Proximity-Induced Drug Discovery 1

• 4591 · PDF 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 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, 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, 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 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 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 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 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 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 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 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 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 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 Brigatinib based degraders as a therapeutic strategy for triple negative breast cancer Manu Khosla, Suresh Alahari, Guangdi Wang
• 4606 · PDF 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 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: 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 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 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 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 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, 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 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 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 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, 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, 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 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: 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

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