LBPO.ET03 · 实验与分子治疗 · Late-Breaking
Late-Breaking Research: Experimental and Molecular Therapeutics 3
- LB344 LB344 CNP200137的发现：一种具有卓越临床前特性并对获得性耐药具有抗白血病活性的第二代menin-MLL抑制剂 Discovery of CNP200137, a second-generation menin-MLL inhibitor with superior preclinical properties and anti-leukemic activity against acquired resistance Jin-Hee Park, Seongshick Ryu, Jae-Seon Lee, Shin-Hae Lee, Dohee Oh, Chaehyeon Seong, Yujung Park, Sumin Kim, Eunbin Park, Jiah Kim, An-Na Moon, Heung Sik Hahm, Jinsun Kwon, Jung Beom Son, Ky-Youb Nam, Jeong Hyeok Yoon, Nam Doo Kim, Hwan Geun Choi
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- LB346 LB346 一种首创的TAU-1定向的雄激素受体（AR）和AR-V7降解剂，募集DDB1-CUL4-RBX1 E3连接酶以消除致死性前列腺癌中的AR信号 A first-in-class TAU-1-directed androgen receptor (AR) and AR-V7 degrader recruits DDB1-CUL4-RBX1 E3 ligase to eliminate AR signaling in lethal prostate cancer Michelle K. Naidoo, Cherie Au, Kiran K. Sahu, Paraskevi Giannakakou
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- LB349 LB349 AIG07025的发现及临床前表征：一种具有广泛联合潜力的强效选择性USP1抑制剂 Discovery and preclinical characterization of AIG07025, a potent and selective USP1 inhibitor with broad combination potential Minjoong Kim, Hyerim Yoo, Miyeon Kim, Ho-Jeong Lee, Eok Park, Jinkwan Kim, Jaewoo Kang
- LB350 LB350 ABK-EGFR-1的发现与表征：一种具有优异选择性和脑穿透性的第四代EGFR C797S抑制剂 Discovery and characterization of ABK-EGFR-1, a 4 th generation EGFR C797S Inhibitor with excellent selectivity and brain penetration Mei Ning, Juan Peng, Wei Guo, Jie Wang, Jie Zhang, Weijia Lu, Manqi Liu, Haiyan Ying, Haibing Deng, Hongping Yu, Yao-chang Xu
- LB351 LB351 发现高选择性、口服可利用的小分子DDR1抑制剂，重编程胶原-DDR1肿瘤微环境 Discovery of highly selective, orally available small-molecule DDR1 inhibitors that reprogram the collagen-DDR1 tumor microenvironment Jungwook Chin, Sun Jun Park, Su-Jeong Lee, Jong-Hyun Park, Jun Young Hong
- LB352 LB352 首创hSSB2激活剂作为一种双重治疗策略，克服RAS/MAPK抑制剂耐药性同时保护侵袭性癌症中的正常上皮 First in class hSSB2 activator as a dual therapeutic strategy for overcoming RAS/MAPK inhibitor resistance while protecting normal epithelia in aggressive cancers Elizabeth M. Singer, Rishi M. Chugh, Payel Bhanja, Julian P. Whitelegge, William H. McBride, Jesus Rodriguez, Anusha Ravisankar, Mandeep Kumari, Andrew John Norris, Subhrajit Saha
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- LB354 LB354 药理学TSC2抑制通过mTORC1介导的线粒体灾难使急性髓系白血病对蛋白酶体抑制敏感 Pharmacologic TSC2 inhibition sensitizes acute myeloid leukemia to proteasome inhibition via mTORC1 mediated mitochondrial catastrophe Shakti Pattanayak, Boaz Tirosh, Omid Hajihassani, Jordan M. Winter, Kelsey H Fisher-Wellman, Leif A Eriksson
- LB355 LB355 ICP-B794，一种采用新型linker-payload的B7H3靶向ADC，在临床前研究中表现出优越的抗肿瘤活性和较大的治疗窗 ICP-B794, a B7H3-targeting ADC with a novel linker-payload, demonstrated superior anti-tumor activity and large therapeutic window in preclinical studies Dongliang Mo, Yingxiang Gao, Xiaoyan Wang, Yuan Qian, Hongjuan Zhang, Yingrui Han, Richard Liu, Junjian Liu, Charles Wang, Xiangyang Chen, Bin Zhang
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- LB359 LB359 Bcl-xL特异性PROTAC——DT2216提高不同来源临床前肿瘤模型对靶向治疗的敏感性 The Bcl-xL specific PROTAC, DT2216, increases the sensitivity to target therapy of preclinical tumor models from different origin Giulia Gentile, Elisabetta Valentini, Marta Di Martile, Simona D'Aguanno, Matteo Brignone, Adriana Maria Di Stefano, Marica Di Caprio, Elisa Melucci, Claudio Botti, Fabio Pelle, Arianna Ortolano, Luigi Fattore, Rita Mancini, Gennaro Ciliberto, Dante Rotili, Michela Chiappa, Giovanna Damia, Donatella Del Bufalo
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- LB361 LB361 选择性降解一种新型驱动蛋白作为应对高危型染色体外DNA（ecDNA）阳性癌症（包括乳腺癌）的潜在治疗策略 Selective degradation of a novel kinesin as a potential therapeutic strategy addressing high-risk extrachromosomal DNA (ecDNA) positive cancers, including breast cancer Deepti Wilkinson, Frederick A. Derheimer, Ardalan Adreshi, Joan Chen, Yuan Chien, Cory DuPai, Rachel Elsdon, Ryan J. Hansen, Kimberly Johnson, Shailaja Kasibhatla, Laura Layman, Zhengke Li, Ronghua Li, Debbie Liao, Taylor Loe, Jacques Mauger, Jafar Moininazeri, Ben Norman, Anne Marie Pferdekamper, Joshua Plum, Casey Sarkissian, Dave Solis, Auzon Steffy, Huikai Sun, Yen Truong, Julie Wiese, Anthony B. Pinkerton, Christian A. Hassig
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- LB363 LB363 TXN-A的发现与表征：一种首创的、口服生物利用度良好的ULK1降解剂，具有高选择性和强效性，用于TNBC治疗 Discovery and characterization of TXN-A: A first-in-class, orally bioavailable ULK1 degrader with high selectivity and potency for TNBC treatment Yo Han Hong, Jung-eun Park, Jiah Lim, Yong-Chang Kim, Jun Young Choi, Ye Jin Kim, Young Hoon Choi, Hye Jung Park, Hee Jin Jeong, Chang Won Min, Eunmyong Lee, Hong Jun Kang, Hyouk Woo Lee, Sungjoon Kim, Chan Sun Park
- LB364 LB364 TOP1-DNA蛋白复合物作为PARP抑制剂耐药性卵巢癌中NKTR-102/Rucaparib联合治疗的预测性生物标志物 TOP1-DNA protein complex as a predictive biomarker for NKTR-102/Rucaparib combination therapy in PARP-inhibitor resistant ovarian cancer Annapoorna Venkatachalam, Caroline C. Nitschmann, Karen S. Flatten, Rachel Hurley, Xiaonan Hou, Cristina Correia, Paula A. Schenider, Krista Goergen, Matthew Maurer, Ethan P. Heinzen, Ann L. Oberg, S. John Weroha, Paul Haluska, Scott H. Kaufmann, Elizabeth M. Swisher
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- LB367 LB367 新型非糖类糖胺聚糖模拟物通过选择性靶向关键酪氨酸激酶受体抑制结直肠癌干细胞 Novel non saccharide glycosaminoglycan mimetic inhibit colorectal cancer stem cells by selectively targeting key tyrosine kinase receptors. Shoja M. Haneefa, Bharath Villuri, Rio Boothello, Priyanka Mishra, Umesh R. Desai, Bhaumik Patel
