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Synthesis and biological activity of semipeptoid farnesyltransferase inhibitors.

Abstract：

:Semipeptoids derived from the Ras farnesyl transferase inhibitor, CVFM, were synthesized by the Simultaneous Multiple Analogue Peptide Synthesis methodology. The semipeptoids were screened for their in vitro inhibition potency towards farnesyl transferase and geranylgeranyl transferase. Structure-activity relationship studies led to a potent and selective inhibitor, HR-11, which blocks Ras farnesylation in vitro with an IC50 of 1.2 nM. The cell permeable methyl ester derivative of HR-11, HR-12, inhibits Ras farnesylation in intact cells with an IC50 of 10 microM and with no detectable inhibition of Rap1A/K-rev geranyl-geranylation.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Reuveni H,Gitler A,Poradosu E,Gilon C,Levitzki A

doi

10.1016/s0968-0896(96)00197-6

subject

Has Abstract

pub_date

1997-01-01 00:00:00

pages

85-92

issue

1

eissn

0968-0896

issn

1464-3391

pii

S0968089696001976

journal_volume

5

pub_type

杂志文章

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