Description: SMART is a highly potent tubulin inhibitor with IC50 in the nanomolar range (20-30 nM) in a number various cancer cell lines including prostate cancer and melanoma cells. It is discovered by Dr. Duane D Miller's group in the University of Tennessee Health Science Center based on the structure of 2-aryl-thiazolidine-4-carboxylic acid amides (ATCAA), a chemical scaffold designed from lysophosphatidic acid (LPA) with a lipid chain in order to inhibit guanine-binding protein-coupled receptor (GPCR) signaling, which was involved in proliferation and survival of prostate cancer. SMART exerts the anticancer activity by binding to the colchicine binding site of tubulin and inhibiting the polymerization of microtubules, thereby resulting in the inhibition of cell division.
References: J Med Chem. 2009 Mar 26;52(6):1701-11; J Med Chem. 2011 Jul 14;54(13):4678-93.