A cembranolide diterpene farnesyl protein transferase inhibitor from the marine soft coral Lobophytum cristagalli

被引：42

作者：

Coval, SJ

Patton, RW

Petrin, JM

James, L

Rothofsky, ML

Lin, SL

Patel, M

Reed, JK

McPhail, AT

Bishop, WR

机构：

[1] HARBOR BRANCH OCEANOG INST INC,FT PIERCE,FL 34946

[2] DUKE UNIV,PAUL M GROSS CHEM LAB,DEPT CHEM,DURHAM,NC 27708

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1996年 / 6卷 / 07期

关键词：

D O I：

10.1016/0960-894X(96)00142-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A previously described cembranolide diterpene from Lobophytum cristagalli was identified as a potent (IC50 0.15 mu M) inhibitor of famesyl protein transferase (FPT). The compound showed selectivity for FPT as compared to the closely related enzyme geranylgeranyl protein transferase-1 (IC50 5.3 mu M). Kinetic evaluation suggests that this compound competes with the protein/peptide farnesyl acceptor substrate, and not with farnesyl pyrophosphate for inhibition of FPT. Copyright (C) 1996 Elsevier Science Ltd

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页码：909 / 912

页数：4

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