Proximity-Induced Drug Discovery 1

• 4591 · PDF SC3613（IN-207387），一种突变选择性EGFR降解剂，在EGFR TKI耐药的NSCLC中展现出强效抗肿瘤活性和改善的安全性 SC3613 (IN-207387), a mutant-selective EGFR degrader, exhibits potent anti-tumor activity and improved safety profile in EGFR TKI-resistant NSCLC Jun Gyu Kim, Jihoon Choi, Ok Young Lee, Young Jun Park, Young Min Jeong, Choongsil Lee, Seo Yoon Jeong, Hye Yeon Lee, Yu Jin Lee, Punna Reddy Ullapu, Hyesun  Lee, Dae Young Lee, Ah Yeon Park, Hyoeun Jo, Sun Ho Choi, Sun Ho Jeon, Ji-Young An, Jong Hyun Lee, Yang Hun Tae, Mirae An, Keunho Lee, Jong Ryoul Choi, Bong Tae Kim, Mi-Kyung Kim
• 4592 · PDF 高选择性、强效的可逆共价FGFR4抑制剂BB102通过溶酶体自噬诱导靶蛋白降解 The highly selective and potent reversible-covalent FGFR4 inhibitor, BB102, induces targeted-protein degradation through lysosomal autophagy Min Li, Qi Wang, Gongping Duan, Xiaoyi Ma, Junheng Wang, Lijie Wei, Xingmin Zhang
• 4593 · PDF PBI-381，一种针对KRasG12D实体瘤的开发候选PROTAC PBI-381, a development candidate PROTAC for KRasG12D solid tumors Bing Zhang, Yuxin Liu, Yufeng Chen, Danqiu Lin, Jinhua Chai, Yang Meng, Mixue Tong, Ganng Yang, Michael Xiang, Liping Zhao, Rui Yang, Lan Xu, He Zhou, Jason Xiang
• 4594 · PDF LY4584180，一种新型BCL6分子胶，在B细胞NHL的临床前模型中展现出抗肿瘤疗效 LY4584180, a novel BCL6 molecular glue, demonstrates antitumor efficacy in preclinical models of B Cell NHL Candace Langan, Nicholas E. Brown, Bryan G. Perria, Petia Gatzeva-Topalova, Bonita D. Jones, Lisa J. Kindler, Wayne D. Blosser, Rebecca J. Metivier, Eric S. Fischer, Xueqian Gong, Nathan A. Brooks
• 4595 · PDF 一种同类首创的强效EZH2降解剂AXT-1003在多种淋巴瘤和实体瘤中展现出稳健的抗肿瘤活性 A first-in-class potent EZH2 degrader, AXT-1003, exhibits robust anti-tumor activity across multiple lymphomas and solid tumors Yong Yang, Huiya Huang, Enxing Zhou, Yan Lin, Qian Gao, Alex Xu
• 4596 · PDF AR PROTAC AZD9750 与 AKT 抑制剂 capivasertib 联用在前列腺癌中疗效优于单药治疗 The combination of the AR PROTAC AZD9750 and AKT inhibitor capivasertib delivers improved efficacy over monotherapy in prostate cancer Antonio Ramos-Montoya, Chrysiis Michaloglou, Nuria Galeano-Dalmau, Ana Quiroga, Michael Niedbala, Claire Crafter
• 4598 · PDF 一种口服生物利用度良好、特异性 PLK1 双功能降解剂，用于治疗小细胞肺癌及其他癌症 An orally bioavailable, specific PLK1 bifunctional degrader for the treatment of small cell lung cancer and other cancers Keum Young Kang, Im Suk Min, Seong Hye Ahn, Gi Bbeum Lee, Sol Hee Noh, Yeon Jung Song, Hyun Lim, Boas Nam, Hanbit Lee, Su Gwon Lee, Woojeung Song, Kyungsik Ha, Junyang Jung, Jihoon Ryu, Soo Hee Ryu, Na Young Lee, Seong Hoon Kim, Hwajin Lee
• 4599 · PDF 合理设计的变构 EGFR 降解剂 SC3499（IN-207375）在非小细胞肺癌中选择性清除突变型 EGFR 并克服 osimertinib 耐药 Rationally designed allosteric EGFR degrader SC3499 (IN-207375) selectively eliminates mutant EGFR and overcomes osimertinib resistance in non-small cell lung cancer Jihoon Choi, Jun Gyu Kim, Yu Jin Lee, Young Jun Park, Ok Young Lee, Young Min Jeong, Choongsil Lee, Seo Yoon Jeong, Hye Yeon Lee, Hye Sun Lee, Punna Reddy Ullapu, Moon Jung Goo, Hyun Woo Park, Ah Yeon Park, Hyoeun Jo, Sun Ho Choi, Soo jung Choi, Dae Young Lee, Sun Ho Jeon, Jong Ryoul Choi, Jong Hyun Lee, Mirae An, Keunho Lee, Yanghun Tae, Ji-Young An, Bong Tae Kim, Mi-Kyung Kim
• 4600 4600 发现 PLX-66140：一种首创、强效且选择性的 CDK2 分子胶降解剂，用于 CCNE1 扩增肿瘤 Discovery of PLX-66140, a first-in-class, potent and selective CDK2 molecular glue degrader for CCNE1-amplified tumors Leenus Martin, Jean-Francois Brazeau, Nasrin Rastgoo, Quinn Spalding, Gabrielle Blanco, Kyohei Hayashi, Susan Song, Jianguo Ma, Shu You, Campos Alex, Jay Chung, Farhana Barmare, Kevin Freeman-Cook, Peggy A. Thompson
• 4601 · PDF 通过 AI 辅助分子建模合理设计强效雄激素受体降解剂并验证其在前列腺癌中的抗肿瘤疗效 Rational design of potent androgen receptor degraders via AI-assisted molecular modeling and validation of anti-tumor efficacy in prostate cancer Chih-Chang Chou, You-Sheng Lin, Cheng-Li Chou, Kuan-Hung Chen, Shu-Jen Chen, Chu-Chiang Lin
• 4602 · PDF 双重 HDAC3/8 PROTAC 降解剂在弥漫性大 B 细胞淋巴瘤中发挥抗肿瘤和免疫调节作用 Dual HDAC3/8 PROTAC degraders exert anti-tumor and immunomodulating effects in diffuse large B-cell lymphoma Michael Y. He, Yufeng Xiao, Mehran Bakhtiari, Ting Liu, Wenxi Xu, David G. Brooks, Housheng Hansen He, Guangrong Zheng, Robert Kridel
• 4603 · PDF 良好的 DMPK 特性使新型芳基磺酰胺 RBM39 分子胶降解剂 PPI-101 的开发成为可能，用于治疗神经母细胞瘤 Favorable DMPK properties enable development of a novel arylsulfonamide RBM39 molecular glue degrader, PPI-101, for the treatment of neuroblastoma Jian Wu, Lei Zhou, Yongzhi Gao, Shanshan Wang, Qi Zhang, Jingping Mei, Fang Bai, Song Feng, James X. Rong
• 4604 · PDF 一种 PROTAC 泛 KRAS 降解剂在 KRAS G12D 同基因小鼠模型中的临床前疗效及同期免疫肿瘤微环境变化 Preclinical efficacy of a PROTAC pan-KRAS degrader in a KRAS G12D syngeneic mouse model and concurrent immune tumor microenvironment changes Jason M. Berk, Andrea Lopez-Arroyo, Dana M. Klug, John P. Caldwell, Peter Hegan, Samantha Andella, Jessica Kraus, Amanda Chapman, Jennifer Pizzano, Mark Bookbinder, Gregory Cadelina, Debbie Gordon, Kim Davenport, Wendy Wu, Madeline A. Dorso, Morena Scopel, Rebecca Conrad, William Corwin, Goutham Pattabiraman, Keith R. Hornberger, Angela Cacace, Ignacio J. Juncadella, Kathryn D. Smith
• 4605 · PDF 基于Brigatinib的降解剂作为三阴性乳腺癌的治疗策略 Brigatinib based degraders as a therapeutic strategy for triple negative breast cancer Manu Khosla, Suresh Alahari, Guangdi Wang
• 4606 · PDF 新型DCAF16介导的SMARCA2选择性Targeted Glues™的理性开发用于治疗SMARCA4缺陷型肿瘤 Rational development of novel DCAF16-mediated SMARCA2 selective Targeted Glues ™ for the treatment of SMARCA4 deficient tumors James T. Lynch, Martin Ambler, Nicole Zordan, Claudia De Fusco, Laura Casares Perez, Kathryn Bosson, Alexander Fawcett, Paula MacGregor, Tarun Narwani, Colin T. R. Davies, Mahad Gatti Lou, Edward Hooper-Greenhill, Liliana Greger, Giles A. Brown, Martin Pass, Louise K. Modis
• 4607 · PDF 一种心脏安全的首创（first-in-class）MCL-1降解剂用于治疗血液系统恶性肿瘤的临床前评估 Preclinical evaluation of a cardiosafe first-in-class MCL-1 degrader for the treatment of hematological malignancies Tomasz Tomczyk, Anna Maria Serwotka-Suszczak, Robert Dyjas, Jose Arencibia, Monika Milewicz, Klaudia Poniatowska, Jolanta Skalska, Andrzej Tracz, Diana Trębicka, Karolina Wójcik, Sylvain Cottens, Piotr Kowalczyk, Paweł Dobrzański, Michał Biśta, Katarzyna Brach, Toshimitsu Takagi, Martyna Pastok, Justyna Adamczyk, Iwona Mames, Michał Walczak
• 4608 · PDF GSK5471713：一种新型、选择性口服雄激素受体降解剂，具有同类最佳（best-in-class）潜力用于治疗前列腺癌 GSK5471713: A novel, selective oral androgen receptor degrader with best-in-class potential for the treatment of prostate cancer Christine Thompson, Yang Lee, Melissa C. Musso, Kwok-Ho Chan, Kamelia Behnia, Edward Hooper-Greenhill, Christian S. Sherk, Nanhua Deng, Nadeesha Rajapaksha, Mansi Babbar, Sarah Gerhart, Julie Bullock, Kenneth W. Hance, Benjamin Schwartz, Laure Rittié, Christopher P. Tinworth, Anastasia Wyce
• 4609 · PDF PRMT5/MEP50降解剂的发现与开发用于选择性靶向MTAP缺失型癌症 Discovery and development of PRMT5/MEP50 degraders for the selective targeting of MTAP-null cancers Yue Zhong, Qian Chao, Yan Xiong, Husnu Kaniskan, Jian Jin
• 4610 · PDF B-hCRBN小鼠模型有助于基于CRBN配体的PROTAC研究 The B-hCRBN mice model facilitates PROTACs studies based on CRBN ligands Jay Zhang, Yue Zhang, Chonghui Liu, Ying Zhao, Xiao Liu, Jiansu Zhang
• 4611 · PDF 小分子稳定非天然c-Myc多聚体利用靶向IDP的发现平台驱动降解 Small-molecule stabilization of non-native c-Myc multimer drives degradation using an IDP-targeting discovery platform Markus K. Muellner, Christian Kuehne, Michael Ahrweiler, Antony Crisp, Florian Kellner, Katharina Strasser, Paulina Pacak, Bechir Zitouni, Joonsun Lee, Milanka Gavrilovic, Lisa Wurm, Bernadette Winter, Manuela Richter, Fiona Liebig, Noel Riedl, Christoph Berger, Stefan Seidl, David Fischer, Christine Triska
• 4612 · PDF 应用机制性临床前PK/PD/疗效建模以支持AZD9750（一种新型口服雄激素受体降解剂，PROTAC）的联合策略 Application of mechanistic preclinical PK/PD/efficacy modeling to support combination strategy for AZD9750, a novel oral androgen receptor degrader (PROTAC) Ana Quiroga, Pablo Morentin Gutierrez, Antonio Ramos-Montoya, Chrysiis Michaloglou, Nuria Galeano-Dalmau, Claire Crafter, Aaron Smith, Jamie Scott, Michael Niedbala
• 4613 · PDF ZMS-4426，一种口服SMARCA2降解剂，表现出强效抗肿瘤活性，但在不同物种间对SMARCA4存在选择性差异 ZMS-4426, an oral degrader of SMARCA2 shows potent anti-tumor activity, but variant selectivity against SMARCA4 across species Lu Liu, Fanxun Zeng, Ruonan Chen, Mengnan Hu, Yao Guo, Wenjing Li, Mei Lan, Liting Xue, Zhengtao Li, Renheng Tang
• 4614 · PDF 利用高通量泛素化检测评估靶向蛋白降解剂以进行机制与构效关系分析 Evaluation of targeted protein degraders using high-throughput ubiquitination assays for mechanistic and SAR analysis Yuzhou Xu, Jichuan Zhang, Yanfei Hu, Ye Tian, Min Lyu, Yinfei Yin
• 4615 · PDF 新型AR降解剂JSB462（Luxdegalutamide）及其在前列腺癌中的联合方案的临床前表征与评估 Preclinical characterization and evaluation of JSB462 (Luxdegalutamide), a novel AR degrader, and its combinations in prostate cancer Stephane Ferretti, Daniel A. Guthy, Marco Taddio, Marc Hattenberger, Marion Dourdoigne, Ramona Stump, Sabina Ciaghi, Mylene Lanter, Alessandra Amadori, Laurent Laborde, Asif Khan, Rafael Caparica, James Warburton, Marta Cortes Cros
• 4616 · PDF 整合的类器官筛选方法可实现对蛋白降解剂疗效和靶点结合的临床前评估 Integrated organoid screening approaches enable preclinical assessment of protein degrader efficacy and target engagement Marten Hornsveld, Dennis van der Grinten, Dorrith Verstegen, Shannon Kouters, Esther Kingma, Tomas Veenendaal, Mariusz Madej, Aaron Hua, Jinxi Wang, Lenno Krenning, Jessie Wang, Marrit Putker, Ludovic Bourre
• 4617 · PDF NRX-0305，一种口服生物可利用、可穿透中枢神经系统的泛突变BRAF降解剂，在黑色素瘤脑转移和原发性胶质瘤颅内模型中表现出强效疗效 NRX-0305, an orally bioavailable, CNS penetrant pan-mutant BRAF degrader demonstrates robust efficacy in intracranial models of melanoma brain metastasis and primary glioma Alexandra Borodovsky, Ya-Wen Lu, Ge Peng, Karthik Arumugam, Paul L. Auger, Delia Bradford, Lilly G. Carlson, Scott K. Kimura, Daniel Medina-Cleghorn, Mariah J. Mesner, Davorka Messmer, Madeleine P. Nemchek, Ryan B. Rountree, Rusha M. Sardhara, Sangita Sridharan, Jennifer M. Stokes, Leslie Tong, Alexandra M. S. Trotier, Jennifer S. Tung, Ge Wei, Jeffrey Wu, Jordan Ye, Gwenn M. Hansen
• 4618 · PDF TRI-611，一种处于开发阶段的ALK分子胶降解剂，用于治疗包括中枢神经系统转移在内的ALK阳性NSCLC TRI-611, a development stage molecular glue degrader of ALK for the treatment of ALK-positive NSCLC including central nervous system metastases Andrew R. Conery, Daniel S. La, Artyom A. Alekseyenko, David Marcoux, Aaron G. Bart, Matt L. Harlow, Patrick R. Arsenault, Nico R. Cantone, Rebecca L. Casaubon, Hari B. Kamadurai, Aravind Prasad Medikonda, Duncan E. Nunes, Tim J. Wigle, Maolin Yu, Aleksandra Zagulyaeva, Christine Zarate, Kathleen I. Seyb, Patrick Trojer, Vito J. Palombella
• 4619 · PDF 利用Apertor Interceptor——诱导邻近的双位点分子——使致癌信号失效 Disabling oncogenic signaling with Apertor Interceptors - Proximity inducing bisteric molecules Andrew Robertson, Shinji Kasahara, Jennifer Schmidt, Bo Pang, Nage Yarravarapu, Diego Garrido Ruiz, Rose Citron, Arash Samadi, Denisse Martinez, Nefeli Chanoutsi, Colleen Mulvihill, Arushi Singhai, Vinh Thai, Raissa Estrela Curado, Ericka Mendez, Edmund Graziani, Lawrence Lum
• 4620 · PDF RCZY-698：一种口服生物可利用、高效力、选择性的可逆KRAS G12V（ON）状态抑制剂，在KRAS G12V驱动的实体瘤临床前模型中具有强健的抗肿瘤活性 RCZY-698: An orally bioavailable, highly potent, and selective reversible KRAS G12V (ON)-state inhibitor with robust antitumor activity in preclinical models of KRAS G12V -driven solid tumors Xiaojing (Celia) Chen, Lin Wang, Xiaohong Liu, Zhengyong Wan, Qiaoni You, Jianming Bao

在会议检索中浏览本分会场