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Journal of Biomolecular Screening
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Cell-Based Assays for G-Protein-Coupled/Tyrosine Kinase-Coupled Receptors

Mark R. Brann

Receptor Technologies Inc., 276 East Allen, Winooski, Vermont 05404

Terri Messier

Receptor Technologies Inc., 276 East Allen, Winooski, Vermont 05404

Christine Dorman

Receptor Technologies Inc., 276 East Allen, Winooski, Vermont 05404

Deborah Lannigan

Receptor Technologies Inc., 276 East Allen, Winooski, Vermont 05404

Using mammalian cells transiently transfected with receptors, we have developed an assay [Receptor Selection and Amplification Technology (R-SAT); patents pending] that links ligand-dependent cellular transformation to induction of 8-galactosidase in a 96-well plate format. Using these procedures, we have performed high throughput functional assays of receptors that mediate signal transduction by a diversity of mechanisms. Examples include the prostanoid, muscarinic, and neurokinin receptor subtypes that signal via the G-proteins Gq and Gi, the JAK/STAT-linked GM-CSF receptor, the tyrosine kinase neurotrophin receptors, and the classical oncogenes v-ras and p53. The assays have been formatted such that many receptors can be assayed simultaneously (>10 receptors per well) and precise discrimination of ligand efficacy can be obtained (e.g., full and partial agonists, negative and neutral antagonists).

Journal of Biomolecular Screening, Vol. 1, No. 1, 43-45 (1996)
DOI: 10.1177/108705719600100114


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