Germline RET V804M mutation associated with multiple endocrine neoplasia type 2A. Br J Surg 2004: 91 (11): 1458-1459.Gibelin H, Bezieau S, Misso C, Bouin-Pineau M-H, Mare´chaud R, Kraimps J-L 2004 Germline RET V804M mu- tation associated with multiple endocrine neoplasia type 2A....
Coexisting RET alteration has been observed as one of mechanisms of primary resistance to MKIs. The RET M918T mutation, which affects the C-lobe of the kinase, is the most frequent mutation in MTC. It has been observed that the half maximal inhibitory concentrations (IC50s) of Vandetanib, C...
图1.RET信号异常可导致肿瘤发生 RET的靶向突变(例如RET M918T,V804M/L)通过三种广泛的机制导致异常激活-通过形成分子间半胱氨酸二硫键形成二聚作用,影响ATP结合结构域并最终增强激酶结构域活性。染色体重排(例如KIF5B-RET,CCDC6-RET)产生杂交蛋白,该杂交蛋白的融合伴侣通常包含一个RET激酶结构域的二聚体结构域。 ...
Coexisting RET alteration has been observed as one of mechanisms of primary resistance to MKIs. The RET M918T mutation, which affects the C-lobe of the kinase, is the most frequent mutation in MTC. It has been observed that the half maximal inhibitory concentrations (IC50s) of Vandetanib, C...
突变与药物 M918T FUSION KIF5B-RET C634W C609Y EXPRESSION OVEREXPRESSION KIF5B-RET G810A MUTATION V804M CCDC6-RET KIF5B-RET V804L C634R 更多>> 相关基因检测 genes 癌基因 靶向药 医生 医院癌症分类 肺癌 乳腺癌 胃癌 肝癌 结直肠癌 食管癌 子宫癌 卵巢癌 宫颈癌 前列腺癌 脑瘤 胰腺癌 膀胱癌 ...
体外研究显示,Pralsetinib能够抑制RET V804L、RET V804M和RET V804E等其它MKI耐药位点。同时,Pralsetinib对RET的选择性比将近96%的被检MKI高100倍,并且在KIF5B-RET融合的Ba/F3细胞中抑制RET自身磷酸化能力比凡德他尼、卡博替尼及临床试验药RXDX-105高10倍[2]。
BLU-667还具有抗RET V804L、RET V804M和RET V804E的效力,这三种突变可产生MKI抗性,从而抑制体外增殖。BLU-667对RET的选择性超过96%,在抑制KIF5B-RET融合的Ba/F3细胞RET自磷酸化方面,BLU-667的抑制效力至少是Vandetanib、Cabozantinib和RXDX-105的10倍。BLU-667在体内保持了这种抗肿瘤活性和RET选择性[9]。I/II...
The highly-selective RET inhibitor LOXO-292 demonstrated robust clinical activity across RET-altered solid tumors, including in patients with brain metastases and the RET V804M gatekeeper mutation, which usually confers resistance to multikinase inhibitors, according to findings from the phase I LIBRETTO...
2000. Variable expressivity of familial medullary thyroid carcinoma (FMTC) due to a RET V804M (GTG ! ATG) mutation. Surgery 128:93-98.Feldman GL, Edmonds MW, Ainsworth PJ, et al. 2000 Variable expressivity of familial medullary thyroid carcinoma (FMTC) due to a RET V804M (GTG3 ATG) ...
22. The method of any one of embodiments 1-3 and 12-19, wherein the cancer is MTC having a C634R mutation. 23. The method of any one of embodiments 1-3 and 12-19, wherein the cancer is MTC having a V804M mutation. 24. The method of any one of embodiments 1-3, 6, and...