PO.ET09.06 · 实验与分子治疗
Novel Antitumor Agents 1
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398 · PDF 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
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399 · PDF Cyclopamine tartrate enhances antitumor immunity and suppresses triple-negative breast cancer growth Tianyuan Wang, Lorena Arango, Li Liu
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400 · PDF 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
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401 · PDF 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
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402 · PDF 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
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403 · PDF Synthesis and anti-cancer screening of benzopyran derivatives Razia Shaika, Brijesh Sharma, Mariappan Gurusamy
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404 · PDF 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
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405 · PDF (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
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406 · PDF 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 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
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408 · PDF 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
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409 · PDF 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
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410 · PDF 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 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
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413 · PDF 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
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414 · PDF 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
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415 · PDF 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
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416 · PDF 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
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417 · PDF 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
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418 · PDF 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
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419 · PDF 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
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420 · PDF 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
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421 · PDF 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
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422 · PDF A novel potent tetrahydroisoquinoline analog: A cytostatic taxol-like agent Kinfe K. Redda, Madhavi Gangapuram, Suresh Eyunni, Elizabeth Mazzio, Karam F. A. Soliman
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423 · PDF 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
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424 · PDF 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
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425 · PDF 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
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426 · PDF 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
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427 · PDF 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