title: Micromechanical measurement of membrane receptor binding for label-free drug discovery.
abstract: 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.
authors.affiliation: Institute for Micromanufacturing, Louisiana Tech University, Ruston, LA 71272, USA.
authors.forename: Yifei
authors.initials: Y
authors.lastname: Zhang
authors.forename: Srinivasan P
authors.initials: SP
authors.lastname: Venkatachalan
authors.forename: Hao
authors.initials: H
authors.lastname: Xu
authors.forename: Xiaohe
authors.initials: X
authors.lastname: Xu
authors.forename: Prasad
authors.initials: P
authors.lastname: Joshi
authors.forename: Hai-Feng
authors.initials: HF
authors.lastname: Ji
authors.forename: Marvin
authors.initials: M
authors.lastname: Schulte
mesh_terms: D002462:Cell Membrane / Q000378:metabolism*; D036103:Nanotechnology; D044406:Receptors, Serotonin, 5-HT3 / Q000378:metabolism*; D013997:Time Factors
chemical_list: D044406:Receptors, Serotonin, 5-HT3