Салирасиб

Описание

Association of Ras protein with the inner surface of the plasma membrane is required for Ras signaling activity. Farnesyl thiosalicylic acid (FTS) is an inhibitor of Ras-mediated signaling that functions by dislodging Ras from the cell membrane thereby rendering it susceptible to proteolytic degradation. FTS inhibits the growth of human Ha-ras-transformed Rat1 fibroblasts with an IC₅₀ value of 7.5 μM. It does not inhibit Ras farnesylation in vitro and although FTS does inhibit prenylated protein methyltransferase (PPMTase) in cell-free systems with a K_i value of 2.6 μM, it is relatively ineffective at inhibiting methylation in whole cells. Treatment of chow-fed ApoE-deficient mice with 5 mg/kg FTS three times per week for six weeks reduces early atherosclerotic lesion development by 52% compared to controls.

Химические свойства

Pale Yellow Solid

Использование

Salirasib is a new specific nontoxic drug with a mild hydrophobic nature, which acts as a Ras antagonist and can therefore be used for stent applications as well as for local cancer treatment.