(-)-FR182877 is a potent and selective inhibitor of carboxylesterase-1

被引:49
作者
Adam, GC
Vanderwal, CD
Sorensen, EJ
Cravatt, BF
机构
[1] Skaggs Inst Chem Biol, La Jolla, CA 92037 USA
[2] Scripps Res Inst, Dept Chem, La Jolla, CA 92037 USA
[3] Scripps Res Inst, Dept Cell Biol, La Jolla, CA 92037 USA
关键词
activity-based profiling; hydrolases; inhibitors; natural products; proteomics;
D O I
10.1002/anie.200352576
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Activity-based profiling and reporter-group-tagged compounds were used to identify carboxylesterase-1 (CE-1) as a specific target of the natural product (-)-FR182877 (see scheme). Now that a target is known, specific modification of the lactone natural product may lead to even more effective inhibitors of CE-1.
引用
收藏
页码:5480 / 5484
页数:5
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共 42 条
  • [11] HADVARY P, 1991, J BIOL CHEM, V266, P2021
  • [12] AN EXTREMELY SIMPLE, CONVENIENT, AND SELECTIVE METHOD FOR ACETYLATING PRIMARY ALCOHOLS IN THE PRESENCE OF SECONDARY ALCOHOLS
    ISHIHARA, K
    KURIHARA, H
    YAMAMOTO, H
    [J]. JOURNAL OF ORGANIC CHEMISTRY, 1993, 58 (15) : 3791 - 3793
  • [13] Enzyme activity profiles of the secreted and membrane proteome that depict cancer cell invasiveness
    Jessani, N
    Liu, YS
    Humphrey, M
    Cravatt, BF
    [J]. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 2002, 99 (16) : 10335 - 10340
  • [14] Profiling serine hydrolase activities in complex proteomes
    Kidd, D
    Liu, YS
    Cravatt, BF
    [J]. BIOCHEMISTRY, 2001, 40 (13) : 4005 - 4015
  • [15] Molecular cloning, characterization, and differential expression pattern of mouse lung surfactant convertase
    Krishnasamy, S
    Teng, AL
    Dhand, R
    Schultz, RM
    Gross, NJ
    [J]. AMERICAN JOURNAL OF PHYSIOLOGY-LUNG CELLULAR AND MOLECULAR PHYSIOLOGY, 1998, 275 (05) : L969 - L975
  • [16] Protease inhibitors: Current status and future prospects
    Leung, D
    Abbenante, G
    Fairlie, DP
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 2000, 43 (03) : 305 - 341
  • [17] Discovering potent and selective reversible inhibitors of enzymes in complex proteomes
    Leung, D
    Hardouin, C
    Boger, DL
    Cravatt, BF
    [J]. NATURE BIOTECHNOLOGY, 2003, 21 (06) : 687 - 691
  • [18] Proteome analysis of hepatocellular carcinoma
    Lim, SO
    Park, SJ
    Kim, W
    Park, SG
    Kim, HJ
    Kim, YI
    Sohn, TS
    Noh, JH
    Jung, G
    [J]. BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 2002, 291 (04) : 1031 - 1037
  • [19] Structure of human methionine aminopeptidase-2 complexed with fumagillin
    Liu, SP
    Widom, J
    Kemp, CW
    Crews, CM
    Clardy, J
    [J]. SCIENCE, 1998, 282 (5392) : 1324 - 1327
  • [20] REGULATION OF 2 RAT-LIVER MICROSOMAL CARBOXYLESTERASE ISOZYMES - SPECIES-DIFFERENCES, TISSUE DISTRIBUTION, AND THE EFFECTS OF AGE, SEX, AND XENOBIOTIC TREATMENT OF RATS
    MORGAN, EW
    YAN, BF
    GREENWAY, D
    PARKINSON, A
    [J]. ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS, 1994, 315 (02) : 513 - 526