Enzyme microarrays: On-chip determination of inhibition constants based on affinity-label defection of enzymatic activity

被引:30
作者
Eppinger, J
Funeriu, DP
Miyake, M
Denizot, L
Miyake, J
机构
[1] Tech Univ Munich, ForschungsDozentur Mol Katalyse Lehrstuhl Anorgan, D-85748 Garching, Germany
[2] Natl Inst Adv Ind Sci & Technol, Tissue Engn Res Ctr, Amagasaki, Hyogo 6610974, Japan
关键词
enzymes; fluorescent probes; high-throughput screening; inhibitors; microarrays; on-chip kinetics;
D O I
10.1002/anie.200353623
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
High-throughput screening of libraries of potential inhibitors is possible by using an enzyme microarray method that combines low sample consumption with accuracy and speed. Information about enzyme inhibition can be obtained on-chip" by the addition of a fluorescently tagged affinity label to a microarray of functional enzymes (see picture)."
引用
收藏
页码:3806 / 3810
页数:5
相关论文
共 18 条
[1]   Proteomic profiling of mechanistically distinct enzyme classes using a common chemotype [J].
Adam, GC ;
Sorensen, EJ ;
Cravatt, BF .
NATURE BIOTECHNOLOGY, 2002, 20 (08) :805-809
[2]   L-TRANS-EPOXYSUCCINYL-LEUCYLAMIDO(4-GUANIDINO)BUTANE (E-64) AND ITS ANALOGS AS INHIBITORS OF CYSTEINE PROTEINASES INCLUDING CATHEPSINS B, H AND L [J].
BARRETT, AJ ;
KEMBHAVI, AA ;
BROWN, MA ;
KIRSCHKE, H ;
KNIGHT, CG ;
TAMAI, M ;
HANADA, K .
BIOCHEMICAL JOURNAL, 1982, 201 (01) :189-198
[3]  
Burke M. D., 2004, ANGEW CHEM, V116, P48
[4]   A planning strategy for diversity-oriented synthesis [J].
Burke, MD ;
Schreiber, SL .
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION, 2004, 43 (01) :46-58
[5]   Developing a strategy for activity-based detection of enzymes in a protein microarray [J].
Chen, GYJ ;
Uttamchandani, M ;
Zhu, Q ;
Wang, G ;
Yao, SQ .
CHEMBIOCHEM, 2003, 4 (04) :336-339
[6]   Printing chemical libraries on microarrays for fluid phase nanoliter reactions [J].
Gosalia, DN ;
Diamond, SL .
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 2003, 100 (15) :8721-8726
[7]   Epoxide electrophiles as activity-dependent cysteine protease profiling and discovery tools [J].
Greenbaum, D ;
Medzihradszky, KF ;
Burlingame, A ;
Bogyo, M .
CHEMISTRY & BIOLOGY, 2000, 7 (08) :569-581
[8]   Small molecule affinity fingerprinting:: a tool for enzyme family subclassification, target identification, and inhibitor design [J].
Greenbaum, DC ;
Arnold, WD ;
Lu, F ;
Hayrapetian, L ;
Baruch, A ;
Krumrine, J ;
Toba, S ;
Chehade, K ;
Brömme, D ;
Kuntz, ID ;
Bogyo, M .
CHEMISTRY & BIOLOGY, 2002, 9 (10) :1085-1094
[9]   Chemical proteomics and its application to drug discovery [J].
Jeffery, DA ;
Bogyo, M .
CURRENT OPINION IN BIOTECHNOLOGY, 2003, 14 (01) :87-95
[10]   High-throughput screening of enzyme inhibitors: Automatic determination of light-binding inhibition constants [J].
Kuzmic, P ;
Sideris, S ;
Cregar, LM ;
Elrod, KC ;
Rice, KD ;
Janc, JW .
ANALYTICAL BIOCHEMISTRY, 2000, 281 (01) :62-67