LONAFARNIB (C005B-312081)

General description

Lonafarnib (SCH66336) is a farnesyl transferase inhibitor (FTI). K- and N-Ras are substrates of farnesyl transferase.

Biochem/physiol Actions

Lonafarnib is a potent inhibitor of farnesyltransferase, an enzyme responsible for a post-translational modification of proteins (including Ras) that gives a protein sufficient hydrophobicity to translocate to the plasma membrane. Farnesylation regulates signaling cascades controlling cell survival, proliferation and differentiation, so variety of possible uses is not surprising a post-translational modification of proteins (including Ras) that gives a protein sufficient hydrophobicity to translocate to the plasma membrane. Lonafarnib has been studies for possible treatment of progeria, various cancers, and hepatitis D.

Lonafarnib prevents the post-translational lipid modification of H-Ras and other farnesylated proteins. Lonafarnib treatment results in microtubule bundling, increased microtubule acetylation and stabilization and suppression of microtubule dynamics.