Novel Antitumor Agents 1

• 398 · PDF NOVO-111：一种为改善肿瘤靶向性和耐受性而设计的大环药物偶联物 NOVO-111: A macrocycle drug conjugate engineered for improved tumor targeting and tolerability Jonathan Felipe Aramubla, Guangan He, Gregory Thiabaud, Kathryn Shelton, Luke J. Segura, Jonathan L. Sessler, Rick A. Finch, Zahid H. Siddik
• 399 · PDF 环巴胺酒石酸盐增强抗肿瘤免疫并抑制三阴性乳腺癌生长 Cyclopamine tartrate enhances antitumor immunity and suppresses triple-negative breast cancer growth Tianyuan Wang, Lorena Arango, Li Liu
• 400 · PDF 以替莫唑胺（TMZ）联合 5-乙炔基-2'-脱氧尿苷（EdU）治疗胶质母细胞瘤 Combinatorial treatment of glioblastoma with temozolomide (TMZ) plus 5-ethynyl-2'-deoxyuridine (EdU) Humeyra Kaanoglu, Yasemin Akyel, Adebimpe Adefolaju, Alain Valdivia, Dominique Higgins, Shawn D. Hingtgen, Andrew B. Satterlee, Aziz Sancar
• 401 · PDF 靶向 Hsp90beta 增强胰腺癌模型对 nab-紫杉醇为基础化疗的反应 Targeting Hsp90beta potentiates nab-paclitaxel-based chemotherapy response in pancreatic cancer models Mayra Garcia, Nicola Grimaldi, Nathan Tuchscherer, Md Sazzad Hassan, Urs von Holzen, Brain Blagg, Niranjan Awasthi
• 402 · PDF 发现 JMKX005425——一种在多种 MSI-H 胃癌模型中高效的强效 WRN 抑制剂 Discovery of JMKX005425, a potent WRN inhibitor highly efficacious in multiple MSI-H gastric cancer models Liyan Yue, Xiaoqin Lin, Xinfeng Liu, Yangyang Qiu, Shurong Yang, Dongdong Li, Wei Chen, Taylor B. Guo, Jianbiao Peng
• 403 · PDF 苯并吡喃衍生物的合成与抗癌筛选 Synthesis and anti-cancer screening of benzopyran derivatives Razia Shaika, Brijesh Sharma, Mariappan Gurusamy
• 404 · PDF 非辛辣的 N-AVAM 辣椒素类似物 DOHEVANIL 在体外和体内对人子宫内膜样卵巢癌显示出强效的生长抑制活性 The non-pungent N-AVAM capsaicin analog DOHEVANIL displays robust growth-suppressive activity in human endrometriod ovarian cancers in vitro and in vivo Kaitlyn Conley, Sarah L. Miles, Rama S. Gadepalli, John M. Rimoldi, Timothy E. Long, Yi Charlie Chen, Piyali Dasgupta
• 405 · PDF (Z)-endoxifen 调节雌激素受体和细胞周期信号，在子宫内膜癌模型中与 CDK4/6 抑制产生协同抗增殖效应 (Z)-endoxifen modulates estrogen receptor and cell-cycle signaling to induce synergistic antiproliferative effects with CDK4/6 inhibition in endometrial cancer models Grace Choong, Xiaonan Hou, Sandra Suarez Hammer, Scott M. Blackburn, John Weroha, Steven C. Quay
• 406 · PDF 发现强效、选择性 TRIB2 抑制剂,对治疗耐药的神经内分泌前列腺癌具有治疗疗效 Discovery of potent and selective TRIB2 inhibitors with therapeutic efficacy in therapy-resistant neuroendocrine prostate cancer Jitender Monga, Sang-Yoon Lee, Sharad K. Suthar, Sudha Sadasivan, Shirish Gadgeel, Craig Rogers
• 407 407 靶向 AhR 抑制 EGFR 突变型肺癌中 amivantamab-lazertinib 诱导的耐药持留细胞的产生 Targeting AhR suppresses the generation of amivantamab-lazertinib-induced drug-tolerant persisters in EGFR-mutant lung cancer Joo Sung Shim, Mi Hyun Kim, Heekyung Han, Seongsu Jeong, Jae-Hwan Kim, Mi Ran Yun, Sun Min Lim, Byoung Chul Cho
• 408 · PDF 发现同类首创的微管与 RAF 双靶点抑制剂 Discovery of a first-in-class dual microtubule- and RAF-targeting inhibitor Joshua W. Large, Yeni K. Romero, Kylie Luther, Molly M. Hood, Ranjan Preet, Cale L. Heiniger, Chase K. Crawley, Salim Javed, Yu Mi Ahn, Cynthia B. Leary, Forrrest A. Stanley, Justin T. Proto, Lakshminarayana Vogeti, Bertrand Le Bourdonnec, Bryan D. Smith, Daniel L. Flynn, Jeffery D. Zwicker, Stacie L. Bulfer
• 409 · PDF 使用 HMCD-青蒿素偶联物对转移性去势抵抗性前列腺癌进行亚细胞靶向治疗 Subcellular targeted therapy using HMCD-artemisinin conjugates for metastatic castration-resistant prostate cancer Yan Ou, Adrian Lim, Mouad Edderkaoui, Ruoxiang Wang, Qiang Wang, Stephen J. Pandol, Yi Zhang
• 410 · PDF CGT1263 的表征:一种对突变型 KRAS 具有选择性(优于 HRAS 和 NRAS)的 KRAS(ON/OFF)抑制剂临床候选药物 Characterization of CGT1263, a KRAS (ON/OFF) inhibitor clinical candidate with selectivity for mutant KRAS over HRAS and NRAS John Fischer, Kim Alley, Karyn Bouhana, Richard Brizendine, Paul Carlson, Mark Chicarelli, Michelle Crow, Brad Fell, Jennifer Fulton, Anna Guarnieri, Jackie Harrison, Ravi Jalluri, Amber Johnson, Keith Koch, Cori Malinky, Macedonio J. Mejia, Brad Newhouse, Scott Niman, Rob Rieger, John Robinson, Mareli Rodriguez, Leah Salituro, Vinny Scarato, Aaron Smith, Francis Sullivan, Yang Wang, Shannon Winski, Silas Wood, Yeyun Zhou
• 412 412 丹参酮类似物通过抑制 MYC 和 E2F 通路诱导 ER 应激介导的前列腺癌细胞生长抑制 Tanshinone analog induces ER stress mediated growth suppression via inhibition of MYC and E2F pathways in prostate cancer cells Ching-Feng Cheng, Hui-Chen Ku, Guo-Zhou Cheng
• 413 · PDF ADT-007:一种机制独特的泛 RAS 抑制剂,具有逃避其他 RAS 抑制剂共有的获得性耐药的能力 ADT-007: A mechanistically distinct Pan-RAS inhibitor with capacity to escape acquired resistance common to other RAS inhibitors Junwei Wang, Xi Chen, Sindhu Ramesh, Jeremy B. Foote, Chung-Hui Huang, Kristy L. Berry, Khalda Fadlalla, Dhana Sekhar Reddy Bandi, Purnachandra Ganji, Elmar Nurmemmedov, Ivan Babic, Donald Buchsbaum, Asfar S. Azmi, Yulia Y. Maxuitenko, Adam B Keeton, Bassel El-Rayes, Gary A. Piazza
• 414 · PDF QED-203:一种用于标准治疗耐药的晚期前列腺癌的 TRPV6 与 AR 双靶点小分子临床前候选药物 QED-203, a dual TRPV6 and AR small molecule preclinical candidate for advanced prostate cancer resistant to standard of care Kimberley Beaumont, Rebecca Pouwer, Mei Yeh, Melanie Robitaille, Rebecca Farrow, Matthew McLachlan, Therese Johnson, Akanksha Upadhyaya, Aaron Gregson, Raphael Rahmani, Claire Levrier, Hasanthi Wijesekera, Malika Kumasiri, Grant Stuchbury, Terrie-Anne Cock, Andrew Harvey, Gregory Monteith, Brian Dymock
• 415 · PDF VLS-1488与紫杉烷类联合在癌细胞中诱导抗肿瘤协同效应 Combination of VLS-1488 and taxanes induces anti-tumor synergistic effect in cancer cells Song Chen, Adriana Roopnariane, Arshi Arora, Samuel Bakhoum, Timothy Bowler, Sarah Bettigole, Scott Drutman, Celia Andreu-Agullo
• 416 · PDF HEC201625——一种新型口服PD-L1小分子抑制剂，在体外和体内均表现出强效抗肿瘤活性 HEC201625, a novel oral small molecule inhibitor of PD-L1, demonstrated potent anti-tumor activities both in vitro and in vivo Bing Liu, Mingyu Guan, Shaoyan Li, Ning Kang, Ming Li, Ying Zeng, Jing Li, Cliff Cheng, Yingjun Zhang, Kai Lin
• 417 · PDF 结构导向设计的JZY3032——一种在前列腺癌中使AR-p300错误连接的双重结合DALTAC Structure-guided design of JZY3032, a dual-engaging DALTAC that miswires AR-p300 in prostate cancer Jianzhang Yang, Jie Luo, Mi Wang, Shicheng Jin, Arul M. Chinnaiyan, Shaomeng Wang
• 418 · PDF ETX-929——一种潜在同类最优的口服、高强效且选择性的双ON/OFF状态泛KRAS小分子抑制剂，用于治疗KRAS突变型及野生型扩增型癌症 ETX-929, a potential best-In-class, oral, highly potent and selective dual ON / OFF state Pan-KRAS small molecule inhibitor for the treatment of KRAS mutant and wild-type amplified cancers Meghana M. Kulkarni, Lei Cui, Hongbo Deng, Tao Liu, Jingyan Gao, Fei Peng, Ying Lin, Yong Tang, Karan Kapoor, Minghong Hao, Robert F. Koncar, Robbie Chen, Eric Simone, Raj Nagaraja, Shengfang Jin, Jeffery Kutok
• 419 · PDF 使用新型抑制剂RPT-E-037靶向NAMPT治疗胰腺神经内分泌肿瘤 Targeting NAMPT using Novel Inhibitor RPT-E-037 in Pancreatic Neuroendocrine Tumor Md Hafiz Uddin, Husain Yar Khan, Amro Aboukameel, Sahar F. Bannoura, Irfana Muqbil, Hugo Jimenez, Filza Khan, Rafic Beydoun, Gregory Dyson, Yang Shi, Mohammed N. Al Hallack, Nitin Vaishampayan, Ibrahim Azar, Steve Kim, Eliza W. Bael, Miguel Tobon, Khalil Choucair, Walid Sukkari, Hafsa Imtiaz, Herbert Chen, Muhammad W. Saif, Anthony Frank Shields, Ramzi M. Mohammad, Philip Philip, Bassel F. El Rayes, Min Wu, Michael Schelle, Boris Pasche, Asfar S. Azmi
• 420 · PDF 通过miRNA-CSC轴靶向增殖细胞核抗原作为多发性骨髓瘤的一种新治疗策略 Targeting proliferating cell nuclear antigen via a miRNA-CSC axis as a new therapeutic approach in multiple myeloma Jeffrey A. Zonder, Bin Bao, Amro Aboukameel, Sahar F. Bannoura, MD Hafiz Uddin, Husain Y. Khan, Rayyan Siddiqui, Yin Wan, Yang Shi, Ramzi Mohammad, Long Gu, Pouya Haratipour, Robert J. Hickey, Linda Malkas, Asfar Azmi
• 421 · PDF Kirsten大鼠肉瘤病毒（KRAS）癌蛋白作为多发性骨髓瘤的一种新治疗靶点 Kirsten rat sarcoma virus (KRAS) oncoprotein as a new therapeutic target in multiple myeloma Jeffreay Zonder, Bin Bao, Amro AbouKameel, Sahar Bannoura, Husain Y. Khan, MD Hafiz Uddin, Walid M. Sukkari, Ramzi Mohammad, Long Gu, Pouya Haratipour, Robert J. Hickey, Linda Malkas, Asfar S. Azmi
• 422 · PDF 一种新型强效四氢异喹啉类似物：一种细胞抑制性紫杉醇样药物 A novel potent tetrahydroisoquinoline analog: A cytostatic taxol-like agent Kinfe K. Redda, Madhavi Gangapuram, Suresh Eyunni, Elizabeth Mazzio, Karam F. A. Soliman
• 423 · PDF ETX-880：一种潜在的同类最佳、口服、高效且选择性的Werner解旋酶共价抑制剂，用于治疗微卫星高度不稳定（MSI-H）癌症 ETX-880, a potential best-in-class, oral, highly potent and selective covalent inhibitor of Werner helicase for the treatment of microsatellite instability-high (MSI-H) cancers Robert F. Koncar, Daliya Banerjee, Mingzong Li, Tao Liu, Upul Bandarage, Alexandra Weinheimer, Jingyan Gao, Fei Peng, Ying Lin, Yong Tang, Karan Kapoor, Minghong Hao, Robbie Chen, Eric Simone, Raj Nagaraja, Shengfang Jin, Meghana M. Kulkarni, Jeffery Kutok
• 424 · PDF 利用一种新型酮康唑衍生物靶向乳腺癌脑转移中的tGLI1 Targeting tGLI1 in breast cancer brain metastases with a novel ketoconazole derivative Mariana Najjar, Daniel Doheny, Sara Manore, Joshua Cha, Phi-Long Tran, Elissa Bloom, Hui-Wen Lo
• 425 · PDF ISM6166：一种借助生成式AI发现的新型口服pan-KRAS（ON/OFF）抑制剂，在具有KRAS改变的实体瘤中显示出强劲的抗肿瘤活性 ISM6166, a novel oral pan-KRAS (ON/OFF) inhibitor discovered with generative AI shows robust anti-tumor activity in solid tumors with KRAS alterations Sujing Shi, Defeng Shen, Jianping Wu, Tingting Liu, Jinxin Liu, Qingshuo Meng, Zuoxiao Shi, Suguna Rachakonda, David Gennert, Luoheng Qin, Xin Cai, Man Zhang, Feng Ren, Alex Zhavoronkov
• 426 · PDF 开发基于七甲川碳菁的小分子靶向平台用于肿瘤特异性药物递送 Development of heptamethine carbocyanine based small molecule targeting platform for tumor specific drug delivery Paul Algate, Jeffrey A. Kern, Lyle Small, Ruizheng Wang, Ryan Westberry, Margaret Karow, Steve LaMond
• 427 · PDF PMR-116：一种在广谱恶性肿瘤中显示疗效的第二代RNA聚合酶I抑制剂 PMR-116, a second-generation RNA polymerase I inhibitor displaying therapeutic efficacy in a broad spectrum of malignancies Nadine Hein, Rita Ferreira, Amee George, Katherine Hannan, Karagh Loring-White, Konstantin Panov, Eric Kusnadi, Richard Rebello, Alisee Huglo, Shelley Hedwards, Mitchell Lawrence, Mustapha Haddach, Denis Drygin, Ross D. Hannan, Luc Furic

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