Targeted Protein Degradation and Induced Proximity

• 4774 · PDF Targeting Beta-catenin in colorectal cancer: Novel molecular glue drug candidates by Coltac's BOND+ platform Yaron Sfadyah, Orli Even-Or, Michael Mullokandov, Hana Boocholez-Vardi, Valeria Arkadash, Alexandra Brodezki, Daniel Feder, Liraz Harel, Elon Yariv, Gali Prag
• 5151 · PDF Design and synthesis of highly efficacious CRBN-based pan-KRAS degraders targeting cancers with KRAS G12D, G12V and G12C mutations Changwei Wang, Prithwish Ghosh, Shicheng Jin, Longchuan Bai, Donna McEachern, Angelo Aguilar, Qiuxia Li, Bo Wen, DUXIN SUN, Shaomeng Wang
• 5152 · PDF Targeted degradation of KRAS using the AUTOTAC platform Su Ran Mun, Su Jin Lee, Hyeong-Reh C. Kim, Yong Tae Kwon
• 5153 · PDF Characterization of second-generation AUTOTACs targeting the androgen receptor for castrate-resistant prostate cancer treatment Tri Pham, Su Jin Lee, Y. Mindy Huang, Matthew Han, Tae-Hyun Bae, Brianna Temby, Isabella Schena, Abdo J. Najy, Harmant Grewal, Jenna Poole, Young Tae Kwon, Hyeong-Reh C. Kim
• 5154 Proteolysis and gene silencing targeting chimera (PROGENTAC) Abhay Prasad, Rong Zheng, Deeksha Satyabola, Yang Xu, Yichen Yan, Hao Yan
• 5156 · PDF Development of FBXW7 binders for targeted protein degradation Shenghao Guo, Becky Leifer, Yichen Xiang, Angela N. Koehler
• 5157 · PDF Discovery and characterization of XNW34017, a first-in-class, orally bioavailable, and brain-penetrant AURKA-MYC degrader Liqun Chen, Haoran Li, Xiuchun Zhang, Chong Peng, Zhe Zhang, Shihua Wang, Liang Kong, Jiajing Xu, Xiaocheng Hu, Zhenwei Wu, Yanfei Wang, Wengui Wang, Haiyang Wei, Yonghan Hu, Xiaojun Liu, Meijie Le, Jing Qiang
• 5158 Preclinical characterization of HY809382, a highly potent and orally bioavailable PRC2 PROTAC, for the treatment of lymphoma and solid tumors Huangtao Jin, Juan Du, Ruwei Wang, Zengrong Li, Ting Zhang, Xing Yu, Ming Weng, Xiaoxiao Wang, Xiaohong Hou, Feifei Yang, Xin Li, Weixing Zhu, Liming Zhang, Lei Chen, Sai Yang, Feng Xu, Qian Ma, Ruowen Zhang, Xiaotian Huang
• 5159 · PDF Rational development of novel FBXO22-mediated TEAD Targeted Glues™ for mesothelioma and NSCLC treatment Marta Carrara, Martin Fisher, Alice Fletcher, Callum Hamby, Jack Miles, Colin T. Davies, Sara Bisetto, Paula MacGregor, Edward Hooper-Greenhill, Aleksandra Azevedo, Martin O'Rourke, Dominic CG Owens, Liliana Greger, Ivan Del Barco Barrantes, Giles Brown, Martin Pass, Louise K. Modis
• 5161 HJ-004, a potent and selective pan-EGFR mutation targeted protein degrader (TPD) that effectively overcomes osimertinib resistance in EGFR-mutant NSCLC Li Zeng, Yao Liu, Ya Geng, Yue Zhu
• 5163 · PDF Leveraging selective degradation of CBP and EP300 for potent anti-cancer activity Karolina Mizeracka, Elizabeth Wittenborn, Darshan Sappal, Laura La Bonte, Danette L. Daniels
• 5164 · PDF Exploration of novel E3 ligase to support targeted protein degradation drug discovery Zuyuan Shen, Yunyun He, Rui Wang, Nengwei Xu, Peichuan Zhang, Lingbing Sun
• 5166 NRX-4972, a selective, oral, Aurora kinase A degrader, demonstrates increased efficacy in an SCLC tumor model, and greater in vitro synergy than an AURKA inhibitor Hua Tian, Ryan B. Rountree, Jeffrey T. Mihalic, Eric R. Wegrzyniak, Ge Wei, Karthik Arumugam, Paul L. Auger, Graham J. Carlson, Robert T. Cass, Tarra Knotts, Filippo Marchioni, Daniel Medina-Cleghorn, Michael G. Mormino, Madeleine P. Nemchek, Rusha M. Sardhara, Sangita Sridharan, Austin Tenn-McClellan, Simon Vezina-Dawod, Gwenn M. Hansen
• 5167 · PDF Design and applications of novel hydrophobic CRBN binders Hailong Yang, Qingbo Xu, Yongqiang Wang, Zhenyu Wu, Hongbo Zhang
• 5168 · PDF Expanding the landscape of targeted protein degradation: E3-agnostic discovery and proprietary ligand identification Kanae Gamo, Shinya Yokosaka, Michiko Watanabe, Tomoaki Hayashi, Shigeyuki Mori, Naomi Asahara, Noriyasu Sano, Shigeru Furukubo, Kazuteru Aoki
• 5169 · PDF Identification and optimization of pyridylbenzylamine analog 1 as potent and selective Helios degrader Ashok Purandare, Godwin Kumi, Guo Li, Aaron Balog, Emily Cherney, Michael Barnes, Satheesh Nair, Sirish K. Lakharaju, Xin Li, Robin Moore, Petia Shipkova, Silvi Chacko, Cullen Cavallaro, Ling Li, Kimberly Foster, Keith DiPetrillo, Gerry Everlof, Kevin Stefanski, Steven Levine, Lihong Shi, Jinqi Liu, Helen Pham, Ari Salinger, Ashok Dongre, Shailesh Dudhgaonkar, Debarati Mazumder, Anuradha Gupta, Vetrichelvan Muthalagu, Madhusudhan Ravindran, Yan Chen, Weifang Shan, Suresh Babu Viswa Krishna Penmetsa, Carolyn Weigelt, Robert Borzilleri, Louis Lombardo, Gregory Vite, John Hunt
• 5170 · PDF Design and optimization of small-molecule PROTACs targeting KRAS Fidelix Ayobami, Sai Kumar Samala, Ngoc Tuyet Tra, Geraldine V. Raja, Yuri Mackeyev, Sunil Krishnan
• 5171 The EGFR-PROTAC molecule TY-2719 attenuates acquired resistance to 3rd-generation EGFR TKIs and augments the efficacy of KRAS mutant inhibitors in solid tumors Apeng Liang*, #, Shengli Dong*, #, Shaoqing Chen*, Hongqiang Li, Zhiyong He, Zhengfei Guo, Meihua Li, Shunxun Han, Guangbin Liu, Xi Wang, Yanyan Liu, Ling Fang, Yi Long, Xiang Zhang, Wei Wu, Chengshan Niu, Jun Li, Yusheng Wu
• 5172 · PDF Mechanistic insights into PLK1 target inhibition in ovarian cancer: Functional suppression and PROTAC-based therapeutic agents jaesung Ryu, Baek MooJun, HyoWook Gil, Eunjung Yang, Kwangseock Kim, Taewan Kim, Kong Hyejeong, Beamjun Park, Jeong Kyu Bang, Seob Jeon
• 5173 Identification of a small molecule degrader targeting SALL4 oncogene Kim Anh L. Vu, Shiva Moein, Kalpana Kumari, Bee Hui Liu, Miao Liu, Chong Gao, Li Feng, Mahmoud Bassal, Douglas Auld, Dominik Casalena, Qiling Zhou, Daniel G. Tenen, Li Chai
• 5174 · PDF High-throughput capillary immunoassays enable precise quantitation of protein degrader potency and kinetics in oncology discovery Charles Haitjema, Francisco Ramirez, Bhamini Purandare, Pallavi Joshi, Chris Heger
• 5175 Discovery and characterization of once in a month intravenous and orally bioavailable SMARCA2 degraders for treating SMARCA4 mutant cancers Bilash Kuila, Kiran B. Aithal, Sandeep Vitthal Dukare, Charamanna KB, Khaji Abdul Rawoof, Prasath Kothandaraman, Amit A. Dhudashiya, Nandish C, Payel Das, Anuradha Gadeval, Madhu K L, Bhagwan Mahadeo Dhaytadak, Gopinath CH, T Jagadeesh Kumar, Suraj Tgore, Mohamad Fairus Bin Abdul Kadir, Leena Khare, Ranadeep Bokalial, Samiulla DS, Subhendu Mukherjee, Saravanan Thiyagarajan, Kavitha Nellore, Rajesh Eswarappa, Girish Daginakatte, Chandrasekhar Abbineni, Sanjeev Giri, Murali Ramachandra, Susanta Samajdar
• 5176 · PDF Selective degradation of SMARCA4 as a therapeutic strategy in SMARCA4 driven cancers Bilash Kuila, Sandeep Dukare, Kiran Aithal B, Charamanna KB, Khaji Abdul Rawoof, Amit A. Dhudashiya, Nandish C, karthik S, Payel Das, Gopinath CH, Suraj Tgore, Gauri Rahul Petkar, Mohamad Fairus Bin Abdul Kadir, Leena Khare, Ranadeep Bokalial, Samiulla DS, Subhendu Mukherjee, Saravanan Thiyagarajan, Kavitha Nellore, Rajesh Eswarappa, Girish Daginakatte, Chandrasekhar Abbineni, Sanjeev Giri, Murali Ramachandra, Susanta Samajdar
• 5177 · PDF Exceptionally selective and orally bioavailable p300 degraders for the treatment of CBP-mutant and p300-dependent cancers Iram Khan Iqbal, Krishna Chaitanya T, Kishore Narayanan, Naveen Kumar R, Aravind A. B, Avinash Kumar, Dabbeeru Madhu Babu, Pathur Obanna, Ankita Manna, Rabin Madhaiyan, Damodhran B, Shraddha B Shirsat, Shilpa S Nayak, Suraj T Gore, Mohamad Fairus, Girish Daginakatte, Rajesh Eswarappa, Chandrasekhar Abbineni, Saravanan Thiyagarajan, Murali Ramachandra, Susanta Samajdar
• 5178 · PDF Discovery and characterization of a selective p300 degrader reveals deep anti‑tumor activity in CBP mutant cancers Harshil Dhruv, Andrew Fedoriw, Xuqing Zhang, Michael Russell, Jeremy Roach, Nathan Kendsersky, Nelisa Bechtel, Kelsey Annen, Brian Vidal, Timothy Dougherty, Clemente Aguilar-Bonavides, Elham Behshad, Sudeep Banjade, Corey Strickland, Wenxue Wu, Larry Jolivette, Helai Mohammad, Ryan Kruger
• 5179 · PDF Discovery and characterization of a selective p300 degrader reveals broad anti‑tumor activity in p300‑dependent cancers Harshil Dhruv, Andrew Fedoriw, Xuqing Zhang, Michael Russell, Jeremy Roach, Nathan Kendsersky, Nelisa Bechtel, Kelsey Annen, Brian Vidal, Timothy Dougherty, Clemente Aguilar-Bonavides, Elham Behshad, Sudeep Banjade, Corey Strickland, Wenxue Wu, Larry Jolivette, Helai Mohammad, Ryan Kruger
• 5180 · PDF Engaged but not degraded: Proteome-wide CETSA in degrader research Tomas Friman, Sören Bruhn, Merve Kacal, Alexey Chernobrovkin, Daniel Martinez Molina

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