Multi-Axis Antineoplastic Agents

• 5743 · PDF 发现一种新型口服可利用的微管去稳定剂，靶向秋水仙碱结合位点并在KRAS突变模型中表现出抗肿瘤活性 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 新型KIF18A抑制剂ATX-295在染色体不稳定肿瘤临床前模型中展现出强效抗肿瘤活性 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 AZD4956的发现：一种强效、选择性的DNA聚合酶theta抑制剂，作为与saruparib联合治疗HRR缺陷肿瘤的临床候选药物 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 5746 PI3K抑制剂致高级别高血糖的风险——一项meta分析 The risk of high-grade hyperglycemia with PI3K inhibitors-a meta-analysis Zhan Rong, Shenhong Wu
• 5747 · PDF GenSci145：一种克服脑转移治疗障碍的突变选择性PI3Kalpha抑制剂 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 新型微管蛋白抑制剂PM534在软组织肉瘤患者来源异种移植模型中具有抗肿瘤活性 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损伤、凋亡和细胞周期紊乱：一种新型锡(IV)配合物的抗肿瘤效应 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 PI3Kdelta的实体瘤细胞内在功能 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通过稳定c-MYC启动子区G-四链体沉默c-MYC表达 (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 用于AML细胞靶向端粒损伤及免疫刺激的双功能巯基嘌呤类寡核苷酸 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 临床阶段抗癌药物BOLD-100对化疗诱导的周围神经病变具有保护作用 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抑制WNT/beta-catenin信号传导并在胃癌模型中与化疗产生协同作用 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抑制增强STX-478（一种PIK3CA H1047R突变体抑制剂）在PIK3CA H1047R突变型结直肠癌中的作用 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 BH4601的临床前评估：一种新型四价PD-L1和B7H3双特异性抗体药物偶联物（ADC），携带Topo1抑制剂用于治疗实体瘤 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 基于exatecan载药、采用短亲水性beta-葡萄糖醛酸酶可切割连接子的抗体药物偶联物 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 5758 单蛋白包封的SN38：极其有效且低毒性的抗癌药物 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 全基因组CRISPR筛选确定GPX4为经PI3Kalpha突变体选择性抑制剂RLY-2608处理的细胞中的潜在脆弱性 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 代谢重编程使KEAP1突变型肺癌对AKR1C3激活的前药敏感 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-242，一种高效选择性的PI3Kalpha-RAS相互作用共价抑制剂，作为单药及与靶向疗法联用均显示出强劲的抗肿瘤活性 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稳定失活状态的PI3Kdelta，实现特异性靶点阻断并降低免疫毒性 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 评估axitinib在头颈部鳞状细胞癌中反应的分子机制 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 QLS1522的发现，一种用于治疗PIK3CA突变型实体瘤的突变选择性变构PI3Kalpha抑制剂 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 网络水平的激酶活性与B细胞淋巴瘤细胞系的差异性药物敏感性相关 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 联合SUMO抑制与伊立替康增强胰腺癌细胞毒性 Combining SUMO inhibition and irinotecan increases pancreatic cancer cytotoxicity Asimina Courelli, Leonie Ren, Herve Tiriac, Yuan Chen, Andrew Lowy
• 5768 · PDF 将veratridine（一种既往使用的抗高血压补充剂）重新利用于转移性结直肠癌的有效治疗 Repurposing veratridine, a previously used antihypertensive supplement, for effective treatment of metastatic colorectal cancer Morgan Eikanger, Khosrow S. Rezvani
• 5769 · PDF 一种强效TOP2毒剂，具有稳健的临床前疗效和良好的治疗窗口，支持在胰腺癌中开展临床评估 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 5770 用于ADC开发的一类新型duocarmycin有效载荷的设计、合成与生物学研究 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 7780 同类首创的共价过氧化物还原酶3（PRX3）抑制剂RSO-021调节间皮瘤中的免疫表型 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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