日期:
2020 年 — 2026 年
2020
2021
2022
2023
2024
2025
2026
影响因子:

STX-721, a Covalent EGFR/HER2 Exon 20 Inhibitor, Utilizes Exon 20-Mutant Dynamic Protein States and Achieves Unique Mutant Selectivity Across Human Cancer Models

STX-721 是一种共价 EGFR/HER2 外显子 20 抑制剂,它利用外显子 20 突变体的动态蛋白状态,并在人类癌症模型中实现了独特的突变选择性。

Raymond A Pagliarini,Jack A Henderson,Benjamin C Milgram,Deanna R Borrelli,Natasja Brooijmans,Brendan J Hilbert,Michael R Huff,Takahiro Ito,Gregory V Kryukov,Brendon Ladd,Brent R Martin,Hashim Motiwala,Erin O'Hearn,Chia-Feng Tsai,Weixue Wang,Justine Bellier,Luke Boland,Sarah Clark,Emily Hensley,Aaron N Hata,Petr Kuzmic,Angel Guzman-Perez,Erica L Jackson,Darrin D Stuart

STX-478, a Mutant-Selective, Allosteric PI3Kα Inhibitor Spares Metabolic Dysfunction and Improves Therapeutic Response in PI3Kα-Mutant Xenografts

STX-478 是一种突变选择性变构 PI3Kα 抑制剂,可避免代谢功能障碍并改善 PI3Kα 突变异种移植的治疗反应

Leonard Buckbinder, David J St Jean Jr, Trang Tieu, Brendon Ladd, Brendan Hilbert, Weixue Wang, Jacob T Alltucker #, Samantha Manimala, Gregory V Kryukov, Natasja Brooijmans, Gregory Dowdell, Philip Jonsson #, Michael Huff, Angel Guzman-Perez, Erica L Jackson, Marcus D Goncalves, Darrin D Stuart

RAF-Mutant Melanomas Differentially Depend on ERK2 Over ERK1 to Support Aberrant MAPK Pathway Activation and Cell Proliferation

RAF 突变型黑色素瘤对 ERK2 而非 ERK1 的依赖性不同,从而支持异常 MAPK 通路激活和细胞增殖

Matthew S Crowe, Tatiana Zavorotinskaya, Charles F Voliva, Matthew D Shirley, Yanqun Wang, David A Ruddy, Daniel P Rakiec, Jeffery A Engelman, Darrin D Stuart, Alyson K Freeman

Tumor Intrinsic Efficacy by SHP2 and RTK Inhibitors in KRAS-Mutant Cancers

SHP2 和 RTK 抑制剂对 KRAS 突变癌症的肿瘤内在疗效

Huai-Xiang Hao #, Hongyun Wang #, Chen Liu, Steven Kovats, Roberto Velazquez, Hengyu Lu, Bhavesh Pant, Matthew Shirley, Matthew J Meyer, Minying Pu, Joanne Lim, Michael Fleming, LeighAnn Alexander, Ali Farsidjani, Matthew J LaMarche, Susan Moody, Serena J Silver, Giordano Caponigro, Darrin D Stuart,

Modelling vemurafenib resistance in melanoma reveals a strategy to forestall drug resistance

对黑色素瘤中维莫非尼耐药性的建模揭示了一种预防耐药性的策略

Meghna Das Thakur, Fernando Salangsang, Allison S Landman, William R Sellers, Nancy K Pryer, Mitchell P Levesque, Reinhard Dummer, Martin McMahon, Darrin D Stuart

RAF inhibitors activate the MAPK pathway by relieving inhibitory autophosphorylation

RAF 抑制剂通过缓解抑制性自身磷酸化来激活 MAPK 通路

Matthew Holderfield, Hanne Merritt, John Chan, Marco Wallroth, Laura Tandeske, Huili Zhai, John Tellew, Stephen Hardy, Mohammad Hekmat-Nejad, Darrin D Stuart, Frank McCormick, Tobi E Nagel