title: Novel reverse-turn mimics inhibit farnesyl transferase.
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 IC50's in the low micromolar range.
authors: Cold Spring Harbor Laboratory, NY 11724, USA.
authors: R
authors: R
authors: Liu
authors: D L
authors: DL
authors: Dong
authors: R
authors: R
authors: Sherlock
authors: H P
authors: HP
authors: Nestler
authors: C
authors: C
authors: Gennari
authors: A
authors: A
authors: Mielgo
authors: C
authors: C
authors: Scolastico
mesh_terms: D019883:Alkyl and Aryl Transferases / Q000037:antagonists & inhibitors*; D004305:Dose-Response Relationship, Drug; D020128:Inhibitory Concentration 50; D007700:Kinetics; D007769:Lactams / Q000138:chemical synthesis* / Q000378:metabolism*; D008956:Models, Chemical; D017433:Protein Structure, Secondary
chemical_list: D007769:Lactams; D019883:Alkyl and Aryl Transferases; C064911:p21(ras) farnesyl-protein transferase