PO.ET09.10 · 实验与分子治疗
Tyrosine Kinase, Phosphatase, and Other Inhibitors
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5863 · PDF zipalertinib与amivantamab联合在EGFR突变NSCLC模型中增强的抗肿瘤活性 Enhanced antitumor activity of zipalertinib and amivantamab combination in EGFR mutant NSCLC models Kohei Hayashi, Yoshimi Aoyagi, Akihiro Hashimoto, Tomoaki Hitotsumachi, Shuichi Ohkubo
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5864 · PDF Taletrectinib,一种新一代选择性ROS1抑制剂,在ROS1融合模型中展现出差异化特征 Taletrectinib, a next generation selective ROS1 inhibitor, demonstrates a differentiated profile in ROS1 fusion models Hitisha Patel, Laura Heller, Kevin Bowman, Zheyi Hu, Irma M. Grossi, Max Pan, Gary Hattersley
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5865 · PDF 开发COUPLrs——双弹头半胱氨酸反应性化合物,通过相互作用调节和降解靶向致癌蛋白 Developing COUPLrs, dual-warhead cysteine-reactive compounds, to target oncoproteins through interaction modulation and degradation Diane Yang, Stefan Andrew Harry, Harrison Byron Chong, Edwin Zhang, Natalie Shannon Nordenfelt, Stefan Kaluziak, Elizabeth Codd, Nicholas Chen, Samay Trivedi, Wenxin Yang, Abigail Elizabeth Smith, Alexander Daniel Carlin, Dawn R. Mitchell, Neha Khandelwal, Brian B. Liau, Liron Bar-Peled, A. John Iafrate
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5866 · PDF pan-KRAS抑制剂AMG 410在KRAS突变癌症中的临床前联合策略 Preclinical combination approaches with the pan-KRAS inhibitor AMG 410 in KRAS- mutant cancers Ying-Chu Chen, Tao Osgood, Kevin Gaida, Gilbert Diaz, Chun Su, Elissa Swearingen, Daniel Lu, Deanna Mohn, Anne Y. Saiki, Monica Leavitt, Upendra P. Dahal, Ryan P. Wurz, Brian A. Lanman, Jason DeVoss, Karen Rex, Paul E. Hughes, Rati Verma
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5867 · PDF IN10028,为治疗实体瘤而发现的新一代FAK抑制剂 IN10028, a next-generation FAK inhibitor discovered for the treatment of solid tumors Baoyuan Zhang, Hao Wang, Jiaming Gao, Fengmin Xi, Liyuan Liu, Leo Liu, Zaiqi Wang
- 5868 5868 蛋白质组学分析与疗效评估揭示lasmotinib联合menin抑制剂对AML具有强协同抗白血病活性 Proteomic analysis and efficacy evaluation reveal strong synergistic anti-leukemic activity of lasmotinib combined with menin inhibitors for AML An-Na Moon, Hee-sun Hwang, Ky-Youb Nam, KyungMin Cha, Sang Beom Lee, ChongChul Chai, Jinsun Kwon, Kyu-Tae Kim, June H. Han, Jeong Hyeok Yoon
- 5869 5869 CGT4255的临床前特征描述:一种不影响EGFR的泛突变HER2临床开发候选药物,具有潜在同类最佳的脑渗透性 Preclinical characterization of CGT4255, an EGFR sparing, pan-mutant HER2 clinical development candidate with potential best-in-class brain penetration Paul Larsen, Tanna Bettendorf, Abiezer Blandon, Karyn Bouhana, Richard K. Brizendine, Eric Brown, LouAnn Cable, Mark J. Chicarelli, Michelle Crow, Brad Fell, John Fischer, Jennifer Fulton, Anna Guarnieri, Jackie Harrison, Leyla Haygood, Ravi Jalluri, Vijay Kumar, Cori A. Malinky, Maralee McVean, Rob Rieger, John Robinson, Lee Stunkard, Francis Sullivan, John I. Trujillo, Logan E. Vine, Shannon Winski, Yeyun Zhou
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5870 · PDF Momelotinib:独特的多重药理学及针对骨髓纤维化及其他疾病的新型联合策略 Momelotinib: Unique polypharmacology and novel combination strategies for myelofibrosis and beyond Shane O'Brien, Shannon McKearnan, Ashley Lento, Jeffrey Guss, Anna Waszkiewicz, Bin Wu, Allison Hartman, Matthew Powell, Gabriella Cifelli, Maggie Connelly, Hoang Tran, Bryan Strouse, Dwaipayan Patnaik, Mary Antonysamy, Anthony Mazurek, Michael T. McCabe
- 5871 5871 firmonertinib的发现与特征描述:一种对EGFR经典突变和exon 20插入突变均具有广泛活性的新型EGFR抑制剂 Discovery and characterization of firmonertinib, a novel EGFR inhibitor with broad activity against both EGFR classical and exon 20 insertion mutations Huibing Luo, Qing Li, Qiufeng Liu, Huayong Zhou, Yuting Sun, Jerry Y. Hsu, Luna Musib, Marcin Kowanetz, Stuart Lutzker, Zineb Mounir
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5872 · PDF CLK抑制剂BH-30236在临床前AML和CLL模型中通过剪接调控与venetoclax协同发挥抗白血病活性 CLK inhibitor BH-30236 synergizes with venetoclax in anti-leukemia activity via splicing modulation in preclinical AML and CLL models Wei Deng, Ping Jiang, Zhenping Wang, Yue Hu, Nancy Ling, Danan Li, Joshua Choi, Eugene Y. Rui, Zachary Zimmerman, Geoffrey Oxnard, J. Jean Cui
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5873 · PDF OB-001增强多种TKI的脑渗透 OB-001 boost the brain penetration of multiple TKIs Hitesh Mistry, Jim Millen, Josh Fleet, Mark Brimble
- 5875 5875 多激酶抑制剂olverembatinib(HQP1351)在套细胞淋巴瘤(MCL)临床前模型中有效并与BTK抑制剂acalabrutinib协同 Multikinase inhibitor olverembatinib (HQP1351) is efficacious and synergizes with BTK inhibitor acalabrutinib in mantle cell lymphoma (MCL) preclinical models Bo Peng, Zhiyan Liang, Yan Xiong, Bingxing Wu, Shujie He, Zhou Yu, Guoqin Zhai, Dajun Yang, Yifan Zhai
- 5876 5876 阻断可溶性TNF作为增强酪氨酸激酶抑制剂应答并控制HER2阳性乳腺癌转移负荷的策略 Soluble TNF blockade as a strategy to enhance tyrosine-kinase inhibitor response and control metastatic burden in HER2-positive breast cancer Sofia Bruni, Marla Ladera, Camila Jencquel, Federico Waisberg, Martin A. Rivas, Roxana Schillaci, Maria Florencia Mercogliano
- 5877 5877 BH-30643:一种新型大环非共价、突变体选择性EGFR抑制剂,解决当代EGFR TKI在耐药性和效力上的局限 BH-30643, a novel macrocyclic non-covalent, mutant-selective EGFR inhibitor, addresses the resistance and potency limitations of contemporary EGFR TKIs Ping Jiang, Wei Deng, Nancy Ling, Danan Li, Zhenping Wang, Yue Hu, Joshua Choi, Eugene Rui, Geoffrey Oxnard, Jean Cui
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5878 · PDF 肿瘤电场治疗对治疗耐药性胶质母细胞瘤仍然有效,其激酶组变化揭示了新的治疗机会 Tumor Treating Fields remain effective in therapy-resistant glioblastoma with kinome shifts revealing novel therapeutic opportunities Taylor Lynn Schanel, Amber Jones, Rhea Pandit, Johsua C. Anderson, Patricia H. Hicks, Corinne Griguer, Braden C. Mcfarland, Christopher D. Willey, Anita B. Hjelmeland
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5879 · PDF 脾酪氨酸激酶作为髓母细胞瘤的新型靶点 Spleen tyrosine kinase as a novel target in medulloblastoma Veena Salvi, Ganesh Naik, Ajay Sharma, Nagendra K. Chaturvedi
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5880 · PDF 在肉瘤中靶向PI3K和Hippo通路的综合策略 A comprehensive approach to targeting PI3K and Hippo pathways in sarcomas Samuel Y. Yu, Keith Garcia, Ali Khan, Souradip Sinha, Colleen Fullenkamp, Munir R. Tanas
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5881 · PDF 通过片段重组设计具有肉瘤选择性细胞毒性的双重VEGFR2/TIE2抑制剂 Fragment-recombination design of a dual VEGFR2/TIE2 inhibitor with sarcoma-selective cytotoxicity Youngkeun Lee, Bo Kyoung Kim, Ji-yoon Choi, Min-jeong Kim, Sung Wook Seo
- 5882 5882 以结构和生物信息学驱动开发一种选择性、口服生物利用度良好的HER2小分子抑制剂(HM100714)用于癌症治疗 Structure- and bioinformatics-driven development of a selective, orally bioavailable HER2 small molecule inhibitor (HM100714) for cancer therapy Ho Yeon Nam, Sun Young Jang, Jiyoung Jeon, HyungSeok Yoo, Jooyun Byun, Soonki Park, Soye Jeon, Haemin Chon, Yu-Yon Kim, Boram Kim, Young Gil Ahn
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5883 · PDF FAK抑制剂APG-2449通过AKT-FOXO1-ACSL4轴触发胃癌中的免疫原性铁死亡 FAK inhibitor APG-2449 triggers immunogenic ferroptosis in gastric cancer via the AKT-FOXO1-ACSL4 axis Lin Zhang, Jing Xiao, Liqun Chen, Siyi Mao, Peiyao Song, Liqiong Yang, Runduan Lin, Miaozhen Qiu, Dajun Yang
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5884 · PDF 靶向多价受体酪氨酸激酶以增强抗PD-1免疫治疗在胃癌中的疗效 Targeting multivalent receptor tyrosine kinases to enhance the efficacy of anti-PD-1 immunotherapy in gastric cancer Melanie Genoula, SHOUMIN ZHU, Mohammed Soutto, Nadeem Sidiq Bhat, Marwah M. Al-Mathkour, Wael El-Rifai
- 5885 5885 通过NXP900抑制SRC家族激酶靶向髓源性抑制细胞(MDSC)以恢复非小细胞肺癌(NSCLC)的抗肿瘤免疫 Targeting myeloid-derived suppressor cells (MDSCs) to restore antitumor immunity in non-small cell lung cancer (NSCLC) via SRC family kinase Inhibition with NXP900 Bobby Kaghazchi, In Hwa Um, Amber Ortiz, Enrique Podarosu, David J. Harrison, Neil Carragher, Asier Unciti-Broceta
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5886 · PDF IDRX-42和NB003针对TKI耐药GIST中继发性和三级(AP/AL)突变的体外性能分析 In vitro profiling of IDRX-42 and NB003 against secondary and tertiary (AP/AL) mutations found in TKI-resistant GIST Michael C. Heinrich, Ajia Town, Marcelina Roberti, Sebastian Bauer
- 5887 5887 可逆性与共价性HER2激酶抑制剂的抗肿瘤活性及更广泛生物学效应分析,以评估其选择性和功能活性 Profiling of reversible and covalent HER2 kinase inhibitors for anti-tumor activity and broader biological effects to evaluate selectivity and functional activity Luciano Galdieri, Steven Garner, Brogan Epkins, Emily Schultz, Daria Clucas, Pony (Yu-Ling) Lee, Chao-Di Chang, Chien-Chang Shen, Alastair J. King
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5888 · PDF 定量磷酸化蛋白质组学揭示CX-4945对神经母细胞瘤翻译调控和分化的影响 Quantitative phospho-proteomics uncovers CX-4945 effects on translational control and differentiation in neuroblastoma Marudhu Pandiyan Shanmugam, Muhammed Danial, Upendarrao Golla, Rifat Tasnim Juthi, Yasin Uzun, Hannah Valensi, Giselle Saulnier Sholler, Chandrika Gowda Behura
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5889 · PDF EO1001在EGFR-ECD突变实体瘤模型中的临床前评估:迈向生物标志物导向的治疗 Preclinical evaluation of EO1001 in EGFR-ECD mutant solid tumor models: Toward biomarker-directed therapy Jeffrey Bacha, Sophia Frentzas, Malaka Ameratunga, Sarath Kanekal, Ian Nisbet, Neil Sankar, Denni M. Brown, Jasmine Borroel, Rowan Prendergast