Epigenetic Modulators 1

• 4482 4482 NSD2的催化抑制在头颈鳞状细胞癌中显示出体外抗肿瘤活性 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 KAT6/7抑制剂IDE574破坏肿瘤谱系身份和耐药性，在生物标志物选择的适应症中提供强效抗肿瘤活性 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 LG-CBP/p300抑制剂——一种强效且选择性的CBP/p300溴结构域抑制剂的表征与临床前开发 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-045，一种在MC38同基因小鼠模型中具有抗肿瘤活性的新型METTL3抑制剂 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 MTA协同性PRMT5抑制剂CTS3497单药及与基于机制的联合靶向疗法协同用于治疗MTAP缺失型癌症 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 CTS2190，一种处于I/II期临床开发中的首创PRMT1抑制剂，展现出稳健而广泛的单药疗效，并基于转化研究发现为新型联合方案提供了理论依据 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 通过小分子降解靶向PRC2的非经典功能：前列腺癌及其他实体瘤的新型治疗策略 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缺失揭示MTAP缺陷型NSCLC对PRMT5抑制剂AZD3470的易感性 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抑制改变细胞染色质格局并驱动套细胞淋巴瘤对BH3模拟物的易感性 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抑制剂以Brd4-Sp1/Sp3依赖方式诱导人葡萄膜黑色素瘤细胞中NOX5的表达 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 将VHL与SETD2联系于一条汇聚于有丝分裂纺锤体的共同致癌通路 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 面向PRMT5靶向药物发现的综合实验方法 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 一种具有同类最佳潜力和良好药代动力学特征的高选择性KAT6/7双重抑制剂 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 以KC1101抑制TACC3驱动有丝分裂灾难并产生广泛的抗肿瘤活性 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 组蛋白去乙酰化酶抑制剂Imofinostat与免疫检查点抑制剂联用增强结直肠癌的抗肿瘤活性 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通过靶向HDAC3-NRF2通路增强KRAS突变型胰腺癌的化疗应答 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 发现具有同类最佳效力和选择性的新型SMARCA2小分子抑制剂用于治疗SMARCA4突变型癌症 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与PI3K通路抑制剂联用在PIK3CA突变型ER+乳腺癌临床前模型中驱动更优疗效 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 胚胎外胚层发育（EED）抑制剂APG-5918通过化疗敏感性的表观遗传引发作用在临床前小细胞肺癌（SCLC）模型中与拓扑异构酶I抑制剂协同增效 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 4501 靶向多发性骨髓瘤中的表观遗传衔接蛋白menin 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 扩展PRISM平台：新增血液学模型和10天检测改进表观遗传靶点的药物敏感性图谱绘制 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-843：一种潜在同类最佳的第二代menin-MLL抑制剂，经改造以克服临床观察到的menin突变介导的耐药，在急性白血病模型中具有卓越的临床前疗效和安全性 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 MTA协同型PRMT5抑制剂ABSK131与多种治疗药物联用在多种癌症模型中的协同抗肿瘤活性 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是一种高效、高选择性的PRMT5抑制剂，具有MTA阳性和SAM阴性协同性，经优化用于在MTAPdel癌症中与变构MAT2A抑制剂IDE397联用开发 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是一种同类首创的双功能HDAC和自噬抑制剂，具有强效抗白血病活性 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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