Proximity-Induced Drug Discovery 2

• 5774 · PDF Discovery of potent CDK8/CDK19 PROTAC degraders with superior anti-leukemia efficacy Li Zhang, Jia Zheng, Rebekah Martin, Jing Li, Zachary T. Mack, Hao Ji, Eugenia V. Broude, Igor B. Roninson, Campbell McInnes, Mengqian Chen
• 5775 · PDF When CDK meets CIP: Linking target engagement to functional outcomes in CDK2 molecular glue and CDK‑TCIP Qing Xue, Zhu Meng, Xue Yang, Qian Wang, Lili Chai, Wei Liu, Tj (Tiejun) Bing
• 5776 · PDF Discovery of an orally bioavailable AKT degrader with sustained in vivo efficacy and translational potential Seung Jae Jeong, Hyunsun Jo, Juyoung Jung, Hyunah Yoon, Aerim Hwang, So-Eun Son, Iljin Shin, Eun Seo Bae, Narkhyun Bae, Hyounmie Doh
• 5777 · PDF Functional role of PLK1 in colorectal cancer progression and its potential to chemoresistance Kong Hyejeong, Baek MooJun, HyoWook Gil, Eunjung Yang, Kwangseock Kim, Taewan Kim, jaesung Ryu, Beamjun Park, Jeong Kyu Bang, Seob Jeon
• 5778 · PDF RCZY-690: A tri-complex molecular glue pan-RAS (ON) inhibitor exhibiting best-in-class potential for RAS-addicted solid tumors Xiaojing (Celia) Chen, Lin Wang, Xiaohong Liu, Qiaoni You, Shenjun Li, Ling Wang, Shanshan Bi, Jing Jiang, Jianming Bao
• 5779 · PDF RCZY-869: A highly potent, selective, and orally bioavailable covalent KRAS G12D (ON-state) inhibitor with robust antitumor activity in preclinical models of KRAS G12D -driven solid tumors Xiaojing (Celia) Chen, Lin Wang, Xiaohong Liu, Dan Wang, Jianming Bao
• 5780 · PDF Discovery of ATH-007, a novel, potent and highly selective CCNE1 molecule glue shows robust anti-tumor activities and better safety profile Zhiyong Yu, Wenming Li, Yuyao Zhang, Wenwen Zhao, Youxi Chen, Feng Zhou
• 5781 · PDF CXB-7138, A novel GSPT1/ZFP91 dual molecular glue degrader, for targeted treatment of pancreatic ductal adenocarcinoma Jin-Hee Park, Jae-Seon Lee, Shin-Hae Lee, NamKyoung Kim, Sumin Kim, Chaeseon Kim, Yong Chan Kim, Eunbin Park, Jiah Kim, Heung Sik Hahm, Jung Beom Son, Nam Doo Kim, Hwan Geun Choi
• 5782 · PDF Machine learning and structure-guided discovery of EP300-selective, orally bioavailable degraders for cancer therapy Ho Yeon Nam, Sun Young Jang, SeokJong Kang, Yongtaek Lee, Seongil Kang, Taegun Kim, Jooyun Byun, Gunwoo Lee, Wonjong Lee, Hobin Im, Haemin Chon, Yu-Yon Kim, Seunghwan Jung, Young Gil Ahn
• 5783 · PDF HY809382, a PRC2 degrader with best-in-class properties, demonstrates efficacy across multiple tumors and overcomes EZH2 inhibitor clinical resistance caused by EZH2 genetic mutations Xin Li, Weixing Zhu, Ruwei Wang, Zengrong Li, Liming Zhang, Lei Chen, Sai Yang, Feng Xu, Qian Ma, Huangtao Jin, Xiaotian Huang, Ting Zhang, Xing Yu, Ming Weng, Xiaoxiao Wang, Xiaohong Hou, Manli Hu, Tingting Dai, Ruowen Zhang, Juan Du
• 5784 · PDF Discovery of FX-111, a first-in-class heterobifunctional degrader of transcriptionally active androgen receptor (AR ON ), to treat patients with AR-driven prostate cancer Jennifer A. Mertz, Thomas H. Graham, Brian J. Golbourn, Yong Li, Alex P. Rossi, Marco Chiumiento, Phuong A. Nguyen, Jeremy W. Setser, Gregg Chenail, Rainer Wilcken, Jonathan T. Goldstein, Hannah Nguyen, Christina S. Henderson, Kaylyn E. Williamson, Byron DeLaBarre, Christopher M. Bailey, Miljan Kuljanin, Matthew C. Koehler, James E. Audia, Jonathan E. Wilson, Jacob I. Stuckey, Robert J. Sims
• 5785 · PDF RBM39 degrader anticancer activity against neuroblastoma: CDKN2A/B deletion as a biomarker James Finn, Imad salhab, Haihong Jin, Fei Liu, Dong Liu, Yunkai Zhang, Xing Liu, James Tonra, Lan Huang, Dan Lu
• 5786 · PDF Novel non-CRBN based molecular glue identification and corresponding E3 ligase target deconvolution through multi-omics analysis Tongrui Hao, Yi Chen, Yan Gao, Jing Wen, Wenzhang Chen, Zhongyao Ma, Letian Kuai, Wenji Su
• 5787 · PDF TRI-611, a development stage molecular glue degrader of ALK, promotes the degradation of TKI-resistant ALK fusion proteins and leads to regression of ALK TKI-refractory tumors 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, Lauren Highfield, Nobuyuki Kondo, Aaron N. Hata, Kenneth Ngo, Jisu Lee, Prafulla C. Gokhale, Kathleen I. Seyb, Patrick Trojer, Vito J. Palombella
• 5788 · PDF Rational discovery of novel molecular glues Simon Woehrle, Andreas Blum, Beatrix Blume, Jörg Bomke, Hans-Peter Buchstaller, Vincenza Dragone, Isabella Ferrara, Alessia Gambardella, Jakub Gunera, Ulrich Grädler, Ingo Kober, Johannes Krieger, Birgitta Leuthner, Andrea Unzue Lopez, Oliver Schadt, Christina Schindler, Fiona J. Sorrell, Ana M. Esteves, Sandra P. Santos, Raquel L. Sousa, Margarida M. S. Silva, Ana R. Lemos, Pedro M. F. Sousa, Tiago M. Bandeiras, Maria Emanuela Cuomo
• 5789 · PDF Discovery of a selective molecular glue degrader of CCNE1 for the treatment of CCNE1-amplified solid tumors and CDK4/6i-resistant HR+/HER2- breast cancers Benjamin M. Vincent, David Marcoux, Claudia Caligioni, Aaron G. Bart, Matt L. Harlow, Rosaline Y. C. Hsu, Prashant Singh, Rachel Badger, Andrew J. Ingersoll, Thomas B. Jordan, Hari B. Kamadurai, Christine Zarate, Nico R. Cantone, Aravind Prasad Medikonda, Artyom A. Alekseyenko, Duncan E. Nunes, Taras Dauzhenka, Anushka Bhagwat, David Y. Rhee, Patrick R. Arsenault, Andrew R. Conery, Alex Constan, Louis Plamondon, Tim J. Wigle, Daniel S. La, Kathleen I. Seyb, Patrick Trojer, Vito J. Palombella
• 5790 · PDF Next-generation PRMT5 activity modulation through directed degradation Jose C. Clemente, Xuqing Zhang, Brian Vidal, Aaron Stonberger, Sudeep Banjade, Cory T. Rice, Nathan M. Kendsersky, Curran A. Rhodes, Matthew Tudor, Qiaolin Deng, Bomie Han, Clemente Aguilar-Bonavides, Elham Behshad, Steven D. Knight, Corey Strickland, Larry J. Jolivette, Ryan G. Kruger
• 5791 · PDF Preclinical characterization of NEO-811, a novel molecular glue degrader of ARNT for the treatment of clear cell renal cell carcinoma J. Scott Lee, Michelle S. Cruz, Isabella Tran, Kevin Chiu, Jennifer Griffin, Andres H de la Peña, Kurt Januszyk, Xiaoxi Liu, Bryan Lee, Anthony Burt, John Tellew, Mengyu Wu, Leslie Watson, Ana Dominguez-Andres, Ling Huang, Randy Soriano, Devin Knece, Molly FitzGibbon, Jake Fathman, Celin Sanchez, Nathalia Cruz, Zac Neiman, Ana Grant, Mary Matyskiela, Rohan Beckwith, Ben Wen, Klaus Wagner, Philip Chamberlain
• 5792 · PDF Identification of first in class selective ARID1B degraders Madeleine Henley, Benjamin Adams, Richard Caldwell, Jozlyn Clasman, Silvia Escudero, Imran Hossain, Kana Ichikawa, Jamie Im, Alexia Kalogeropulou, Dipti Sadalge, Gabriel Sandoval, Cody Schwarzer, Laura Von der Porten, Nick Yang, Marina Nelen, Gromek Smolen, Kevin Wilson, Steven Bellon
• 5793 · PDF First-in-class potent and selective oral KAT6A degrader development candidate, PRT13722, drives complete tumor regressions as a monotherapy with an improved pre-clinical hematological safety profile Monisha Sivakumar, Sarah Pawley, Corey Basch, Jimin Park, Justin Kurian, Anthony Reichelderfer, Yue Zou, Kirsten Gallagher, Miles Cowart, Joy Cote, Alexander Grego, Jessica Burtell, Amy Crossan, Michael Hulse, Anjana Agarwal, Arpita Mondal, Chun Chen, Vijay Devannah, Sina Rezazadeh, Quincy Lewis, Patrick Wen, Ken Ray, Raul Leal, Daniel Porreca, Ganfeng Cao, Neha Bhagwat, Shanthi Ganesan, Stefan Ruepp, Min Wang, Joseph Rager, Koichi Ito, Sandy Geeganage, Andrew Combs, Peggy Scherle, Andrew Buesking, Jack Carter
• 5794 · PDF Leveraging E2 ligases for induced proximity and modulation of novel cancer-relevant targets and neosubstrates Xiangrong Chen, Vittorio Katis, Qilong Wu, Lukas Scheibelberger, Jesper Hansen, Brian D. Dill, Oksana Zavidji, Maria-Dorothea Nastke, Tiffany V. Saunders, Clifford G. Phaneuf, Andrea Pierangelini, Darragh O'Brien, Alejandro Gonzalez Orta, Niven R. Narain, Stephane Gesta, Alex N. Bullock, Dinesh Chimmanamada, Paul Brennan, Kilian Huber, Vivek K. Vishnudas
• 5795 · PDF The discovery of BLU-020: A potent and selective degrader of CDK2 for the treatment of CCNE1 aberrant cancers Phil Ramsden, Dean Zhang, Maria Iliou, Suhasini Parimi, Jeff Keats, Maxine Chen, Lakshmi Muthuswamy, Guangyan Du, Fereidoon Daryaee, Ben Barlock, James Baker, Sue Spong, Ken Kearney, Gramoz Kondakci, Deborah G. Conrady, Stella Li, Xavier Fradera, Yinghui Dai, Tina Tran, Tom Dineen, Chiara Conti
• 5796 · PDF Rpn13Pru targeting small molecules induce mitotic arrest in breast cancer. Santwana K C, Xiuxiu Lu, Snehal M. Gaikwad, Venkata R. Sabbasani, Rolf Swenson, Beverly A. Mock, Kylie J. Walters, Deborah E. Citrin
• 5797 · PDF PK/PD and preclinical ADME characterization of TB-008, a first-in-class CDK9 degrader in xenograft models Narayana Narasimhan, Mahesh Koirala, Isabelle Dussault, Lindy Yan, Oscar Kashala, Zoser Mohamed, Mario DiPaola
• 5798 · PDF Targeted protein degradation of cell surface proteins through peptide-induced clearance Hadir Marei, Sanjana Sen, Patrick Aouad, Victoria Pham, Christopher Rose, Wen-Ting Tsai, Sheil Kee, Eva Lin, Matthew Grimmer, Tim Sterne-Weiler, Xiaosai Yao, Mark Wang, Diana Wu, Russell Xie, Nicholas Agard, Stephen Miller, Robert Yauch
• 5799 · PDF Lumit-based profiling of degrader dynamics reveals signaling-dependent, cell context-specific sensitivity to degraders Matthew Swiatnicki, Laurie Engel, Hicham Zegzouti
• 5800 · PDF Discovery of pan-KRAS molecular glue degraders via protein-first coevolution-guided E3 ligase recruitment Roman Timakhov, Haishan Li, Nikolay Savchuk, Alexander Khvat
• 5801 · PDF NRX-0305 is an orally bioavailable, pan-mutant BRAF degrader that exhibits single-agent and combination efficacy with MEKi or anti-EGFR across Class 1/2/3 BRAF-mutant cancers Ya-Wen Lu, Alexandra Borodovsky, 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
• 5802 · PDF Long acting injectable of pan-RAF-MEK molecular-glue: Metronomic exposure for the treatment of pancreatic ductal adenocarcinoma Drishti Rathod, Ketankumar Patel
• 5803 · PDF Discovery of a paralog selective p300 protein degrader with potent anti-cancer activity in hematological malignancies Marwa Asem, Yan Zhai, Xiaohong Song, Milad Rouhimoghadam, Sreenivas Punna, Fritz G Buchanan, Daniel T Cohen, Ryan McClure, Stephanie Sandoval, Anlu Chen, Shaun McLoughlin, Colin Woodford, Peter Kovar, Vlasios Manaves, Alla V Korepanova, Justin M Reitsma, Andrea Shergalis, Judith A Ronau, Yifei Kong, Yu Shen, Jurgen Dinges

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