ras inhibitory peptide

Son of sevenless homolog 1 (Sos1) is a guanine nucleotide exchange factor (GEF) that directs the exchange of Ras-GDP to Ras-GTP by binding to SH3 domains of the growth factor receptor-bound protein 2 (Grb2), leading to the activation of ERK. Ras inhibitory peptide is a synthetic peptide that contains the sequence PVPPR, which corresponds to a region within human Sos1 that interacts with an SH3 domain of Grb2. It specifically blocks the interaction of the GEF with Grb2, preventing an interaction that is essential for Ras activation by receptor tyrosine kinases, including epidermal growth factor receptor.

Ras Inhibitory Peptide acetate 是一种参与 Ras 依赖性信号通路的肽，Ras 在致癌受体引发的人类癌症中起重要作用。

KRPEP-2D acetate 被鉴定为针对 K-Ras 的 G12D 突变体的 K-Ras(G12D) 选择性抑制肽，K-Ras 是 Ras 蛋白家族的关键成员和有吸引力的癌症治疗靶点。

KS-58 是 KRpep-2d 的衍生物，是一种 K-Ras(G12D) 的抑制肽，专门与 K-Ras 选择性结合。该化合物能够进入细胞内，阻断细胞中 Ras 和效应蛋白的相互作用，并抑制肿瘤细胞的增殖，呈现出抗肿瘤活性。