Proximity-Induced Drug Discovery 2

• 5774 · PDF 发现具有卓越抗白血病疗效的强效CDK8/CDK19 PROTAC降解剂 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 当CDK遇上CIP：将靶点结合与功能结局相联系——CDK2分子胶与CDK-TCIP 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 发现一种口服生物利用度高、具有持久体内疗效和转化潜力的AKT降解剂 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 PLK1在结直肠癌进展中的功能作用及其对化疗耐药的潜在影响 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-690：一种三元复合物分子胶泛RAS（ON）抑制剂，在RAS依赖性实体瘤中展现出同类最佳潜力 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-869：一种高效、选择性、口服生物利用度高的共价KRAS G12D（ON状态）抑制剂，在KRAS G12D驱动的实体瘤临床前模型中具有强健的抗肿瘤活性 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 发现ATH-007，一种新型、强效、高选择性的CCNE1分子胶，展现出强健的抗肿瘤活性和更佳的安全性特征 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-7138：一种用于胰腺导管腺癌靶向治疗的新型GSPT1/ZFP91双靶点分子胶降解剂 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 基于机器学习和结构导向发现用于癌症治疗的EP300选择性、口服生物利用的降解剂 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 HY809382：一种具有同类最佳性质的PRC2降解剂，在多种肿瘤中显示疗效并克服由EZH2基因突变引起的EZH2抑制剂临床耐药 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 发现FX-111：一种同类首创的转录活性雄激素受体（AR ON）异双功能降解剂，用于治疗AR驱动的前列腺癌患者 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降解剂对神经母细胞瘤的抗癌活性：CDKN2A/B缺失作为一种生物标志物 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 通过多组学分析鉴定新型非CRBN依赖的分子胶及相应E3连接酶靶点解卷积 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-611：一种处于开发阶段的ALK分子胶降解剂，促进TKI耐药的ALK融合蛋白降解并导致ALK TKI难治性肿瘤消退 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 新型分子胶的理性发现 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 发现一种选择性靶向CCNE1的分子胶降解剂，用于治疗CCNE1扩增的实体瘤和CDK4/6i耐药的HR+/HER2-乳腺癌 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 通过定向降解实现下一代PRMT5活性调控 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 NEO-811的临床前表征——一种新型ARNT分子胶降解剂，用于治疗透明细胞肾细胞癌 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 鉴定首创（first-in-class）的选择性ARID1B降解剂 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 首创强效、选择性口服KAT6A降解剂开发候选药物PRT13722作为单药驱动完全的肿瘤消退，并具有改善的临床前血液学安全性特征 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 利用E2连接酶实现诱导邻近效应并调控新型癌症相关靶点和新底物 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 BLU-020的发现：一种强效、选择性的CDK2降解剂，用于治疗CCNE1异常癌症 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 靶向Rpn13Pru的小分子诱导乳腺癌细胞有丝分裂阻滞 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 首创CDK9降解剂TB-008在异种移植模型中的PK/PD及临床前ADME特征研究 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 通过肽诱导清除实现细胞表面蛋白的靶向蛋白降解 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 基于Lumit的降解剂动力学分析揭示对降解剂的信号依赖性、细胞背景特异性敏感性 Lumit-based profiling of degrader dynamics reveals signaling-dependent, cell context-specific sensitivity to degraders Matthew Swiatnicki, Laurie Engel, Hicham Zegzouti
• 5800 · PDF 通过蛋白优先的共进化引导E3连接酶招募发现泛KRAS分子胶降解剂 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是一种口服生物利用度良好的泛突变体BRAF降解剂，在Class 1/2/3 BRAF突变癌症中表现出单药及与MEKi或抗EGFR联合的疗效 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 泛RAF-MEK分子胶的长效注射剂：节拍式暴露用于治疗胰腺导管腺癌 Long acting injectable of pan-RAF-MEK molecular-glue: Metronomic exposure for the treatment of pancreatic ductal adenocarcinoma Drishti Rathod, Ketankumar Patel
• 5803 · PDF 发现一种旁系同源物选择性的p300蛋白降解剂，在血液系统恶性肿瘤中具有强效的抗癌活性 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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