With KRAS-G12C covalent inhibitors entering clinical trials, the myth of this "undruggable" RAS is fading away. In 2021, the Food and Drug Administration (FDA) approved the use of Sotorasib (Lumakras) for the treatment of adult patients with KRAS-G12C mutated locally advanced or metastatic...
Preclinical Characterization, and Early Clinical Activity of JDQ443, a Structurally Novel, Potent, and Selective Covalent Oral Inhibitor of KRASG12C 的文章，该团队开发出一种结构独特的GDP结合KRASG12C共价抑制剂“JDQ443”，有效抑制KRASG12C驱动的细胞信号传导，并在KRASG12C突变...
近日，来自加州大学旧金山分校的研究人员开发出一种药物，该药物可以有效拆穿肿瘤细胞的一些“鬼把戏”——将隐匿的癌症细胞打上标签，以便让免疫系统更快地识别、摧毁癌细胞。9月12日，加州大学旧金山分校研究人员在著名期刊《癌细胞》（Cancer Cell）发表题为“A covalent inhibitor of K-Ras(G12C) induces MHC ...
4. Canon J. et al. The clinical KRAS (G12C) inhibitor AMG 510 drives anti-tumour immunity. Nature. 2019; 575: 217-223. 5. Fell J. et al. Identification of the clinical development candidate MRTX849, a covalen...
新方法让KRAS癌症基因向免疫系统说“吃我” 9月12日,加州大学旧金山分校研究人员在著名期刊《癌细胞》(Cancer Cell)发表题为“A covalent inhibitor of K-Ras(G12C) induces MHC class I presentation of haptenated peptide neoepitopes targetable by immunotherapy” 的研究论文。该研究描述了一种新的治疗方法——...
Glecirasib, a highly selective, covalent oral KRAS G12C inhibitor, has demonstrated promising clinical activity in NSCLC and CRC; however, the efficacy and safety of glecirasib are unknown in PDAC and other solid tum...
[2] Pylayeva-Gupta Y, et al., Rasoncogenes: weaving a tumo rigenic web. Nat Rev Cancer, 2011, 11(11): 761-774.[3] Jay B. Fell, et al., Identificationof the Clinical Development Candidate MRTX849, aCovalentKRASG12C Inhibitor for the Treatment of Cancer. J. Med. Chem, 2020.
期待在未来,随着更多高质量研究数据的披露,氟泽雷塞能够在KRAS G12C突变肿瘤患者治疗方案的联合应用及前线治疗方面有进一步的亮眼表现,为患者带来更多获益! 参考文献:(向上滑动阅览) 1. Zhou Qing, Yang Nong, Zhao Mingfang, et al. Potent covalent irreversible inhibitor of KRAS G12C IBI351 in patients ...
关于最初idea的来源,以及与其它部分KRAS-G12C分子的比较,感兴趣可以见往期 诺华KRAS分子JDQ443的发现 诺华KRAS分子JDQ443 JDQ443, a Structurally Novel, Pyrazole-Based, Covalent Inhibitor of KRAS-G12C for the Treatment of Solid Tumors, J Med Chem, Nov 18, 2022 ...
KRAS G12C共价抑制剂,AMG-510 is a potent KRAS G12C covalent inhibitor with potential antineoplastic activity.体外活性:AMG 510 inhibits SOS1-catalyzed nucleotide exchange of recombinant mutant KRAS (G12C/C118A) but had min