ISOLATION AND STRUCTURE OF CHAETOMELLIC ACIDS A AND B FROM CHAETOMELLA-ACUTISETA - FARNESYL PYROPHOSPHATE MIMIC INHIBITORS OF RAS FARNESYL-PROTEIN TRANSFERASE
Sb. Singh et al., ISOLATION AND STRUCTURE OF CHAETOMELLIC ACIDS A AND B FROM CHAETOMELLA-ACUTISETA - FARNESYL PYROPHOSPHATE MIMIC INHIBITORS OF RAS FARNESYL-PROTEIN TRANSFERASE, Tetrahedron, 49(27), 1993, pp. 5917-5926
Farnesyl-Protein transferase catalyses a post-translational modificati
on of Ras that is obligatory for the cell transforming activity of thi
s oncogene protein. The screening of natural products to identify inhi
bitors of this enzyme as a potential anticancer agents, has led to the
isolation of two novel dicarboxylic acids, named chaetomellic acids f
rom Chaetomella acutiseta , as potent and selective inhibitors which a
ppear to be the first examples of non-phosphorous containing FPP mimic
s.