G-protein-coupled receptor Microarrays for multiplexed compound screening

被引:14
作者
Hong, Yulong
Webb, Brian L.
Pai, Sadashiva
Ferrie, Ann
Peng, Jinlin
Lai, Fang
Lahiri, Joydeep
Biddlecome, Gloria
Rasnow, Brian
Johnson, Michael
Min, Hosung
Fang, Ye
Salon, John
机构
[1] Amgen Inc, Thousand Oaks, CA 91320 USA
[2] Corning Inc, Corning, NY 14831 USA
关键词
GPCR; array; binding assay; fluorescent; HTS;
D O I
10.1177/1087057106287139
中图分类号
Q5 [生物化学];
学科分类号
071010 ; 081704 ;
摘要
Conventional assay methods for discovering and profiling drug-target interactions are typically developed on a target-by-target basis and hence can be cumbersome to enable and orchestrate. Herein the authors report a solid-state ligand-binding assay that operates in a multiplexed mode to report compound activity against a micorarray-configured panel of G-protein-coupled receptor (GPCR) targets. The pharmacological fidelity of the system is high, and its miniaturized "plug-and-play" format provides improved efficiency both in terms of execution time and reagent consumption. Taken together, these features make the system ideally suited to explore the structure-activity relationship of compounds across a broad region of target class space.
引用
收藏
页码:435 / 438
页数:4
相关论文
共 14 条
[1]   SEQUENCE OF THE GENE ENCODING THE HUMAN M1 MUSCARINIC ACETYLCHOLINE-RECEPTOR [J].
ALLARD, WJ ;
SIGAL, IS ;
DIXON, RAF .
NUCLEIC ACIDS RESEARCH, 1987, 15 (24) :10604-10604
[2]   Human urotensin-II is a potent vasoconstrictor and agonist for the orphan receptor GPR14 [J].
Ames, RS ;
Sarau, HM ;
Chambers, JK ;
Willette, RN ;
Alyar, NV ;
Romanic, AM ;
Louden, CS ;
Foley, JJ ;
Sauermelch, CF ;
Coatney, RW ;
Ao, ZH ;
Disa, J ;
Holmes, SD ;
Stadel, JM ;
Martin, JD ;
Liu, WS ;
Glover, GI ;
Wilson, S ;
McNulty, DE ;
Ellis, CE ;
Elshourbagy, NA ;
Shabon, U ;
Trill, JJ ;
Hay, DWP ;
Ohlstein, EH ;
Bergsma, DJ ;
Douglas, SA .
NATURE, 1999, 401 (6750) :282-286
[3]   Cloning and characterization of the human galanin GALR2 receptor [J].
Borowsky, B ;
Walker, MW ;
Huang, LY ;
Jones, KA ;
Smith, KE ;
Bard, J ;
Branchek, TA ;
Gerald, C .
PEPTIDES, 1998, 19 (10) :1771-1781
[4]   MOLECULAR-CLONING OF A NOVEL HUMAN MELANOCORTIN RECEPTOR [J].
CHHAJLANI, V ;
MUCENIECE, R ;
WIKBERG, JES .
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1993, 195 (02) :866-873
[5]   MOLECULAR-CLONING, FUNCTIONAL EXPRESSION AND PHARMACOLOGICAL CHARACTERIZATION OF A HUMAN BRADYKININ-B2 RECEPTOR GENE [J].
EGGERICKX, D ;
RASPE, E ;
BERTRAND, D ;
VASSART, G ;
PARMENTIER, M .
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1992, 187 (03) :1306-1313
[6]  
Fang Y, 2002, CHEMBIOCHEM, V3, P987, DOI 10.1002/1439-7633(20021004)3:10<987::AID-CBIC987>3.0.CO
[7]  
2-M
[8]   Membrane protein microarrays [J].
Fang, Y ;
Frutos, AG ;
Lahiri, J .
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 2002, 124 (11) :2394-2395
[9]   CLONING OF THE CDNA FOR THE HUMAN BETA-1-ADRENERGIC RECEPTOR [J].
FRIELLE, T ;
COLLINS, S ;
DANIEL, KW ;
CARON, MG ;
LEFKOWITZ, RJ ;
KOBILKA, BK .
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1987, 84 (22) :7920-7924
[10]   THE HUMAN MU-OPIOID RECEPTOR - MODULATION OF FUNCTIONAL DESENSITIZATION BY CALCIUM CALMODULIN-DEPENDENT PROTEIN-KINASE AND PROTEIN-KINASE-C [J].
MESTEK, A ;
HURLEY, JH ;
BYE, LS ;
CAMPBELL, AD ;
CHEN, Y ;
TIAN, MT ;
LIU, J ;
SCHULMAN, H ;
YU, L .
JOURNAL OF NEUROSCIENCE, 1995, 15 (03) :2396-2406