Epigenetic Modulators 1

• 4482 Catalytic inhibition of NSD2 demonstrates in vitro antitumor activity in head and neck squamous cell carcinoma Amr Ismail, Iuliia Topchu, Tingting Zhang, Ahmed Ismail, Peter Makhov, Jia Xu, Kang Le, Michael Soth, Yanis Boumber
• 4483 · PDF The KAT6/7 inhibitor IDE574 disrupts tumor lineage identity and drug tolerance to deliver robust antitumor activity in biomarker selected indications Manav Gupta, Scott R. Tyler, Nour Ghaddar, Carl Schultz, Pranav Gupta, Steven L. Spivak, Katelyn N. Lukas, Zabrisky Roland, Anjali Bisaria, Mona Khalaj, Mason Appel, Oscar Aubi, Kelly S. Trego, Parker Y. Jameson, Jacob Burch-Konda, Angelica Gonzalez-Sanchez, Brittany Cruzan, Rushika Pandya, Jay Prakash Jain, Michael E. Dalziel, Julie Deichert, Sunjay Sethi, Ivan G. Shabalin, Jonathon S. Ryan, Daniel M. Walden, Muzaffar Alam, Daniel Severance, Amber C. Donahue, Edward Chan, Rebeca Choy, Diana M. Muñoz, Richard Zang, Xin Linghu, Peter Teriete, Christian R. Frey, Yuchen Bai, Claire L. Neilan, Josh Taygerly, Paul A. Barsanti, Michael A. White, Brian T. Jones
• 4484 · PDF Characterization and pre-clinical development of LG-CBP/p300 inhibitor, a potent and selective bromodomain inhibitor of CBP/p300 Sinae Lee, Yuna Chang, Ik Sun Kim, Sung Woong Jang, Rira Kim, Gyungah Pak, Bitna Oh, Byung Gyu Kim, Sugyeong Woo
• 4485 · PDF ASTU-045, a novel METTL3 inhibitor with anti-tumor activity in the MC38 syngeneic mouse model Laurence Mévellec, Nicolas George, Ludovic Waeckel, Rémi Longuespée, Nathalie Weidner, Hugues Prevet, Céline Ronin, Jean-Michel Linget, Anna Bonhoure, Roland Blanqué, Sabine Gratzer
• 4486 · PDF The MTA-cooperative PRMT5 inhibitor CTS3497 alone and in synergy with mechanism-based combination targeted therapies for the treatment of MTAP -deleted cancers Yilin Liu, Xinyue Duan, Hui Shi, Qiugeng Ouyang, Jiaxin Huang, Meng Wang, Xingnian Fu, Yiqin Wang, Guoliang Xu, Haiping Wu
• 4487 · PDF CTS2190, a first-in-class PRMT1 inhibitor in phase I/II clinical development, demonstrates robust and broad monotherapy efficacy and provides a rationale for novel combinations based on translational findings​ Hui Shi, Qiugeng Ouyang, Jiaxin Huang, Xingnian Fu, Guoliang Xu, Haiping Wu
• 4488 · PDF Targeting non-canonical PRC2 functions via small-molecule degradation: A novel therapeutic strategy for prostate cancer and other solid tumors Hui Shi, Xinyue Duan, Jiaxin Huang, Qiugeng Ouyang, Xingnian Fu, Guoliang Xu, Haiping Wu
• 4489 · PDF CAAP1 loss uncovers vulnerability of MTAP-deficient NSCLC to PRMT5 inhibition with AZD3470 Jelena Urosevic, Angelos Papadopoulos, Shaun Moore, Ted Hong, Valentina Quarantotti, Harriet Southgate, Maximilian Wechsung, Lukasz Magiera, Daniel Barrell, Grainne Gernon, Elissavet Kentepozidou, Laura Rosenberg, Anisha Solanki, James T. Lynch, Stephen Fawell, Ho Man Chan, Susan Critchlow, Emma Dean
• 4490 · PDF PRMT5 inhibition alters cellular chromatin landscape and drives vulnerability to BH3 mimetics in mantle cell lymphoma Christoph Weigel, Claire Hinterschied, Shirsha Koirala, Mackenzie Long, Shelby Sloan, Jessica Weist, Lynda Villagomez, Allesandro La Ferlita, Coinne Gao, Ian Hout, Sydney Leon, Fiona Brown-Burke, Betsy Pray, Maggie Harper, Neha Bhagwat, Kris Vaddi, Peggy A. Scherle, Cem Meydan, Selina Chen-Kiang, Maurizio DiLiberto, Olivier Elemento, Christopher E. Mason, Jihye Paik, Lapo Alinari, Rosa Lapalombella, Lalit Sehgal, Robert Baiocchi
• 4491 · PDF HDAC inhibitors induce NOX5 expression in human uveal melanoma cells in a Brd4-Sp1/Sp3-dependent manner Smitha Antony, Ballachanda N. Devaiah, Mariam M. Konaté, Yongzhong Wu, Guojian Jiang, Jennifer L. Meitzler, Jiamo Lu, Becky A. Diebold, David J. Mallick, Krishnendu K. Roy, Dinah S. Singer, James H. Doroshow
• 4492 · PDF Linking VHL and SETD2 in a common oncogenic pathway that converges on the mitotic spindle Manga Motrapu, Pratim Chowdhury, Sung Yun Jung, Xiaoli Wang, Ashley Boice, Ruhee Dere
• 4493 · PDF Comprehensive assay approaches for PRMT5 targeted drug discovery Jianghong Wu, Charles Schmidt, Jamin Steffen, Joseph J. Ferry, Li Liang, Shawn McGinley, Joshua Rettew, Yong Wan, Haiching Ma
• 4494 · PDF A highly selective KAT6/7 dual inhibitor with best-in-class potential and favorable pharmacokinetic profile Yang Yang, Xin Nie, Zhen Mi, Yin Guo, Yinyin Zhang, Yong Peng, Lei Zhang
• 4495 · PDF TACC3 inhibition with KC1101 drives mitotic catastrophe and broad antitumor activity Lei Zhang, Xin Nie, Zhen Mi, Yin Guo, Xiaona Yang, Yinyin Zhang, Huaying Wang, Bingqian Li, Yong Peng, Yang Yang
• 4496 · PDF Imofinostat, a histone deacetylase inhibitor, enhances anti-tumoral activity on colorectal cancer with an immune checkpoint inhibitor Chung-Yen Li, Chin-Wen Wei, Ka-Po Tse, Shih-Han Huang, Tzu-Hsien Yang, Meng-Chieh Lin, Chien-Ting Lin, Sue-Ming Chang, Mark Shiuh-Sheng Horng, John Tsu-An Hsu, Kien Thiam Tan
• 4497 · PDF Imofinostat enhances chemotherapy response by targeting HDAC3-NRF2 pathway in KRAS-mutant pancreatic cancer Yi-Chen Lin, Ka-Po Tse, Chung-Yen Li, Tzu-Hsien Yang, Shih-Han Huang, Sue-Ming Chang, Mark Shiuh-Sheng Horng, John Tsu-An Hsu, Kien Thiam Tan
• 4498 · PDF Discovery of novel SMARCA2 small molecule inhibitors with best-in-class potency and selectivity for the treatment of SMARCA4-mutant cancers Lijs Beke, Sandrine Grosse, Shaun Martin, Godelieve Lammens, Pieter Peeters, Bart Stoops, Sandrine Vendeville, Stéphane De Cesco, Kenneth Goossens, Sara Musch, David Moreno Delgado, Line Oste, Pierre Raboisson, Francois Gonzalvez
• 4499 · PDF KAT6i prifetrastat combines with PI3K pathway inhibitors to drive superior efficacy in preclinical models of PIK3CA mutated ER+ BC Kamakoti Prakash Bhat, Joan Q. Cao, Christopher Beldon Proffitt, Jelena Petrovic, Xinmeng Jasmine Mu, Kyle Spinler, Colin Ashton Flaveny, Thomas A. Paul, Joal Garrido Mayor, Heather Neumann, Shikhar Sharma
• 4500 · PDF Embryonic ectoderm development (EED) inhibitor APG-5918 synergizes with topoisomerase I inhibitors in preclinical small-cell lung cancer (SCLC) models through epigenetic priming of chemosensitivity Yan Yin, Zhiyan Liang, Baisong Li, Zhou Yu, Daojie Liu, Dajun Yang, Yifan Zhai
• 4501 Targeting the epigenetic adaptor protein menin in multiple myeloma Emily Gruber, Sree Kumar, Rheana Franich, Tiffany Khong, Daniel Neville, Andrew Spencer, Omer Gilan, Lev Kats
• 4502 · PDF Expanding the PRISM platform: Addition of new hematologic models and a 10-day assay improve drug sensitivity mapping for epigenetic targets Colleen T. Harrington, Antonella Masciotti, Ursula Widocki, Laura Doherty, Tenzin Sangpo, Li Wang, Mustafa Kocak, Anthony Fazio, Aydin Golabi, Rachael Barry, Emily Reeves, John Davis, Melissa Ronan, Matthew G. Rees, Jennifer A. Roth
• 4503 · PDF RCZY-843: A potential best-in-class, second-generation menin-MLL inhibitor engineered to overcome clinically observed menin-mutation-mediated resistance, with superior preclinical efficacy and safety in acute leukemia models Xiaojing (Celia) Chen, Zhengyong Wan, Xiaohong Liu, Qiaoni You, Shenjun Li, Ling Wang, Shanshan Bi, Jing Jiang, Jianming Bao
• 4504 · PDF Synergistic antitumor activity of the MTA-cooperative PRMT5 inhibitor ABSK131 in combination with multiple therapeutic agents in diverse cancer models Bin Shen, Qianqian Chen, Xiao Chen, Jie Wang, Jie Zhang, Manqi Liu, Hongping Yu, Nannan Zhang
• 4505 · PDF IDE892 is a highly potent and selective PRMT5 inhibitor, with MTA-positive and SAM-negative cooperativity, optimized for development in MTAPdel cancers in combination with the allosteric MAT2A inhibitor IDE397 Arjun A. Rao, Marcus M. Fischer, Rebeca M. Choy, Angelica M. Gonzalez-Sanchez, Natalie Bresnahan, Zhipeng Fang, Mason J. Appel, Atul Rathore, Oscar Aubi, Shannon Faris, Parker Y. Jameson, Zabrisky Roland, David Trinh, Kelly Trego, John Vivian, Michael E. Dalziel, Christian R. Frey, Yuchen Bai, Jasgit Sachdev, Claire L. Neilan, Jay Prakash Jain, Michael A. White, Paul A. Barsanti, Peter Teriete, Melissa Fleury
• 4506 · PDF H11 is a first-in-class bifunctional HDAC and autophagy inhibitor with potent antileukemic activity Natalie L. Hakim, Claudia M. Espitia, Sruthi Sureshkumar, Madison Gamble, Bi Fangchao, Wei Wang, Kevin Kelly, Jennifer S. Carew, Steffan T. Nawrocki

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