Multi-Axis Antineoplastic Agents

• 5743 · PDF Discovery of a novel orally available microtubule-destabilization agent that targets the colchicine binding site and exhibits antitumor activity in KRAS -mutant models Yeni K. Romero, Joshua W. Large, Kylie Luther, Molly M. Hood, Ranjan Preet, Chase K. Crawley, Salim Javed, Yu Mi Ahn, Forrest A. Stanley, Bertrand Le Bourdonnec, Bryan D. Smith, Daniel L. Flynn, Jeffery D. Zwicker, Stacie L. Bulfer
• 5744 · PDF Robust anti-tumor activity of the novel KIF18A inhibitor, ATX-295, in preclinical models of chromosomally instable tumors Laura Ghisolfi, Maureen M. Lynes, April Greene-Colozzi, David Sutton, Jie Wu, Livia Shehaj, Brian A. Sparling, Inbal Gazy, Stuart J. Ince, Jason A. Sager, Serena J. Silver
• 5745 · PDF Discovery of AZD4956, a potent and selective inhibitor of DNA polymerase theta, a clinical candidate for treatment of HRR-deficient tumors in combination with saruparib Bernard Barlaam, Josep V. Forment, Lee Mulderrig, de Renty Christelle, Harriet Southgate, Adina Hughes, Derek Barratt, Nina Akrap, Marcello Maresca, Oliver Turner, Dougles Ferguson, Andy Pike, Ross Hill, Lenka Oplustil O’Connor, Kainat Khan, Sonja Gill, Stefan Kavanagh, Susan Critchlow, Sabina Cosulich, David Wilson
• 5746 The risk of high-grade hyperglycemia with PI3K inhibitors-a meta-analysis Zhan Rong, Shenhong Wu
• 5747 · PDF GenSci145: A mutant selective PI3Kalpha inhibitor overcoming brain metastasis treatment barriers Xing Fan, Sheng Zhao, Xiaojing Huang, Yihui Lin, Xiaozhen Wang, Biao Lu, Yuanfeng Xia, Fanglong Yang
• 5748 · PDF PM534, a novel tubulin inhibitor, has antitumor activity in patient-derived xenograft models of soft tissue sarcoma Agathe Bouju, Daniël Gorgels, Chao-Chi (Ally) Wang, Kimberly Verbeeck, Ulla Vanleeuw, Maria J. Guillén, Carmen Cuevas, Pablo M. Avilés, Agnieszka Wozniak, Patrick Schöffski
• 5749 · PDF DNA damage, apoptosis and cell cycle disruption: Antitumor effects of a novel tin(IV) complexes Shubham Sharma, Margret H. Ogmundsdottir, Helga M. Ögmundsdottir, Krishna Kumar Damodaran
• 5750 · PDF Solid tumor cell-intrinsic function of PI3Kdelta Sarah E. Conduit, Elena Lopez-Guadamillas, Daniele Morelli, Harriet Howard, Wayne Pearce, Cheryl Scudamore, Bart Vanhaesebroeck
• 5751 · PDF (E,E)-bisantrene silences c-MYC expression by stabilizing its promotor region G-quadruplex Sumit Sahni, Emily Ryan, Peter Cuthbertson, Feroz Ahmad, Kirsten Curnow, Nehad Elsalamouny, Qiang Zhu, Haibo Yu, Jinho Jang, Jonathan Dickerhoff, Danzhou Yang, Emma-Jayne Proctor, Martina Sanderson-Smith, Daniel Tillett, Michael Kelso
• 5752 · PDF Bi-functional thiopurine-based oligonucleotides for AML cell-targeted telomere damage and immunostimulation Chunsong Yu, Elaine Y. Kang, Piotr Swiderski, Haiqing Li, Ya-Huei Kuo, Guido Marcucci, Marcin Kortylewski
• 5753 · PDF Clinical-stage anticancer agent BOLD-100 demonstrates protective effects against chemotherapy-induced peripheral neuropathy Mark Bazett, Ashish Kumar, Josie C. Setiawan, E. Russell McAllister, Jim Pankovich
• 5754 · PDF PM54 suppresses WNT/beta-catenin signaling and synergizes with chemotherapy in gastric cancer models Francisco Javier Gutierrez Alvarez, Gema Santamaria, Marta Martínez Diez, Maria José Guillen, Pablo Avilés, Marcelo L. Ribeiro, Carmen Cuevas
• 5755 · PDF MTORC1/2 inhibition enhances STX-478, a PIK3CA H1047R mutant inhibitor, in PIK3CA H1047R mutant colorectal cancer Alexa E. Schmitz, Addison Zick, Cheri A. Pasch, Dustin A. Deming
• 5756 · PDF Preclinical evaluation of BH4601, a novel tetravalent PD-L1 and B7H3 bispecific antibody-drug conjugate (ADC) with Topo1 inhibitor for the treatment of solid tumors Jun Wang, Pengfei Rong, Jing Wang, Yang Liu, Mengrui Zhao, Jie Feng, Lijuan Li, Yue Wang, Aihong Zhang, Dongyang Li, Hongjuan Zhang, Jingmei Cai, Xiaochun Li, Jiangcheng Xu, Jiawang Liu, Hui Ding, Fangxing Ouyang, Kyoungwoo Lee
• 5757 · PDF Exatecan payload-based antibody-drug conjugates with a short hydrophilic beta-glucuronidase cleavable linker Vasu Jammalamadaka, Jiang Liu, Sunil Bhakta, Vidya S. Jonnalagadda, Jagath R. Junutula
• 5758 Single protein encapsulated SN38: Extremely effective anticancer drug with low toxicity C. J. Yu, leslie Wang, Kinsley Wang, Mengmeng Liu, Faqing Huang, Warren A. Chow, Xiaojiang Cui
• 5759 · PDF Genome-wide CRISPR screen identifies GPX4 as a potential vulnerability in cells treated with PI3Kalpha-mutant selective inhibitor RLY-2608 Fabiana Napolitano, Yuan Wang, Dan Ye, Jingxuan Lu, JINGXUAN CHEN, Khushi Ahuja, Pamela Luna, Yuki Matsunaga, Dylan Calhoon, María Rosario Chica-Parrado, Yasuaki Uemoto, Javier Garcia Bermudez, Jeon Lee, Chang-Ching A. Lin, Ariella B. Hanker, Carlos L. Arteaga
• 5760 · PDF Metabolic rewiring renders KEAP1 -mutant lung cancers sensitive to AKR1C3-activated prodrugs Michela Ranieri, Matthew Cattle, Doyeon Jang, Kwok-Kin Wong, Charles M. Rudin, John Thomas Poirier
• 5762 · PDF FMC-242, a highly potent and selective covalent inhibitor of the PI3Kalpha -RAS interaction, demonstrates robust anti-tumor activity as monotherapy and in combination with targeted therapies Kevin R. Webster, Ryan McFadden, Abdul Awol, Koli Basu, Barun Bhhatarai, Yu-Hsin Chao, John Conway, Jay Duffner, Dan Erlanson, Robert Everley, Susan Fong, Sarah Gilfillan, Johannes Hermann, Alessandra Ianari, Lata Jayaraman, Svetlana Kholodar, Nathan Lavey, Tiep Le, Laura Marholz, Bethany Parker, Snahel Patel, Emily Sabbey, Shefali Sabhlok, Shayna Simonstein, Luke Utley, John Vassiliadis, Weiru Wang, Yan Wang
• 5763 · PDF Roginolisib stabilizes inactive PI3Kdelta to deliver specific target blockade with reduced immune toxicity Giusy Di Conza, Oscar Vadas, Simon Tiede, Elise Solli, Maria Chaouki, Laura Tesmer, Shanlin Rao, Remy Visentin, Mathias Wenes, Denis Migliorini, Sigrid S. Skånland, Anne Quillet-Mary, Loïc Ysebaert, Julie Guillermet-Guibert, Alessio Bevilacqua, Lars van der Veen, Michael Lahn, Kjetil Tasken, Gerhard Hummer
• 5764 · PDF Evaluating the molecular mechanism of axitinib response in head and neck squamous cell carcinoma Behirda Karaj, Jiayu Wang, Paul L. Swiecicki, An-Yun Teng, J. Chad Brenner
• 5765 · PDF Discovery of QLS1522, a mutant-selective allosteric PI3Kalpha inhibitor for the treatment of PIK3CA-mutant solid tumors Yuxing Zhang, Hua Qin, Jiasheng Fu, Naijie Fu, Difei Dong, Changliang He, Lan Zhang, Yu Zhang, Ling Li, Jun Mao, Jianping Chen, Weibo Zhu, Dong Yang, Xinghua Cheng, Guqin Shi, Jinxiao Bao, Ying Wang, Ping Chen, Su Qian, Liang Xie, Daqing Sun, Weikang Tao
• 5766 · PDF Network‑level kinase activity associate with differential drug sensitivity in B-Cell lymphoma cell lines Simar Pal Singh, Laken Woods, Robin Keijzers, Gitanjali Dharmadhikari, Dóra Schuller, Rik de Wijn
• 5767 · PDF Combining SUMO inhibition and irinotecan increases pancreatic cancer cytotoxicity Asimina Courelli, Leonie Ren, Herve Tiriac, Yuan Chen, Andrew Lowy
• 5768 · PDF Repurposing veratridine, a previously used antihypertensive supplement, for effective treatment of metastatic colorectal cancer Morgan Eikanger, Khosrow S. Rezvani
• 5769 · PDF A potent TOP2 poison with robust preclinical efficacy and a favorable therapeutic window supporting clinical evaluation in pancreatic cancer Krzysztof Grela, Stanislaw Skora, Izabela Fokt, Edd Felix, Zofia Zielinska, Mihai G. Iurascu, Mateusz Kwasnik, Rafal Zielinski, Waldemar Priebe
• 5770 Design, synthesis, and biological investigation of a new class of duocarmycin payloads for ADC development Goreti R. Morais, David Pajtas, Enric A. Picher, Sneha Smarakan, Robert A. Falconer, Klaus Pors
• 7780 The first-in-class covalent peroxiredoxin 3 (PRX3) inhibitor RSO-021 modulates immune phenotypes in mesothelioma Victoria Gibson, Joanna Dzialo, Aida Habibovic, Christopher Landry, Dean Fennell, Brian Cunniff

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