This subproject is one of many research subprojects utilizing the resources provided by a Center grant funded by NIH/NCRR. The subproject and investigator (PI) may have received primary funding from another NIH source, and thus could be represented in other CRISP entries. The institution listed is for the Center, which is not necessarily the institution for the investigator. Fluorescent labeling is used to directly monitor structural changes in a G protein-coupled receptor in response to drug binding. Purified beta2 adrenergic receptor was covalently labeled with withe different cysteine-reactive fluorescent probes. We found that binding of full agonist, isoproterenol result in decrease of steady-state fluorescence intensity. Time-resolved study of labeled beta2 adrenergic receptor are expected to yield a direct information regarding conformational events which follows ligand binding process.
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