PEPTIDE-BASED P21(RAS) FARNESYL TRANSFERASE INHIBITORS - SYSTEMATIC MODIFICATION OF THE TETRAPEPTIDE CA(1)A(2)X MOTIF

被引:38
作者
LEFTHERIS, K
KLINE, T
NATARAJAN, S
DEVIRGILIO, MK
CHO, YH
PLUSCEC, J
RICCA, C
ROBINSON, S
SEIZINGER, BR
MANNE, V
MEYERS, CA
机构
[1] The Bristol-Meyers Squibb Pharmaceutical Research Institute, Princeton, NJ 08540
关键词
D O I
10.1016/S0960-894X(01)80257-2
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A systematic study of CVFM, a CAAX-derived farnesyl transferase inhibitor, was undertaken to determine the structural elements important for intrinsic activity as well as substrate character. Results indicate a narrowly defined profile for nonsubstrate FT inhibition.
引用
收藏
页码:887 / 892
页数:6
相关论文
共 25 条
  • [1] Bodanszky M., 1984, PRINCIPLES PEPTIDE S, DOI [10.1007/978-3-642-96835-8, DOI 10.1007/978-3-642-96835-8]
  • [2] CYANOHYDRIDOBORATE ANION AS A SELECTIVE REDUCING AGENT
    BORCH, RF
    BERNSTEIN, MD
    DURST, HD
    [J]. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1971, 93 (12) : 2897 - +
  • [3] TETRAPEPTIDE INHIBITORS OF PROTEIN FARNESYLTRANSFERASE - AMINO-TERMINAL SUBSTITUTION IN PHENYLALANINE-CONTAINING TETRAPEPTIDES RESTORES FARNESYLATION
    BROWN, MS
    GOLDSTEIN, JL
    PARIS, KJ
    BURNIER, JP
    MARSTERS, JC
    [J]. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1992, 89 (17) : 8313 - 8316
  • [4] P21RAS IS MODIFIED BY A FARNESYL ISOPRENOID
    CASEY, PJ
    SOLSKI, PA
    DER, CJ
    BUSS, JE
    [J]. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1989, 86 (21) : 8323 - 8327
  • [5] N-METHYLAMINO ACIDS IN PEPTIDE-SYNTHESIS .5. SYNTHESIS OF N-TERT-BUTYLOXYCARBONYL, N-METHYLAMINO ACIDS BY N-METHYLATION
    CHEUNG, ST
    BENOITON, NL
    [J]. CANADIAN JOURNAL OF CHEMISTRY-REVUE CANADIENNE DE CHIMIE, 1977, 55 (05): : 906 - 910
  • [6] STUDIES ON AMINO-ACIDS AND PEPTIDES .6. METHODS FOR INTRODUCING THIOAMIDE BONDS INTO THE PEPTIDE BACKBONE - SYNTHESIS OF THE 4 MONOTHIO ANALOGS OF LEUCINE ENKEPHALIN
    CLAUSEN, K
    THORSEN, M
    LAWESSON, SO
    SPATOLA, AF
    [J]. JOURNAL OF THE CHEMICAL SOCIETY-PERKIN TRANSACTIONS 1, 1984, (04): : 785 - 798
  • [7] DIAGOMESEGUER J, 1980, SYNTHESIS-STUTTGART, P547
  • [8] FEHRENTZ JA, 1985, INT J PEPT PROT RES, V26, P236
  • [9] SOLID-PHASE PEPTIDE-SYNTHESIS UTILIZING 9-FLUORENYLMETHOXYCARBONYL AMINO-ACIDS
    FIELDS, GB
    NOBLE, RL
    [J]. INTERNATIONAL JOURNAL OF PEPTIDE AND PROTEIN RESEARCH, 1990, 35 (03): : 161 - 214
  • [10] FRIEDINGER RM, 1983, J ORG CHEM, V48, P77