Inhibition of KRAS(G12D) mutant cell lines The promising results for the inhibitory activity and mutant-selectivity from the ITC and KRAS–CRAF interaction assays motivated us to evaluate the potential anti-cancer effects of TH-Z827. The KRAS G12D mutation is the most prevalent mutation form ...
The KRASG12D state was, instead, characterized by several other distinct functional changes as for example those related to chromatin organization and cell-cell adhesion without affecting apoptosis related genes. Conclusion These data predict that the G12D mutation may be more likely selected in a ...
评估GFH375在携带KRAS G12D 突变的晚期实体瘤患者中的安全性/耐受性、PK 和初步有效性,并确定GFH375 的 MTD 和/或 RP2D。 评估GFH375 在携带KRAS G12D 突变的晚期实体瘤患者中的有效性。 开始日期2024-07-02 申办/合作机构 劲方医药科技(上海)股份有限公司 ...
在结直肠癌中超过50%的患者会出现KRAS突变[1,2],其中KRASG12C热点错义突变占全部KRAS突变超60%,包括G12D(40%)、G12V(35%)、G12C(11%)等[3]。而在结直肠癌中KRASG12C突变占比约为4%,与非G12C 突变相比,这类患者预...
下期内容将为您带来“KRAS G12C破译之旅——第2站:突破新生,KRAS G12C突变晚期NSCLC的成药机制与研发现状”,敬请期待! 参考文献: 1. Burns Timothy F, Borghaei Hossein, Ramalingam Suresh S, et al. Targeting KRAS-Mut...
综述:靶向KRASG12C突变:克服耐药性和疗效局限的有效策略开发 《European Journal of Medicinal Chemistry》:Targeting KRASG12C Mutation: Development of Effective Strategies to Overcome Drug Resistance and Limited Efficacy Abstract KRASG12C突变导致KRAS蛋白持续激活状态,驱动细胞恶性增殖。随着共价抑制剂(如AMG510)...
化合物 KRAS G12D MUTATION REGULATOR 4 CAS号: 2621927-57-7 英文名: 2-Naphthalenol, 4-[4-(3,8-diazabicyclo[3.2.1]oct-3-yl)-8-fluoro-2-[(tetrahydro-1H-pyrrolizin-7a(5H)-yl)methoxy]pyrido[4,3-d]pyrimidin-7-yl]-5-ethynyl- 英文别名: KRAS G12D mutation regulator 4;2-...
Wouter W等人分析比较了464例应用不同方案化疗对KRAS突变患者的影响[3],发现紫杉醇联合铂的客观缓解率(ORR)及PFS要优于应用培美曲塞联合铂类的治疗方案,在亚组分析中发现存在G12V突变患者,紫杉醇类药物显著改善了ORR(67%, P <0.01),但未观察到PFS和总生存(OS)的延长;然而存在G12C或G12D突变的患者在所有...
KRAS(G12D)- and BRAF(V600E)-induced transformation of murine pancreatic epithelial cells requires MEK/ERK-stimulated IGF1R signaling. Mol Cancer Res 2012; 10: 1228–1239. Article CAS PubMed PubMed Central Google Scholar Zhang W, Nandakumar N, Shi Y, Manzano M, Smith A, Graham G et ...
Surprisingly, the results showed that there was one patient who was detected with KRAS G12D mutation in the plasma turned out to be negative in the tissue (filled in green, Supplementary Table 3). This might be due to the spatial heterogeneity within a tumour, which is an advantage of ct...