Author/Authors :
Ruiping Liu، نويسنده , , Dennis L. -Y. Dong، نويسنده , , Rosemarie Sherlock، نويسنده , , H. Peter Nestler، نويسنده , , Cesare Gennari، نويسنده , , Antonia Mielgo and، نويسنده , , Carlo Scolastici، نويسنده ,
Abstract :
Reverse-turn inducing bicyclic lactams were incorporated into the substrate sequence recognized by farnesyl transferase to create inhibitors of RAS farnesylation. While the free peptides did not show any effect on the farnesylation, their Fmoc-protected counterparts impede the transformation of RAS with IC50ʹs in the low micromolar range.
