Salirasib
Ras inhibitor / Salirasib is a synthetic farnesylcysteine mimetic that inhibits ras proteins1,2 via disruption of interactions between the S-Prenyl moiety of Ras and the membrane anchorage domains3. It has been investigated in the treatment of various cancers.4,5 HCC cells pretreated with salirasib were sensitized to TRAIL-induced apoptosis.6 Salirasib has also been shown to inhibit TRPA1 (EC50 = 1.3 µM).7
Biochemicals & reagents
162520-00-5
1) Marciano et al. (1995), Farnesyl Derivatives of Rigid Carboxylic Acids – Inhibitors of ras-Dependent Cell Growth; J.Med.Chem. 38 1267 2) Marom et al. (1995), Selective inhibition of Ras-dependent cell growth by farnesylthiosalicylic acid (salirasib) in patients with solid tumors; J.Biol.Chem. 270 22263 3) Haklai et al. (1998), Dislodgement and Accelerated Degradation of Ras; Biochemistry 37 1306 4) Laheru et al. (2012), Integrated preclinical and clinical development of S-trans,trans-Farnesylthiosalicylic acid (FTS, Salirasib) in pancreatic cancer; Invest.New Drugs 30 2391 5) Tsimberidou et al. (2010), Phase 1 first-in-human clinical study of S-trans,trans-farnesylthiosalicylic acid (salirasib) in patients with solid tumors; Cancer Chemother.Pharmacol. 65 235 6) Charette et al. (2013), Salirasib sensitizes hepatocarcinoma cells to TRAIL-induced apoptosis through DR5 and survivin-dependent mechanisms; Cell Death and Disease. 4 e471 7) Maher et al. (2008), Activation of TRPA1 by farnesyl thiosalicylic acid; Mol.Pharmacol. 73 1225
RT
TARGET: GTPase -- PATHWAY: Apoptosis inducer; Posttranslational modification -- RESEARCH AREA: Cell death -- DISEASE AREA: Cancer