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. (C) 1999 Elsevier Science Ltd. All rights reserved.
Novel reverse-turn mimics inhibit farnesyl transferase / R. Liu, D. Dong, R. Sherlock, H. Nestler, C.M.A. Gennari, A. Mielgo, C. Scolastico. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - 9:6(1999), pp. 847-852.
Novel reverse-turn mimics inhibit farnesyl transferase
C.M.A. Gennari;C. ScolasticoUltimo
1999
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. (C) 1999 Elsevier Science Ltd. All rights reserved.
File in questo prodotto:
Non ci sono file associati a questo prodotto.
Pubblicazioni consigliate
I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
