(-)-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

来源：

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION | 2003年 / 42卷 / 44期

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

页码：5480 / 5484

页数：5

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

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