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Mark Merchant
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Journal Articles

Abstract 679: Inhibition of Notch signaling causes progenitor-to-hepatocyte differentiation and regressions in a subset of hepatocellular carcinoma by controlling C/EBPα expression and HNF4α activity

Kerstin Seidel, Robert Piskol, Thi Thu Thao Nguyen, Charisa Cottonham, Mark Merchant, Christian Siebel
Journal: Cancer Research
Cancer Res (2022) 82 (12_Supplement): 679.
https://doi.org/10.1158/1538-7445.AM2022-679
Published: 15 June 2022
View article titled, Abstract 679: Inhibition of Notch signaling causes progenitor-to-hepatocyte differentiation and regressions in a subset of hepatocellular carcinoma by controlling C/EBPα expression and HNF4α activity
Journal Articles

Abstract 3327: Discovery and characterization of the potent, allosteric SHP2 inhibitor GDC-1971 for the treatment of RTK/RAS driven tumors

Bret Williams, Alexander Taylor, Olivia Orozco, Christopher Owen, Elizabeth Kelley, Andre Lescarbeau, Kelley Shortsleeves, Randy Kipp, Vy Nguyen, Erin Brophy, Jeremy Wilbur, Yong Tang, David Lanzetta, Nigel Waters, Sherri Smith, Fabrizio Giordanetto, Paul Maragakis, Jack Greismann, Lindsay Willmore, Eric Therrien, Yang Xiao, Marie Evangelista, Luca Gerosa, Eva Lin, Mark Merchant, Alfonso Arrazate, Emily Chan, Pablo Sáenz-López Larrocha, Stefan Chun, Thomas Hunsaker, Gauri Deshmukh, Christine M. Bowman, David E. Shaw, Mark Murcko, Mahesh Padval, W Patrick Walters, James Watters, Donald A. Bergstrom
Journal: Cancer Research
Cancer Res (2022) 82 (12_Supplement): 3327.
https://doi.org/10.1158/1538-7445.AM2022-3327
Published: 15 June 2022
View article titled, Abstract 3327: Discovery and characterization of the potent, allosteric SHP2 inhibitor GDC-1971 for the treatment of RTK/RAS driven tumors
Journal Articles

Abstract PO-101: Transcriptional heterogeneity in lung adenocarcinoma reveals distinct therapeutic vulnerabilities

Anneleen Daemen, Jonathan E. Cooper, Szymon Myrta, Matthew J. Wongchenko, Eva Lin, Jason E. Long, Oded Foreman, Zora Modrusan, Jarrod Tremayne, Cecile C. de la Cruz, Mark Merchant, Scott E. Martin, Yibing Yan, Melissa R. Junttila
Journal: Cancer Research
Cancer Res (2020) 80 (21_Supplement): PO-101.
https://doi.org/10.1158/1538-7445.TUMHET2020-PO-101
Published: 03 November 2020
View article titled, Abstract PO-101: Transcriptional heterogeneity in lung adenocarcinoma reveals distinct therapeutic vulnerabilities
Journal Articles

Abstract 5687: Selective, chemically-induced degradation of BRM (SMARCA2) enables in vivo efficacy in BRG1 (SMARCA4)-deficient xenograft tumor models

Michael Berlin, Jennifer Cantley, Jing Wang, Mark Bookbinder, Gregory Cadelina, Emily Chan, Huifen Chen, Xin Chen, Kim Davenport, Tharu Fernando, Debbie Gordon, Brian Hamman, Roy Haskell, Alexey Ishchenko, Donald S. Kirkpatrick, Jonathan Maher, Mark Merchant, John Moffat, Alicia Morgan, An Nguyen, Jennifer Pizzano, Connor Quinn, Christopher M. Rose, Emma Rousseau, Vijay Sethuraman, Leanna Staben, Catherine Wilson, Xiaofen Ye, Fabio Broccatelli, Robert Yauch, Peter S. Dragovich
Journal: Cancer Research
Cancer Res (2020) 80 (16_Supplement): 5687.
https://doi.org/10.1158/1538-7445.AM2020-5687
Published: 15 August 2020
View article titled, Abstract 5687: Selective, chemically-induced degradation of BRM (<em>SMARCA2</em>) enables <em>in vivo</em> efficacy in BRG1 (<em>SMARCA4</em>)-deficient xenograft tumor models
Journal Articles

IRE1α Disruption in Triple-Negative Breast Cancer Cooperates with Antiangiogenic Therapy by Reversing ER Stress Adaptation and Remodeling the Tumor Microenvironment

Jonathan M. Harnoss, Adrien Le Thomas, Mike Reichelt, Ofer Guttman, Thomas D. Wu, Scot A. Marsters, Anna Shemorry, David A. Lawrence, David Kan, Ehud Segal, Mark Merchant, Klara Totpal, Lisa M. Crocker, Kathryn Mesh, Monika Dohse, Margaret Solon, Zora Modrusan, Joachim Rudolph, Hartmut Koeppen, Peter Walter, Avi Ashkenazi
Journal: Cancer Research
Series: Author Choice
Cancer Res (2020) 80 (11): 2368–2379.
https://doi.org/10.1158/0008-5472.CAN-19-3108
Published: 02 June 2020
View article titled, IRE1α Disruption in Triple-Negative Breast Cancer Cooperates with Antiangiogenic Therapy by Reversing ER Stress Adaptation and Remodeling the Tumor Microenvironment
Open the PDF for IRE1α Disruption in Triple-Negative Breast Cancer Cooperates with Antiangiogenic Therapy by Reversing ER Stress Adaptation and Remodeling the Tumor Microenvironment in another window
Includes: Supplementary data
Journal Articles

ERBB3 and IGF1R Signaling Are Required for Nrf2-Dependent Growth in KEAP1-Mutant Lung Cancer

Steffan Vartanian, James Lee, Christiaan Klijn, Florian Gnad, Maria Bagniewska, Gabriele Schaefer, Donglu Zhang, Jenille Tan, Sara A. Watson, Liling Liu, Honglin Chen, Yuxin Liang, Colin Watanabe, Trinna Cuellar, David Kan, Ryan J. Hartmaier, Ted Lau, Michael R. Costa, Scott E. Martin, Mark Merchant, Benjamin Haley, David Stokoe
Journal: Cancer Research
Cancer Res (2019) 79 (19): 4828–4839.
https://doi.org/10.1158/0008-5472.CAN-18-2086
Published: 01 October 2019
View article titled, ERBB3 and IGF1R Signaling Are Required for Nrf2-Dependent Growth in KEAP1-Mutant Lung Cancer
Open the PDF for ERBB3 and IGF1R Signaling Are Required for Nrf2-Dependent Growth in KEAP1-Mutant Lung Cancer in another window
Includes: Supplementary data
Journal Articles

Abstract 3894: Determination of the efficacious Entrectinib exposures required for pathway inhibition and anti-tumor activity in a subcutaneous and intracranialTPM3-NTRK1mutant tumor model

Cecile C. de la Cruz, Thomas Hunsaker, Faye Vazvaei, Dragomir Draganov, Li Yu, Mark Merchant
Journal: Cancer Research
Cancer Res (2019) 79 (13_Supplement): 3894.
https://doi.org/10.1158/1538-7445.AM2019-3894
Published: 01 July 2019
View article titled, Abstract 3894: Determination of the efficacious Entrectinib exposures required for pathway inhibition and anti-tumor activity in a subcutaneous and intracranial<em>TPM3-NTRK1</em>mutant tumor model
Journal Articles

Abstract 1483: Targeting oncogenic enhancer activity with a small-molecule CBP/P300 bromodomain inhibitor

Ryan Raisner, Russell Bainer, Emily Chan, Jesse Garcia, Mark Merchant, Karen Gascoigne
Journal: Cancer Research
Cancer Res (2018) 78 (13_Supplement): 1483.
https://doi.org/10.1158/1538-7445.AM2018-1483
Published: 01 July 2018
View article titled, Abstract 1483: Targeting oncogenic enhancer activity with a small-molecule CBP/P300 bromodomain inhibitor
Journal Articles

Abstract 874: Pharmacologically induced RAS-GTP levels and CRAF-BRAF hetero-dimerization drive sensitization to Type II pan-RAF inhibitors in KRAS mutant cancer

Christiaan N. Klijn, Ivana Yen, Frances Shanahan, Mark Merchant, Christine Orr, Thomas Hunsaker, Matthew Durk, Hank La, Xiaoling Zhang, Scott Martin, Eva Lin, John Chan, Yihong Yu, Dhara Amin, Amy Gustafson, Scott Foster, Joachim Rudolph, Shiva Malek
Journal: Cancer Research
Cancer Res (2018) 78 (13_Supplement): 874.
https://doi.org/10.1158/1538-7445.AM2018-874
Published: 01 July 2018
View article titled, Abstract 874: Pharmacologically induced RAS-GTP levels and CRAF-BRAF hetero-dimerization drive sensitization to Type II pan-RAF inhibitors in KRAS mutant cancer
Journal Articles

Therapeutic Targeting of the CBP/p300 Bromodomain Blocks the Growth of Castration-Resistant Prostate Cancer

Lingyan Jin, Jesse Garcia, Emily Chan, Cecile de la Cruz, Ehud Segal, Mark Merchant, Samir Kharbanda, Ryan Raisner, Peter M. Haverty, Zora Modrusan, Justin Ly, Edna Choo, Susan Kaufman, Maureen H. Beresini, F. Anthony Romero, Steven Magnuson, Karen E. Gascoigne
Journal: Cancer Research
Series: Author Choice
Cancer Res (2017) 77 (20): 5564–5575.
https://doi.org/10.1158/0008-5472.CAN-17-0314
Published: 15 October 2017
View article titled, Therapeutic Targeting of the CBP/p300 Bromodomain Blocks the Growth of Castration-Resistant Prostate Cancer
Open the PDF for Therapeutic Targeting of the CBP/p300 Bromodomain Blocks the Growth of Castration-Resistant Prostate Cancer in another window
Includes: Supplementary data
Journal Articles

Abstract 4967: RAF kinase inhibition synergizes with MEK inhibitors in KRAS mutant tumors

Ivana Yen, Christiaan Klijn, Frances Shanahan, Mark Merchant, Christine Orr, Thomas Hunsaker, Matthew Durk, Hank La, Xiaolin Zhang, Scott Martin, Eva Lin, John Chan, Yihong Yu, Amy Gustafson, Joachim Rudolph, Shiva Malek
Journal: Cancer Research
Cancer Res (2017) 77 (13_Supplement): 4967.
https://doi.org/10.1158/1538-7445.AM2017-4967
Published: 01 July 2017
View article titled, Abstract 4967: RAF kinase inhibition synergizes with MEK inhibitors in KRAS mutant tumors
Journal Articles

Abstract 4905: Effects of MAPK pathway inhibitors in the tumor immune microenvironment

Marcia P. Belvin, Erin Williams, Shiuh-Ming Luoh, Jeanne Cheung, Christine Orr, Emily Chan, Peter Ebert, Ira Mellman, Jeong Kim, Mark Merchant
Journal: Cancer Research
Cancer Res (2016) 76 (14_Supplement): 4905.
https://doi.org/10.1158/1538-7445.AM2016-4905
Published: 15 July 2016
View article titled, Abstract 4905: Effects of MAPK pathway inhibitors in the tumor immune microenvironment
Journal Articles

Abstract 392: Combined targeting of MET and PI3K improves efficacy in breast cancer models with concurrent MET/PI3K aberrations

Shuying Liu, Naoto T. Ueno, Bailiang Wang, Mihai Gagea, Prahlad T. Ram, Mark Merchant, John Mendelsohn, Debasish Tripathy, Gordon B. Mills, Ana M. Gonzalez-Angulo
Journal: Cancer Research
Cancer Res (2016) 76 (14_Supplement): 392.
https://doi.org/10.1158/1538-7445.AM2016-392
Published: 15 July 2016
View article titled, Abstract 392: Combined targeting of MET and PI3K improves efficacy in breast cancer models with concurrent MET/PI3K aberrations
Journal Articles

Abstract 417: A novel predictive biomarker model for MEK sensitivity

Marie Wagle, Christiaan Klijn, Bonnie Liu, Shilpi Mahajan, Peter Haverty, John Moffat, Mark Merchant, Bob Yauch, Garret Hampton, Lukas Amler, Mark Lackner, Shih-Min A. Huang
Journal: Cancer Research
Cancer Res (2016) 76 (14_Supplement): 417.
https://doi.org/10.1158/1538-7445.AM2016-417
Published: 15 July 2016
View article titled, Abstract 417: A novel predictive biomarker model for MEK sensitivity
Journal Articles

Abstract 1430: Identification of distinct metabolic subtypes within pancreatic ductal adenocarcinoma through broad metabolite profiling

Anneleen Daemen, David Peterson, Nisebita Sahu, Ron McCord, Kaska Kowanetz, Anna Hitz, Xiangnan Du, Bonnie Liu, Min Gao, John Moffat, Rebecca Hong, Deepak Sampath, Mark Merchant, Thomas O'Brien, Bob Yauch, Jeff Settleman, Jing Qing, Georgia Hatzivassiliou, Marie A. Evangelista
Journal: Cancer Research
Cancer Res (2014) 74 (19_Supplement): 1430.
https://doi.org/10.1158/1538-7445.AM2014-1430
Published: 01 October 2014
View article titled, Abstract 1430: Identification of distinct metabolic subtypes within pancreatic ductal adenocarcinoma through broad metabolite profiling
Journal Articles

Abstract DDT02-03: Discovery of GDC-0994, a potent and selective ERK1/2 inhibitor in early clinical development

Kirk Robarge, Jacob Schwarz, Jim Blake, Michael Burkard, Jocelyn Chan, Huifen Chen, Kang-Jye Chou, Dolores Diaz, John Gaudino, Stephen Gould, Jonas Grina, Xin Linghu, Lichuan Liu, Matthew Martinson, David A. Moreno, Christine Orr, Patricia Pacheco, Ann Qin, Kevin Rasor, Li Ren, Sheerin Shahidi-Latham, Jeffrey Stults, Francis Sullivan, Weiru Wang, Peter Yin, Aihe Zhou, Marcia Belvin, Mark Merchant, John G. Moffat
Journal: Cancer Research
Cancer Res (2014) 74 (19_Supplement): DDT02-03.
https://doi.org/10.1158/1538-7445.AM2014-DDT02-03
Published: 01 October 2014
View article titled, Abstract DDT02-03: Discovery of GDC-0994, a potent and selective ERK1/2 inhibitor in early clinical development
Journal Articles

The Cancer Stem Cell Marker Aldehyde Dehydrogenase Is Required to Maintain a Drug-Tolerant Tumor Cell Subpopulation

Debasish Raha, Timothy R. Wilson, Jing Peng, David Peterson, Peng Yue, Marie Evangelista, Catherine Wilson, Mark Merchant, Jeff Settleman
Journal: Cancer Research
Cancer Res (2014) 74 (13): 3579–3590.
https://doi.org/10.1158/0008-5472.CAN-13-3456
Published: 30 June 2014
View article titled, The Cancer Stem Cell Marker Aldehyde Dehydrogenase Is Required to Maintain a Drug-Tolerant Tumor Cell Subpopulation
Open the PDF for The Cancer Stem Cell Marker Aldehyde Dehydrogenase Is Required to Maintain a Drug-Tolerant Tumor Cell Subpopulation in another window
Includes: Supplementary data
Journal Articles

A Novel Tankyrase Small-Molecule Inhibitor Suppresses APC Mutation–Driven Colorectal Tumor Growth

Ted Lau, Emily Chan, Marinella Callow, Jo Waaler, Jason Boggs, Robert A. Blake, Steven Magnuson, Amy Sambrone, Melissa Schutten, Ron Firestein, Ondrej Machon, Vladimir Korinek, Edna Choo, Dolores Diaz, Mark Merchant, Paul Polakis, Daniel D. Holsworth, Stefan Krauss, Mike Costa
Journal: Cancer Research
Series: Author Choice
Cancer Res (2013) 73 (10): 3132–3144.
https://doi.org/10.1158/0008-5472.CAN-12-4562
Published: 12 May 2013
View article titled, A Novel Tankyrase Small-Molecule Inhibitor Suppresses <em>APC</em> Mutation–Driven Colorectal Tumor Growth
Open the PDF for A Novel Tankyrase Small-Molecule Inhibitor Suppresses <em>APC</em> Mutation–Driven Colorectal Tumor Growth in another window
Includes: Supplementary data
Journal Articles

Abstract 2340: Preferential targeting of KRAS mutant or BRAF mutant tumors using MEK inhibitors with distinct mechanisms of action.

Georgia Hatzivassiliou, Jacob Haling, Huifen Chen, Kyung Song, Shiuh-Ming Luoh, Steve Price, Robert Heald, Mark Zak, Mark Merchant, Klaus Hoeflich, Lori Friedman, Shiva Malek, Marcia P. Belvin
Journal: Cancer Research
Cancer Res (2013) 73 (8_Supplement): 2340.
https://doi.org/10.1158/1538-7445.AM2013-2340
Published: 15 April 2013
View article titled, Abstract 2340: Preferential targeting of KRAS mutant or BRAF mutant tumors using MEK inhibitors with distinct mechanisms of action.
Journal Articles

Abstract 2335: Structure of the anti-MET antibody, onartuzumab (MetMAb) with MET demonstrates the primary mechanism of action is inhibition of hepatocyte growth factor (HGF) α-chain binding.

Henry R. Maun, Xiaolei Ma, Mark Merchant, Robert A. Lazarus, Melissa A. Starovasnik
Journal: Cancer Research
Cancer Res (2013) 73 (8_Supplement): 2335.
https://doi.org/10.1158/1538-7445.AM2013-2335
Published: 15 April 2013
View article titled, Abstract 2335: Structure of the anti-MET antibody, onartuzumab (MetMAb) with MET demonstrates the primary mechanism of action is inhibition of hepatocyte growth factor (HGF) α-chain binding.