FUSIDIENOL - A NOVEL INHIBITOR OF RAS FARNESYL-PROTEIN TRANSFERASE FROM FUSIDIUM-GRISEUM

Authors
SINGH SB JONES ET GOETZ MA BILLS GF NALLINOMSTEAD M JENKINS RG LINGHAM RB SILVERMAN KC GIBBS JB
Citation
Sb. Singh et al., FUSIDIENOL - A NOVEL INHIBITOR OF RAS FARNESYL-PROTEIN TRANSFERASE FROM FUSIDIUM-GRISEUM, Tetrahedron letters, 35(27), 1994, pp. 4693-4696
Citations number
22
Categorie Soggetti
Chemistry Inorganic & Nuclear
Journal title
Tetrahedron letters → ACNP
ISSN journal
00404039
Volume
35
Issue
27
Year of publication
1994
Pages
4693 - 4696
Database
ISI
SICI code
0040-4039(1994)35:27<4693:F-ANIO>2.0.ZU;2-A
Abstract
Ras (p21) protein is frequently found mutated in human cancers and mus t be farnesylated by farnesyl protein-transferase (FPTase) to achieve cell-transforming activity. Our continued search for inhibitors of FPT ase as potential cancer chemotherapeutics led to the isolation of fusi dienol from extracts of the fungus Fusidium griseum. Fusidienol is a n ovel and potent oxygen-containing [7/6/6] tricyclic heterocycle.