Micromechanical measurement of membrane receptor binding for label-free drug discovery.
A potential novel binding assay based on binding-driven micromechanical motion is described. A membrane preparation containing 5-HT(3AS) receptors was used to modify a microcantilever. The modified microcantilever was found to bend on application of the naturally occurring agonist (5-hydroxytryptamine, which is also called serotonin) or the antagonist MDL-72222, but not to other similar molecules. Control experiments show that cantilevers modified by membrane preparations that do not contain 5-HT(3AS) receptors do not respond to serotonin or MDL-72222. K(d) values obtained for serotonin and MDL-72222 are identical to those obtained from radio-ligand binding assays. These results suggest that the microcantilever system has potential for use in label-free, drug screening applications.
Zhang
Yifei
Y
Institute for Micromanufacturing, Louisiana Tech University, Ruston, LA 71272, USA.
Venkatachalan
Srinivasan P
SP
Xu
Hao
H
Xu
Xiaohe
X
Joshi
Prasad
P
Ji
Hai-Feng
HF
Schulte
Marvin
M
D002462:Cell Membrane / Q000378:metabolism*; D036103:Nanotechnology; D044406:Receptors, Serotonin, 5-HT3 / Q000378:metabolism*; D013997:Time Factors
D044406:Receptors, Serotonin, 5-HT3