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Single Molecule Analysis of G Protein Coupled Receptor Activation
Brian
Kobilka, Molec. & Cell. Phys.
Gadi Peleg, Chemistry
Richard
Zare, Chemistry
Peiman Ghanouni, Molec. & Cell. Phys
G protein coupled receptors (GPCR) constitute
one of the largest families of integral membrane
proteins and are responsible for the majority
of transmembrane signal transduction. They represent
the largest group of targets for drug development.
The b2 adrenergic receptor (b2AR) is a prototypical
member of this large family of integral membrane
proteins. It serves as a paradigm for GPCR activation
and regulation. We used single-molecule spectroscopy
to study drug-induced conformational changes in
the b2AR in an effort to understand the mechanism
by which agonist binding to the extracellular
surface of the receptor leads to intracellular
G protein activation.
These studies provide insight into the conformational
heterogeneity of G protein coupled receptors in
the presence and absence of a bound agonist. |
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