Tyrosine Kinase, Phosphatase, and Other Inhibitors

• 5863 · PDF Enhanced antitumor activity of zipalertinib and amivantamab combination in EGFR mutant NSCLC models Kohei Hayashi, Yoshimi Aoyagi, Akihiro Hashimoto, Tomoaki Hitotsumachi, Shuichi Ohkubo
• 5864 · PDF 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
• 5865 · PDF 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
• 5866 · PDF 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
• 5867 · PDF 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 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 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
• 5870 · PDF 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 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
• 5872 · PDF 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
• 5873 · PDF OB-001 boost the brain penetration of multiple TKIs Hitesh Mistry, Jim Millen, Josh Fleet, Mark Brimble
• 5875 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 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 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
• 5878 · PDF 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
• 5879 · PDF Spleen tyrosine kinase as a novel target in medulloblastoma Veena Salvi, Ganesh Naik, Ajay Sharma, Nagendra K. Chaturvedi
• 5880 · PDF 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
• 5881 · PDF 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 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
• 5883 · PDF 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
• 5884 · PDF 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 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
• 5886 · PDF 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 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
• 5888 · PDF 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
• 5889 · PDF 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

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