PO.CH01.01 · 化学
Targeted Protein Degradation and Induced Proximity
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4774 · PDF 在结直肠癌中靶向Beta-catenin:Coltac公司BOND+平台开发的新型分子胶候选药物 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
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5151 · PDF 设计与合成靶向携带KRAS G12D、G12V和G12C突变癌症的高效CRBN基pan-KRAS降解剂 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
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5152 · PDF 使用AUTOTAC平台靶向降解KRAS Targeted degradation of KRAS using the AUTOTAC platform Su Ran Mun, Su Jin Lee, Hyeong-Reh C. Kim, Yong Tae Kwon
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5153 · PDF 针对雄激素受体的第二代AUTOTAC用于去势抵抗性前列腺癌治疗的表征研究 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 5154 蛋白水解与基因沉默靶向嵌合体(PROGENTAC) Proteolysis and gene silencing targeting chimera (PROGENTAC) Abhay Prasad, Rong Zheng, Deeksha Satyabola, Yang Xu, Yichen Yan, Hao Yan
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5156 · PDF 用于靶向蛋白降解的FBXW7结合剂的开发 Development of FBXW7 binders for targeted protein degradation Shenghao Guo, Becky Leifer, Yichen Xiang, Angela N. Koehler
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5157 · PDF XNW34017的发现与表征:一种首创、口服生物利用度高且可穿透脑部的AURKA-MYC降解剂 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 5158 HY809382的临床前表征:一种高效、口服生物利用度高的PRC2 PROTAC,用于治疗淋巴瘤和实体瘤 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
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5159 · PDF 通过FBXO22介导的新型TEAD靶向胶(Targeted Glues™)用于间皮瘤和NSCLC治疗的合理开发 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 5161 HJ-004:一种强效、选择性的泛EGFR突变靶向蛋白降解剂(TPD),可有效克服EGFR突变型NSCLC中的奥希替尼耐药 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
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5163 · PDF 利用CBP和EP300的选择性降解实现强效抗癌活性 Leveraging selective degradation of CBP and EP300 for potent anti-cancer activity Karolina Mizeracka, Elizabeth Wittenborn, Darshan Sappal, Laura La Bonte, Danette L. Daniels
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5164 · PDF 探索新型E3连接酶以支持靶向蛋白降解药物研发 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 5166 NRX-4972,一种选择性口服Aurora激酶A降解剂,在SCLC肿瘤模型中表现出更高的疗效,并显示出比AURKA抑制剂更强的体外协同作用 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
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5167 · PDF 新型疏水性CRBN结合剂的设计与应用 Design and applications of novel hydrophobic CRBN binders Hailong Yang, Qingbo Xu, Yongqiang Wang, Zhenyu Wu, Hongbo Zhang
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5168 · PDF 拓展靶向蛋白降解的版图:E3连接酶无关的发现与专有配体鉴定 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
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5169 · PDF 作为强效选择性Helios降解剂的吡啶基苄胺类似物1的鉴定与优化 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
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5170 · PDF 靶向KRAS的小分子PROTAC的设计与优化 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 5171 EGFR-PROTAC分子TY-2719减弱对第三代EGFR TKI的获得性耐药并增强KRAS突变体抑制剂在实体瘤中的疗效 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
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5172 · PDF 卵巢癌中PLK1靶点抑制的机制洞察:功能性抑制与基于PROTAC的治疗药物 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 5173 靶向SALL4致癌基因的小分子降解剂的鉴定 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
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5174 · PDF 高通量毛细管免疫分析实现肿瘤学研发中蛋白降解剂效力与动力学的精确定量 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 5175 用于治疗SMARCA4突变型癌症的每月一次静脉给药及口服可生物利用的SMARCA2降解剂的发现与表征 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
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5176 · PDF 选择性降解SMARCA4作为SMARCA4驱动型癌症的治疗策略 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
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5177 · PDF 用于治疗CBP突变型和p300依赖型癌症的高选择性且口服可生物利用的p300降解剂 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
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5178 · PDF 一种选择性p300降解剂的发现与表征揭示其在CBP突变型癌症中的深度抗肿瘤活性 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
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5179 · PDF 一种选择性p300降解剂的发现与表征揭示其在p300依赖型癌症中的广泛抗肿瘤活性 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
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5180 · PDF 结合但未被降解:降解剂研究中的蛋白质组范围CETSA Engaged but not degraded: Proteome-wide CETSA in degrader research Tomas Friman, Sören Bruhn, Merve Kacal, Alexey Chernobrovkin, Daniel Martinez Molina