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. Scolastico
Ultimo
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.
Settore CHIM/06 - Chimica Organica
1999
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2434/175912
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