the PDF for Allosteric SHP2 Inhibitor, IACS-13909, Overcomes EGFR-Dependent and EGFR-Independent Resistance Mechanisms toward Osimertinib in another window
Includes: Supplementary data
Journal Articles

Abstract 1091: BI-3406 and BI 1701963: Potent and selective SOS1::KRAS inhibitors induce regressions in combination with MEK inhibitors or irinotecan

Daniel Gerlach, Michael Gmachl, Juergen Ramharter, Jessica Teh, Szu-Chin Fu, Francesca Trapani, Dirk Kessler, Klaus Rumpel, Dana-Adriana Botesteanu, Peter Ettmayer, Heribert Arnhof, Thomas Gerstberger, Christiane Kofink, Tobias Wunberg, Christopher P. Vellano, Timothy P. Heffernan, Joseph R. Marszalek, Mark Pearson, Darryl B. McConnell, Norbert Kraut, Marco H. Hofmann
Journal: Cancer Research
Cancer Res (2020) 80 (16_Supplement): 1091.
https://doi.org/10.1158/1538-7445.AM2020-1091
Published: 15 August 2020
View article titled, Abstract 1091: BI-3406 and BI 1701963: Potent and selective SOS1::KRAS inhibitors induce regressions in combination with MEK inhibitors or irinotecan
Journal Articles

Abstract GS4-02: Investigating genomic and phenotypic evolution of triple negative breast cancer chemoresistance and metastasis in patient-derived xenografts

Gloria V Echeverria, Mingchu Xu, Jiansu Shao, Xiaomei Zhang, Sabrina Jeter-Jones, Xinhui Zhou, Stacy L Moulder, Joseph R Marszalek, Timothy P Heffernan, Fraser W Symmans, Jeffrey T Chang, Helen Piwnica-Worms
Journal: Cancer Research
Cancer Res (2020) 80 (4_Supplement): GS4-02.
https://doi.org/10.1158/1538-7445.SABCS19-GS4-02
Published: 15 February 2020
View article titled, Abstract GS4-02: Investigating genomic and phenotypic evolution of triple negative breast cancer chemoresistance and metastasis in patient-derived xenografts