Late-Breaking Research: Experimental and Molecular Therapeutics 3

• LB344 LB344 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
• LB345 · PDF HZ-V055, an oral, highly potent pan-Ras molecular glue inhibitor demonstrated robust potency in Ras Mut cancer models Yizhe Wu, Bo Feng, Jiangfeng Xie, Peipei Wang, Jinglai Huang, Xiaobei Hu, Gaoya Xu, Yubo Zhou, Jia Li, Xinglu Zhou
• LB346 LB346 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
• LB347 · PDF Discovery and identification of SHR-RAS001: A structurally novel, highly potent tri-complex RAS multi (ON) inhibitor Xin Li, Feng Shen, Limin Zhang, Bin Gui, Wei Wang, Yong Liu, Yong Bao, Lu Wang, Yixiu Li, Yuchang Mao, Zaiyong Wang, Chunyue Wang, Jun Feng, Min Hu, Feng He
• LB348 · PDF Small-molecule targeting of p27 enables coordinated CDK2/4/6 inhibition in CDK4/6i-resistant breast cancer Grace Chen, Carolina Guido, Charles H. Reynolds, Krishna P. Allamneni, Stacy W. Blain
• LB349 LB349 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 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 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 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
• LB353 · PDF NPP-2-21: A rationally designed prodrug of a UBA1 inhibitor with improved pharmacologic properties and antitumor activity Yi Bao, Pengpeng Niu, Ke Ding, Arul M. Chinnaiyan
• LB354 LB354 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, 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
• LB357 · PDF Preclinical evaluation of ARTS-876, an AKR1C3-activated prodrug targeting KEAP1/NFE2L2-mutant NSCLC Cong Zhu, Jiaqi Liang, Xiaozhi Yang, Yin Pan, Wenheng Liang, Xiaobin Zhang, Nathan Schomer, Xiang Zhai, Lina Gu, Qing Sheng, Yaoyu Chen, Fang Li
• LB358 · PDF BPI-585771: A novel, potent pan-KRAS degrader with potent in vitro and in vivo efficacy in KRAS-driven tumors Zhengqing Li, Renqi Xu, Yanju Liu, Jiayu Zhao, Ying Zhao, Tianyi Ma, Tao Zhang, Bo Yan, Liang Chen, Jing Guo, Cheng Yang, Han Han, Xiaoyun Liu, Haibo Chen, Quan Zhou, Hong Lan, Li Mao, Lieming Ding
• LB359 LB359 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
• LB360 · PDF Targeted degradation of p300 and CBP via antibody-drug conjugate in prostate cancer cells Fabiola Shelton, Yongqin Wan, Stephen Fuhs, Jocelyn Cheung, Sergio Briones, Gabrielle Cauvi, Hui Qin Wang, Carie Jackson, Bei Chen, Wenqi Gao, Xiaodong Liu, Donnie Delarosa, Eric Peters, Analisa Benedetto, De Shon Hall, Sandra Gao, Julian Wong, John Taraszka, Glenn Federe, John Walker, Saravanan Parthasarathy, Charles Cho, John Hoerter, Jacob R. Haling
• LB361 LB361 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
• LB362 · PDF P65-047, a novel TEAD degrader, overcomes KRAS inhibitor resistance through Hippo pathway disruption in NSCLC Rajiv Sawant, Matthis Geitmann, Per Källblad, Samrat T. Kundu, Sofia Garza, Don L. Gibbons, Konrad Koehler, Peter Brandt
• LB363 LB363 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 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
• LB365 · PDF Mechanistic and early clinical characterization of VRN101099, a selective HER2 inhibitor with receptor degradation activity Jun-Young Park, Jihye Yoo, Rasha Cosman, Jee Hung Kim, Christopher Steer, Jieun Lee, Yeon Hee Park, Seock-ah Im, Sun Young Rha, Jee Hyun Kim, Kyung Hae Jung
• LB366 · PDF Zidesamtinib has differentiated preclinical brain penetrance and intracranial activity compared to other ROS1 inhibitors Anupong Tangpeerachaikul, Joshua C. Horan, Henry E. Pelish
• LB367 LB367 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

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