KRAS基因编码的蛋白是一种小GTP酶（small GTPase），它属于RAS超蛋白家族，并参与细胞内的信号转导。目前已知的三种最致命癌症（肺癌、结直肠癌和胰腺癌）很大比例上是由KRAS突变驱动的。在这些肿瘤类型中，KRAS突变主要发生在第12、13、61密码子上（致癌热点残基为G12、G13和Q61）。突变发生后会影响GTP的水解，使突变体保持KRAS-GTP结合激活状态，持续激活下游信号通路，促使肿瘤形成。三十多年来，RAS一直被认为是“不可成药靶点”。然而，AMG 510的问世为一系列突变的RAS等位基因特异性靶向治疗带来了希望。

现优爱推出KRAS野生型及多种突变蛋白蛋白，并通过SDS-PAGE、SPR/HTRF等平台验证了蛋白纯度及活性（可提供与GTP/GDP结合的KRAS蛋白）。

KRAS G12C是在第12个密码子处发生突变，从甘氨酸突变为半胱氨酸。目前相关药物有：ARS-1620，ARS-853，Sotorasib ，JDQ443 ，JAB-21822等；相关疾病涉及：结肠癌，结直肠癌，肺癌，非小细胞肺癌，多发性骨髓瘤，皮肤鳞状细胞癌等。

KRAS-G12C activity test using HTRF method

The KRAS-G12C activity was assayed with HTRF technology. The reaction was performed by incubating the KRAS-G12C protein, GTP, cRAF and beads at 25℃ for 60 min, then reading Ratio 665/620nm signal.

KRAS-G12D是在第12号密码子出发生突变引入天冬氨酸。目前相关药物有：MRTX1133，JAB-22000，RMC-9805 (RM-036)等。相关疾病涉及：结肠癌，结直肠癌，毛细胞白血病，肺癌，非小细胞肺癌，黑色素瘤多发性骨髓瘤，卵巢癌，胰腺癌，胰腺导管癌，皮肤鳞状细胞癌，甲状腺癌，外分泌胰腺肿瘤等。

KRAS-G12D activity test using HTRF method

The KRAS-G12D activity was assayed with HTRF technology. The reaction was performed by incubating the KRAS-G12D protein, GTP, cRAF and beads at 25℃ for 60 min, then reading Ratio 665/620nm signal

目前相关药物有：ELI-002 2P，mDC3/8-KRAS vaccine等。相关疾病涉及：结肠癌，结直肠癌，非小细胞肺癌，胰腺癌，罗莎多夫曼病，甲状腺癌等。

KRAS-G12R activity test using HTRF method

The KRAS-G12R activity was assayed with HTRF technology. The reaction was performed by incubating the KRAS-G12R protein, GTP, cRAF and beads at 25℃ for 60 min, then reading Ratio 665/620nm signal.

目前相关药物有：JAB-23000，K27-SPOP等。相关疾病涉及：癌症，结肠癌，结直肠癌，肺癌，非小细胞肺癌等。

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KRAS-G12V activity test using HTRF method

The KRAS- G12V activity was assayed with HTRF technology. The reaction was performed by incubating the KRAS- G12V protein, GTP, cRAF and beads at 25℃ for 60 min, then reading Ratio 665/620nm signal.

目前相关药物有：RMC-8839等。相关疾病涉及：结直肠癌，非小细胞肺癌等。

KRAS-G13C activity test using HTRF method

The KRAS-G13C activity was assayed with HTRF technology. The reaction was performed by incubating the KRAS-G13C protein, GTP, cRAF and beads at 25℃ for 60 min, then reading Ratio 665/620nm signal.

KRAS基因第61位编码子的谷氨酰胺突变为组氨酸。目前相关药物有：K27-SPOP等。相关疾病涉及：结直肠癌，肺癌，非小细胞肺癌等。

KRAS-Q61H activity test using HTRF method

The KRAS-Q61H activity was assayed with HTRF technology. The reaction was performed by incubating the KRAS-Q61H protein, GTP, cRAF and beads at 25℃ for 60 min, then reading Ratio 665/620nm signal.

目前相关药物有：帕尼单抗等。相关疾病涉及：结直肠癌等。

KRAS-WT activity test using HTRF method

The KRAS-WT activity was assayed with HTRF technology. The reaction was performed by incubating the KRAS- WT protein, GTP, cRAF and beads at 25℃ for 60 min, then reading Ratio 665/620nm signal.

Punekar SR, Velcheti V, Neel BG, Wong KK. The current state of the art and future trends in RAS-targeted cancer therapies. Nat Rev Clin Oncol. 2022 Oct;19(10):637-655.

来源于优宁维药物研发官网