Characterization of constitutively active mutants of G protein-coupled receptors.

Publication/Presentation Date

1-1-2006

Abstract

The ability of G protein-coupled receptors to transduce signaling typically is induced by the binding of an appropriate ligand (agonist), resulting in a conformational change of the receptor and the subsequent interaction with the G protein heterotrimer. Some mutants of G protein-coupled receptors, known as constitutively active mutants, have the capacity to activate the G protein-signaling cascade even in the absence of ligand. In this chapter, we describe three methods that most directly allow characterization of constitutively active mutants and discriminate them from the wild-type receptors. All methods are based on the spontaneous signaling function in the absence of ligand and its consequences on the receptor.

Volume

332

First Page

129

Last Page

139

ISSN

1064-3745

Disciplines

Business Administration, Management, and Operations | Health and Medical Administration | Management Sciences and Quantitative Methods

PubMedID

16878689

Department(s)

Administration and Leadership

Document Type

Article

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