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Journal Articles

Abstract 3294: The GSPT1 molecular glue degrader MRT-2359 is active against prostate cancer

Ralph Tiedt, Martin Schillo, Arnaud Osmont, Débora Bonenfant, Rajiv Narayan, Owen Wallace, Markus Warmuth
Journal: Cancer Research
Cancer Res (2024) 84 (6_Supplement): 3294.
https://doi.org/10.1158/1538-7445.AM2024-3294
Published: 22 March 2024
View article titled, Abstract 3294: The GSPT1 molecular glue degrader MRT-2359 is active against prostate cancer
Journal Articles

Abstract ND10: Discovery of MRT-2359, an orally bioavailable GSPT1 molecular glue degrader, for MYC-driven cancers

Owen B. Wallace, Gerald Gavory, Mahmoud Ghandi, Anne-Cecile d’Alessandro, Debora Bonenfant, Maciej Cabanski, Lisa Cantagallo, Agustin Chicas, Qian Chen, Anna Diesslin, Christopher King, Vittoria Massafra, Rajiv Narayan, Arnaud Osmont, Dave Peck, Carolina Perdomo Ortiz, Martin Schillo, Ambika Singh, Ralph Tiedt, Simone Tortoioli, Silvia Buonamici, Markus Warmuth, Filip Janku, Bernhard Fasching
Journal: Cancer Research
Cancer Res (2023) 83 (7_Supplement): ND10.
https://doi.org/10.1158/1538-7445.AM2023-ND10
Published: 29 May 2023
View article titled, Abstract ND10: Discovery of MRT-2359, an orally bioavailable GSPT1 molecular glue degrader, for MYC-driven cancers
Journal Articles

Abstract PS12-23: Development of H3B-6545, a first-in-class oral selective ER covalent antagonist (SERCA), for the treatment of ERaWT and ERaMUT breast cancer

Manav Korpal, Craig Furman, Xiaoling Puyang, Zhaojie Zhang, Zhenhua Wu, Deepti Banka, Subhasree Das, Benoit Destenaves, Lei Gao, Erika Hamilton, Ming-Hong Hao, Sean Irwin, Stephen Johnston, Jaya J Joshi, Dejan Juric, Amy Kim, Tuong-Vi Nguyen, Marc Pipas, Timothy Pluard, Victoria Rimkunas, Nathalie Rioux, Joanne Schindler, Peter Smith, Michael Thomas, John Wang, Judy S Wang, Markus Warmuth, Huilan Yao, Shihua Yao, Lihua Yu, Frédéric H Vaillancourt, David M Bolduc, Nicholas A Larsen, GuoZhu Zheng, Sudeep Prajapati, Tarek Sahmoud, Antonio Gualberto, Ping Zhu
Journal: Cancer Research
Cancer Res (2021) 81 (4_Supplement): PS12-23.
https://doi.org/10.1158/1538-7445.SABCS20-PS12-23
Published: 15 February 2021
View article titled, Abstract PS12-23: Development of H3B-6545, a first-in-class oral selective ER covalent antagonist (SERCA), for the treatment of ERa<sup>WT</sup> and ERa<sup>MUT</sup> breast cancer
Journal Articles

Abstract 281: Sensitivity to splicing modulation of BCL2 family genes reveals cancer therapeutic strategies for splicing modulators

Daniel Aird, Teng Teng, Chia-Ling Huang, Ermira Pazolli, Deepti Banka, Kahlin Cheung-Ong, Cheryl Eifert, Craig Furman, Jeremy Wu, Michael Seiler, Silvia Buonamici, Peter Fekkes, Craig Karr, James Palacino, Eunice Park, Peter Smith, Lihua Yu, Yoshiharu Mizui, Markus Warmuth, Agustin Chicas, Laura Corson, Ping Zhu
Journal: Cancer Research
Cancer Res (2019) 79 (13_Supplement): 281.
https://doi.org/10.1158/1538-7445.AM2019-281
Published: 01 July 2019
View article titled, Abstract 281: Sensitivity to splicing modulation of BCL2 family genes reveals cancer therapeutic strategies for splicing modulators
Journal Articles

Abstract 3406: Comprehensive genomic profiling of hematologic malignancies identifies recurrent somatic splicing factor mutations in non-Hodgkin's lymphoma (NHL) and multiple myeloma (MM)

Lee A. Albacker, Silvia Buonamici, Garrett M. Frampton, Peter Smith, Philip J. Stephens, Markus Warmuth, Ping Zhu, Lihua Yu
Journal: Cancer Research
Cancer Res (2018) 78 (13_Supplement): 3406.
https://doi.org/10.1158/1538-7445.AM2018-3406
Published: 01 July 2018
View article titled, Abstract 3406: Comprehensive genomic profiling of hematologic malignancies identifies recurrent somatic splicing factor mutations in non-Hodgkin's lymphoma (NHL) and multiple myeloma (MM)
Journal Articles

H3B-6527 Is a Potent and Selective Inhibitor of FGFR4 in FGF19-Driven Hepatocellular Carcinoma

Jaya Julie Joshi, Heather Coffey, Erik Corcoran, Jennifer Tsai, Chia-Ling Huang, Kana Ichikawa, Sudeep Prajapati, Ming-Hong Hao, Suzanna Bailey, Jeremy Wu, Victoria Rimkunas, Craig Karr, Vanitha Subramanian, Pavan Kumar, Crystal MacKenzie, Raelene Hurley, Takashi Satoh, Kun Yu, Eunice Park, Nathalie Rioux, Amy Kim, Weidong G. Lai, Lihua Yu, Ping Zhu, Silvia Buonamici, Nicholas Larsen, Peter Fekkes, John Wang, Markus Warmuth, Dominic J. Reynolds, Peter G. Smith, Anand Selvaraj
Journal: Cancer Research
Cancer Res (2017) 77 (24): 6999–7013.
https://doi.org/10.1158/0008-5472.CAN-17-1865
Published: 14 December 2017
View article titled, H3B-6527 Is a Potent and Selective Inhibitor of FGFR4 in FGF19-Driven Hepatocellular Carcinoma
Open the PDF for H3B-6527 Is a Potent and Selective Inhibitor of FGFR4 in FGF19-Driven Hepatocellular Carcinoma in another window
Includes: Supplementary data
Journal Articles

Abstract 126: A chemogenomic approach reveals the action of splicing modulators at the branch point adenosine binding pocket defined by the PHF5A/SF3b complex

Teng Teng, Jennifer Tsai, Xiaoling Puyang, Michael Seiler, Shouyong Peng, Daniel Aird, Silvia Buonamici, Benjamin Caleb, Betty Chan, Laura Corson, Jacob Feala, Peter Fekkes, Craig Karr, Manav Korpal, Yoshiharu Mizui, Eunice Park, James Palacino, Peter Smith, Vanitha Subramanian, Jeremy Wu, Lihua Yu, Agustin Chicas, Markus Warmuth, Nicholas Larsen, Ping Zhu
Journal: Cancer Research
Cancer Res (2017) 77 (13_Supplement): 126.
https://doi.org/10.1158/1538-7445.AM2017-126
Published: 01 July 2017
View article titled, Abstract 126: A chemogenomic approach reveals the action of splicing modulators at the branch point adenosine binding pocket defined by the PHF5A/SF3b complex
Journal Articles

Abstract 2084: Conformational activation and allosteric inhibition of SHP2 in RTK-driven cancers

Michael G. Acker, Ying-Nan P. Chen, Matthew J. LaMarche, Ho Man Chan, Peter Fekkes, Jorge Garcia-Fortanet, Jonathan R. LaRochelle, Brandon Antonakos, Christine Hiu-Tung Chen, Zhuoliang Chen, Vesselina G. Cooke, Jason R. Dobson, Zhan Deng, Fei Feng, Brant Firestone, Michelle Fodor, Cary Fridrich, Hui Gao, Huai-Xiang Hao, Jaison Jacob, Samuel Ho, Kathy Hsiao, Zhao B. Kang, Rajesh Karki, Mitsunori Kato, Jay Larrow, Laura R. La Bonte, Gang Liu, Shumei Liu, Dyuti Majumdar, Matthew J. Meyer, Mark Palermo, Minying Pu, Edmund Price, Subarna Shakya, Michael D. Shultz, Kavitha Venkatesan, Ping Wang, Markus Warmuth, Sarah Williams, Guizhi Yang, Jing Yuan, Ji-Hu Zhang, Ping Zhu, Stephen C. Blacklow, Timothy Ramsey, Nicholas J. Keen, William R. Sellers, Travis Stams, Pascal D. Fortin
Journal: Cancer Research
Cancer Res (2017) 77 (13_Supplement): 2084.
https://doi.org/10.1158/1538-7445.AM2017-2084
Published: 01 July 2017
View article titled, Abstract 2084: Conformational activation and allosteric inhibition of SHP2 in RTK-driven cancers
Journal Articles

Abstract 3126: H3B6527, a selective and potent FGFR4 inhibitor for FGF19-driven hepatocellular carcinoma

Anand Selvaraj, Erik Corcoran, Heather Coffey, Sudeep Prajapati, Ming-Hong Hao, Nicholas Larsen, Jennifer Tsai, Takashi Satoh, Kana Ichikawa, Julie Jaya Joshi, Raelene Hurley, Jeremy Wu, Chia-Ling Huang, Suzanna Bailey, Craig Karr, Pavan Kumar, Victoria Rimkunas, Crystal Mackenzie, Nathalie Rioux, Amy Kim, Sandeep Akare, George Lai, Lihua Yu, Peter Fekkes, John Wang, Markus Warmuth, Peter Smith, Dominic Reynolds
Journal: Cancer Research
Cancer Res (2017) 77 (13_Supplement): 3126.
https://doi.org/10.1158/1538-7445.AM2017-3126
Published: 01 July 2017
View article titled, Abstract 3126: H3B6527, a selective and potent FGFR4 inhibitor for FGF19-driven hepatocellular carcinoma
Journal Articles

Abstract DDT01-04: Discovery and development of H3B-6545: A novel, oral, selective estrogen receptor covalent antagonist (SERCA) for the treatment of breast cancer

Peter G. Smith, Xiaoling Puyang, Craig Furman, Guo Zhu Zheng, Deepti Banka, Michael Thomas, Vanitha Subramanian, Sean Irwin, Nicholas Larsen, Benjamin Caleb, Craig Karr, Jeremy Wu, Morgan O’Shea, Joyce Yang, Allison Davis, Amy Kim, Nathalie Rioux, Victoria Rimkunas, Huilan Yao, Crystal MacKenzie, Pavan Kumar, Sherri Smith, Sean Eckley, Andrew Hart, George Lai, Christopher Rowbottom, Peter Fekkes, Silvia Buonamici, Dominic Reynolds, Lihua Yu, Tarek Sahmoud, Markus Warmuth, Lorna Mitchell, Ping Zhu, Manav Korpal
Journal: Cancer Research
Cancer Res (2017) 77 (13_Supplement): DDT01-04.
https://doi.org/10.1158/1538-7445.AM2017-DDT01-04
Published: 01 July 2017
View article titled, Abstract DDT01-04: Discovery and development of H3B-6545: A novel, oral, selective estrogen receptor covalent antagonist (SERCA) for the treatment of breast cancer
Journal Articles

Abstract 1185: H3B-8800, a novel orally available SF3b modulator, shows preclinical efficacy across spliceosome mutant cancers

Silvia Buonamici, Akihide Yoshimi, Michael Thomas, Michael Seiler, Betty Chan, Benjamin Caleb, Fred Csibi, Rachel Darman, Peter Fekkes, Craig Karr, Gregg Keaney, Amy Kim, Virginia Klimek, Pavan Kumar, Kaiko Kunii, Stanley Chun-Wei Lee, Xiang Liu, Crystal MacKenzie, Carol Meeske, Yoshiharu Mizui, Eric Padron, Eunice Park, Ermira Pazolli, Sudeep Prajapati, Nathalie Rioux, Justin Taylor, John Wang, Markus Warmuth, Huilan Yao, Lihua Yu, Ping Zhu, Omar Abdel-Wahab, Peter Smith
Journal: Cancer Research
Cancer Res (2017) 77 (13_Supplement): 1185.
https://doi.org/10.1158/1538-7445.AM2017-1185
Published: 01 July 2017
View article titled, Abstract 1185: H3B-8800, a novel orally available SF3b modulator, shows preclinical efficacy across spliceosome mutant cancers
Journal Articles

Abstract 3013: Identification of PHF5A as a common cellular target of splicing-modulating chemical probes

Teng Teng, Xiaoling Puyang, Shouyong Peng, Jacob Feala, Betty Chan, Jennifer Tsai, Benjamin Caleb, Craig Karr, Eunice Park, Laura Corson, Yoshiharu Mizui, Peter Smith, Nicholas Larsen, Lihua Yu, Markus Warmuth, Ping Zhu, Agustin Chicas
Journal: Cancer Research
Cancer Res (2016) 76 (14_Supplement): 3013.
https://doi.org/10.1158/1538-7445.AM2016-3013
Published: 15 July 2016
View article titled, Abstract 3013: Identification of PHF5A as a common cellular target of splicing-modulating chemical probes
Journal Articles

Abstract 5564: Total synthesis of 6-deoxypladienolide D and assessment of splicing inhibitory activity in a mutant SF3B1 cancer cell line

Kenzo Arai, Silvia Buonamici, Betty Chan, Laura Corson, Atsushi Endo, Baudouin Gerard, Ming-Hong Hao, Craig Karr, Kazunobu Kira, Linda Lee, Xiang Liu, Jason T. Lowe, Tuoping Luo, Lisa A. Marcaurelle, Yoshiharu Mizui, Marta Nevalainen, Morgan Welzel O'Shea, Eun Sun Park, Samantha A. Perino, Sudeep Prajapati, Mingde Shan, Peter G. Smith, Parcharee Tivitmahaisoon, John Yuan Wang, Markus Warmuth, Kuo-Ming Wu, Lihua Yu, Huiming Zhang, Guo Zhu Zheng, Gregg F. Keaney
Journal: Cancer Research
Cancer Res (2015) 75 (15_Supplement): 5564.
https://doi.org/10.1158/1538-7445.AM2015-5564
Published: 01 August 2015
View article titled, Abstract 5564: Total synthesis of 6-deoxypladienolide D and assessment of splicing inhibitory activity in a mutant SF3B1 cancer cell line
Journal Articles

Abstract 2941: Targeting MCL1-dependent cancers through RNA splicing modulation

Eun Sun Park, Michelle Aicher, Daniel Aird, Silvia Buonamici, Betty Chan, Cheryl Eifert, Peter Fekkes, Craig Furman, Baudouin Gerard, Craig Karr, Gregg Keaney, Kaiko Kunii, Linda Lee, Ermira Pazolli, Sudeep Prajapati, Takashi Satoh, Peter Smith, John Yuan Wang, Karen Wang, Markus Warmuth, Lihua Yu, Ping Zhu, Yoshiharu Mizui, Laura B. Corson
Journal: Cancer Research
Cancer Res (2015) 75 (15_Supplement): 2941.
https://doi.org/10.1158/1538-7445.AM2015-2941
Published: 01 August 2015
View article titled, Abstract 2941: Targeting MCL1-dependent cancers through RNA splicing modulation
Journal Articles

Abstract 2040: Mutations in SF3B1 lead to aberrant splicing through cryptic 3′ splice site selection and impair hematopoietic cell differentiation

Silvia Buonamici, Samantha Perino, Kian Huat Lim, Jacob Feala, Rachel Darman, Esther Obeng, Richard R. Furman, Suzanna Bailey, Gregg Keaney, Pavan Kumar, Yoshiharu Mizui, Eunice Park, John Wang, Markus Warmuth, Lihua Yu, Ping Zhu, Benjamin L. Ebert, Peter Smith
Journal: Cancer Research
Cancer Res (2015) 75 (15_Supplement): 2040.
https://doi.org/10.1158/1538-7445.AM2015-2040
Published: 01 August 2015
View article titled, Abstract 2040: Mutations in SF3B1 lead to aberrant splicing through cryptic 3′ splice site selection and impair hematopoietic cell differentiation
Journal Articles

Abstract 2932: SF3B1 mutations induce aberrant mRNA splicing in cancer and confer sensitivity to spliceosome inhibition

Silvia Buonamici, Kian Huat Lim, Jacob Feala, Eunice Park, Laura Corson, Michelle Aicher, Daniel Aird, Betty Chan, Erik Corcoran, Rachel Darman, Peter Fekkes, Gregg Keaney, Pavan Kumar, Kaiko Kunii, Linda Lee, Xiaoling Puyang, Jose Rodrigues, Anand Selvaraj, Michael Thomas, John Wang, Markus Warmuth, Lihua Yu, Ping Zhu, Peter Smith, Yoshiharu Mizui
Journal: Cancer Research
Cancer Res (2014) 74 (19_Supplement): 2932.
https://doi.org/10.1158/1538-7445.AM2014-2932
Published: 01 October 2014
View article titled, Abstract 2932: SF3B1 mutations induce aberrant mRNA splicing in cancer and confer sensitivity to spliceosome inhibition
Journal Articles

Abstract 1191: Translational Proof-of-Concept (TransPoC), a not-for-profit research organization enabling access to large-scale translational oncology platforms: The Patient-Derived Xenograft network

Peter G. Smith, David Sutton, Andrea Bertotti, Livio Trusolino, Susan Airhart, Ming S. Tsao, Bradly G. Wouters, S. Gail Eckhardt, Lai Wang, Tim Heffernan, David Verbel, Andrea Gerken, Peter Fekkes, Lihua Yu, Lihua Yu, Markus Warmuth
Journal: Cancer Research
Cancer Res (2014) 74 (19_Supplement): 1191.
https://doi.org/10.1158/1538-7445.AM2014-1191
Published: 01 October 2014
View article titled, Abstract 1191: Translational Proof-of-Concept (TransPoC), a not-for-profit research organization enabling access to large-scale translational oncology platforms: The Patient-Derived Xenograft network
Journal Articles

Abstract 4269: Exome sequencing of tumor cell lines: Optimizing for cancer variants

Alex H. Ramos, Ruibang Luo, Jacob Feala, Binghang Liu, Lara Gong, Markus Warmuth, Ping Zhu, Peter Smith, Lihua Yu
Journal: Cancer Research
Cancer Res (2014) 74 (19_Supplement): 4269.
https://doi.org/10.1158/1538-7445.AM2014-4269
Published: 01 October 2014
View article titled, Abstract 4269: Exome sequencing of tumor cell lines: Optimizing for cancer variants
Journal Articles

Abstract 5455: Integrative analysis of the Cancer Cell Line Encyclopedia reveals genetic and transcriptional predictors of compound sensitivity

Jordi Barretina, Nicolas Stransky, Giordano Caponigro, Sungjoon Kim, Adam Margolin, Kavitha Venkhatesan, Gregory Kryukov, Michael Berger, John Monahan, Paula Morais, Jodi Meltzer, Scott Mahan, Dmitriy Sonkin, Pichai Raman, Michael Jones, Vic Meyer, Christopher Wilson, Joseph Thibault, Lauren Murray, Adam Callahan, John Che, Aaron Shipway, Nanxin Li, Ingo Engels, Andrew Su, Reid Pinchback, Jared Nedzel, Ted Liefeld, Lili Niu, Charles Hatton, Emanuele Palescandolo, Supriya Gupta, Robert Onofrio, Carrie Sougnez, Laura MacConaill, Wendy Winckler, Michael Reich, Jill Mesirov, Kristin Ardlie, Gad Getz, Michael Morrissey, Markus Warmuth, Matthew Meyerson, Peter Finan, Todd Golub, Barbara Weber, Jennifer Harris, William Sellers, Robert Schlegel, Levi Garraway
Journal: Cancer Research
Cancer Res (2011) 71 (8_Supplement): 5455.
https://doi.org/10.1158/1538-7445.AM2011-5455
Published: 15 April 2011
View article titled, Abstract 5455: Integrative analysis of the Cancer Cell Line Encyclopedia reveals genetic and transcriptional predictors of compound sensitivity
Journal Articles

Abstract 923: Separating the wheat from the chaff: A first look at the Cancer Cell Lines Encyclopedia sequencing data

Gregory V. Kryukov, Michael F. Berger, Nicolas Stransky, Jordi Barretina, Robert Onofrio, Giordano Caponigro, Carrie Sougnez, John Monahan, Erica Shefler, Kavitha Venkhatesan, Kristian Cibulskis, Paula Morais, Andrey Sivachenko, Jodi Meltzer, Michael Lawrence, Alex Ramos, Gad Getz, Broad's Genome Sequencing Platform, Joseph Thibault, Scott Mahan, Michael Jones, Michael Morrissey, Dmitry Sonkin, Kristin G. Ardlie, Todd Golub, Barbara Weber, Markus Warmuth, William Sellers, Jennifer Harris, Robert Schlegel, Levi A. Garraway
Journal: Cancer Research
Cancer Res (2011) 71 (8_Supplement): 923.
https://doi.org/10.1158/1538-7445.AM2011-923
Published: 15 April 2011
View article titled, Abstract 923: Separating the wheat from the chaff: A first look at the Cancer Cell Lines Encyclopedia sequencing data