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Poster Presentations - Epigenetic Agents
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Journal Articles

Abstract 5080: BET inhibitors INCB054329 and INCB057643 display significant activity in androgen-independent prostate cancer models

Ramiro Vázquez, Gianluca Civenni, Martina Marchetti, Sabrina Zadic, Phillip Liu, Bruce Ruggeri, Giuseppina M. Carbone, Carlo V. Catapano
Journal: Cancer Research
Cancer Res (2017) 77 (13_Supplement): 5080.
DOI: https://doi.org/10.1158/1538-7445.AM2017-5080
Published: 01 July 2017
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Journal Articles

Abstract 5064: Identifying novel potential epigenetic anti-cancer drugs from natural compounds using a phenotypic-based screening

Hanghang Zhang, Noël J.-M Raynal, Takahiro Sato, Yasuyuki Okamoto, Judith Garriga, Benjamin Garcia, George Morton, Wayne Childers, Marlene A. Jacobson, Stephen B. Baylin, Xavier Graña, Magid Abou-Gharbia, Jean-Pierre J. Issa
Journal: Cancer Research
Cancer Res (2017) 77 (13_Supplement): 5064.
DOI: https://doi.org/10.1158/1538-7445.AM2017-5064
Published: 01 July 2017
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Journal Articles

Abstract 5063: Epigenetic modulators show differential activity on lung adenocarcinoma cells with loss-of-function mutations of SWI/SNF protein SMARCA4

Tomasz Rzymski, Anna Wrobel, Michal Mikula, Karolina Pyziak, Anna Bartosik, Agnieszka Sroka, Agnieszka Paziewska, Aleksandra Grochowska, Malgorzata Statkiewicz, Katarzyna Paczkowska, Michalina Dabrowska, Jerzy Ostrowski, Krzysztof Brzozka
Journal: Cancer Research
Cancer Res (2017) 77 (13_Supplement): 5063.
DOI: https://doi.org/10.1158/1538-7445.AM2017-5063
Published: 01 July 2017
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Journal Articles

Abstract 5083: A novel and highly efficacious small-molecule degrader of BET-BRD proteins for the treatment of acute leukemia

Ester Fernandez-Salas, Zhuo Chen, Mei Lin, Bing Zhou, Donna McEachern, Sally Przybranowski, Karson Kump, Luke F. Peterson, Malathi Kandarpa, Jiantao Hu, Fuming Xu, Liu Liu, Longchuan Bai, Bo Wen, Duxin Sun, Moshe Talpaz, Shaomeng Wang
Journal: Cancer Research
Cancer Res (2017) 77 (13_Supplement): 5083.
DOI: https://doi.org/10.1158/1538-7445.AM2017-5083
Published: 01 July 2017
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Journal Articles

Abstract 5065: Harnessing epigenetic reprogramming by histone deacetylase inhibitor MS275 for pancreatic cancer therapy

Gaoyang Liang, Ruth Yu, Christopher Liddle, Morgan Truitt, Corina Antal, Annette Atkins, Ester Banayo, Michael Downes, Ronald Evans
Journal: Cancer Research
Cancer Res (2017) 77 (13_Supplement): 5065.
DOI: https://doi.org/10.1158/1538-7445.AM2017-5065
Published: 01 July 2017
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Journal Articles

Abstract 5071: Preclinical characterization of the potent and selective BET inhibitor INCB057643 in models of hematologic malignancies

Matthew C. Stubbs, Thomas Maduskuie, Timothy Burn, Sharon Diamond-Fosbenner, Nikoo Falahatpisheh, Alla Volgina, Nina Zolotarjova, Xiaoming Wen, Patricia Feldman, Mark Rupar, Robert Collins, Cindy Marando, Bruce Ruggeri, Maryanne Covington, Xuesong Mike Liu, Richard Wynn, Swamy Yeleswaram, Wenqing Yao, Reid Huber, Gregory Hollis, Peggy Scherle, Andrew P. Combs, Phillip C. Liu
Journal: Cancer Research
Cancer Res (2017) 77 (13_Supplement): 5071.
DOI: https://doi.org/10.1158/1538-7445.AM2017-5071
Published: 01 July 2017
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Journal Articles

Abstract 5067: BET protein proteolysis targeting chimera (BETP-PROTACs) exert more potent activity than BETP bromodomain inhibitor (BETi) against post-myeloproliferative neoplasm (MPN) secondary (s) AML cells

Dyana T. Saenz, Warren C. Fiskus, Kanak Raina, Taghi Manshouri, Kevin G. Coleman, Yimin Qian, Andrew P. Crew, Angela Shen, Christopher P. Mill, Baohua Sun, Misun Kim, Agnieszka J. Nowak, Srdan Verstovsek, Craig M. Crews, Kapil N. Bhalla
Journal: Cancer Research
Cancer Res (2017) 77 (13_Supplement): 5067.
DOI: https://doi.org/10.1158/1538-7445.AM2017-5067
Published: 01 July 2017
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Journal Articles

Abstract 5058: Lysine specific demethylase-1 (LSD-1) Inhibitor SYC-836 in combination with radiation prolongs animal survival in patient-derived posterior fossa ependymoma xenograft mouse models

Sibo Zhao, Huiyuan Zhang, Lin Qi, Holly Lindsay, Yuchen Du, Mari Kogiso, Frank Braun, Sarah Injac, Laszlo Perlaky, Donald W. Parsons, Murali Chintagumpala, Adekunle Adesina, Yongcheng Song, Xiao-Nan Li
Journal: Cancer Research
Cancer Res (2017) 77 (13_Supplement): 5058.
DOI: https://doi.org/10.1158/1538-7445.AM2017-5058
Published: 01 July 2017
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Journal Articles

Abstract 5056: The bromodomain inhibitor JQ1 sensitizes homologous recombination proficient ovarian cancer cells to the PARP inhibitor olaparib

Andrew J. Wilson, Janese Thompson, Abdirahman Osman, Jeanette Saskowski, Dineo Khabele
Journal: Cancer Research
Cancer Res (2017) 77 (13_Supplement): 5056.
DOI: https://doi.org/10.1158/1538-7445.AM2017-5056
Published: 01 July 2017
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Journal Articles

Abstract 5059: Preclinical study on the efficacy of Panobinostat in hepatocellular carcinoma

Chi Tung Choy, Wing Yu Man, Chi Hang Wong, Stephen Lam Chan
Journal: Cancer Research
Cancer Res (2017) 77 (13_Supplement): 5059.
DOI: https://doi.org/10.1158/1538-7445.AM2017-5059
Published: 01 July 2017
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Journal Articles

Abstract 5073: Determination of sensitivity to BET and HDAC inhibitors in lung cancer cell lines

Sara Verdura, Manuel Torres-Diz, Montserrat Sanchez-Cespedes
Journal: Cancer Research
Cancer Res (2017) 77 (13_Supplement): 5073.
DOI: https://doi.org/10.1158/1538-7445.AM2017-5073
Published: 01 July 2017
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Journal Articles

Abstract 5070: Structure-function studies and drug design on the human histone lysine methyltransferases NSD1, NSD2 and NSD3

Eric Di Luccio, Damiaan E.H.F Mevius, Yunpeng Shen, Yeon Jeong Noh, Jihyeon Kim, Masayo Morishita
Journal: Cancer Research
Cancer Res (2017) 77 (13_Supplement): 5070.
DOI: https://doi.org/10.1158/1538-7445.AM2017-5070
Published: 01 July 2017
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Journal Articles

Abstract 5082: The selective bromodomain inhibitor, INCB054329 targets both cancer cells and the tumor microenvironment in the KC inflammatory preclinical model of ductal pancreatic cancer

Ana Sofia Leal, Karen T. Liby, Phillip Liu, Bruce Ruggeri
Journal: Cancer Research
Cancer Res (2017) 77 (13_Supplement): 5082.
DOI: https://doi.org/10.1158/1538-7445.AM2017-5082
Published: 01 July 2017
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Journal Articles

Abstract 5081: Disruption of DNA methyltransferase (DNMT) 1 confers resistance to DNMT inhibitors in human colorectal cancer cells

Angelo B. Laranjeira, Dat Nguyen, Erich Huang, James H. Doroshow, Sherry X. Yang
Journal: Cancer Research
Cancer Res (2017) 77 (13_Supplement): 5081.
DOI: https://doi.org/10.1158/1538-7445.AM2017-5081
Published: 01 July 2017
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Journal Articles

Abstract 5077: A novel small molecule menin-MLL inhibitor for potential treatment of MLL-rearranged leukemias

Tao Wu, Linda Kessler, Shuangwei Li, Trupta Purohit, Shisheng Li, Hongzhi Miao, Brian Linhares, Rasmus Hansen, Jeff Kucharski, Yi Wang, Ke Yu, Katarzyna Kempinska, Tess Ely, Szymon Klossowski, Ata Zarieh, Ulf Peters, Jun Feng, Yvonne Yao, Yuan Liu, Bo Wen, Francis Burrows, Duxin Sun, Jingchuan Zhang, Levan Darjania, Dana Hu-Lowe, Patrick Zarrinkar, Liansheng Li, Tomasz Cierpicki, Jolanta Grembecka, Pingda Ren, Yi Liu
Journal: Cancer Research
Cancer Res (2017) 77 (13_Supplement): 5077.
DOI: https://doi.org/10.1158/1538-7445.AM2017-5077
Published: 01 July 2017
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Journal Articles

Abstract 5074: Therapeutic targeting of bromodomain and extra-terminal proteins degradation in triple-negative breast cancer

Longchuan Bai, Bing Zhou, Chao-Yie Yang, Jiao Ji, Donna McEachern, Sally Przybranowski, Shaomeng Wang
Journal: Cancer Research
Cancer Res (2017) 77 (13_Supplement): 5074.
DOI: https://doi.org/10.1158/1538-7445.AM2017-5074
Published: 01 July 2017
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Journal Articles

Abstract 5069: Inhibition of BET bromodomain, epigenetic regulator, as an effective therapeutic approach for gastric cancer

Sun Kyoung Kang, Tae Soo Kim, Woo Sun Kwon, Jae Kyung Roh, Ho-Yeong Lim, Hyun Cheol Chun, Sun Young Rha
Journal: Cancer Research
Cancer Res (2017) 77 (13_Supplement): 5069.
DOI: https://doi.org/10.1158/1538-7445.AM2017-5069
Published: 01 July 2017
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Journal Articles

Abstract 5075: Phenotypic human tumor cell line profiling and predictive biomarker analysis for epigenetic inhibitors

Usha Warrior, Jesse J. Parry, Samantha C. Burkart, Lee R. Cavedine, Alyssa M. Cracchiolo, Brogan A. Epkins, Steven M. Garner, Timothy J. Sindelar, Charles R. Wageman, Alastair J. King
Journal: Cancer Research
Cancer Res (2017) 77 (13_Supplement): 5075.
DOI: https://doi.org/10.1158/1538-7445.AM2017-5075
Published: 01 July 2017
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Journal Articles

Abstract 5084: Potent and isoform-selective ATAD2 bromodomain inhibitor with unprecedented chemical structure and mode of action

Amaury E. Fernández-Montalván, Markus Berger, Benno Kuropka, Seong Joo Koo, Volker Badock, Joerg Weiske, Simon J. Holton, Apirat Chaikuad, Laura Díaz-Sáez, James Bennett, Oleg Federov, Kilian Huber, Paolo Centrella, Matthew A. Clark, Christoph E. Dumelin, Eric A. Sigel, Holly S. Soutter, Dawn M. Troast, Ying Zhang, John W. Cuozzo, Anthony D. Keefe, Didier Roche, Vincent Rodeschini, Jan Hübner, Hilmar Weinmann, Ingo V. Hartung, Matyas Gorjanacz
Journal: Cancer Research
Cancer Res (2017) 77 (13_Supplement): 5084.
DOI: https://doi.org/10.1158/1538-7445.AM2017-5084
Published: 01 July 2017
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Journal Articles

Abstract 5076: IHC and flow cytometry quantifies BRD4 levels in surrogate tissues after ex-vivo and in-vivo dosing with a BRD4 degrading PROTAC

Sheryl M. Gough, Kanak Raina, Debbie Gordon, Ryan Willard, Martha Altieri, Angela Shen, Yimin Qian, Taavi Neklesa, Kevin Coleman, Ian Taylor
Journal: Cancer Research
Cancer Res (2017) 77 (13_Supplement): 5076.
DOI: https://doi.org/10.1158/1538-7445.AM2017-5076
Published: 01 July 2017
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