G-protein-coupled receptor microarrays for multiplexed compound screening.
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.
Hong
Yulong
Y
Corning Incorporated, Corning, NY, USA.
Webb
Brian L
BL
Pai
Sadashiva
S
Ferrie
Ann
A
Peng
Jinlin
J
Lai
Fang
F
Lahiri
Joydeep
J
Biddlecome
Gloria
G
Rasnow
Brian
B
Johnson
Michael
M
Min
Hosung
H
Fang
Ye
Y
Salon
John
J
D004353:Drug Evaluation, Preclinical / Q000379:methods*; D005456:Fluorescent Dyes; D066298:In Vitro Techniques; D040081:Protein Array Analysis / Q000379:methods*; D043562:Receptors, G-Protein-Coupled / Q000187:drug effects*
D005456:Fluorescent Dyes; D043562:Receptors, G-Protein-Coupled