Functional Selectivity Of G Protein-coupled Receptor Ligands: New Opportunities For Drug Discovery (the Receptors)
by Kim Neve /
2009 / English / PDF
3.1 MB Download
Functional selectivity refers to the ability of different ligands
acting at one receptor subtype to activate multiple signaling
pathways in unique combinations; that is, one drug can be an
agonist at pathway A and an antagonist or partial agonist at
pathway B, and another drug can have the reverse profile.
Functional selectivity has profound implications for drug
development, for chemical biology, and for the design of
experiments to characterize receptor function. In Functional
Selectivity of G Protein-Coupled Receptors expert neuroscientists
and pharmacologists review the work that demonstrated the
existence of functional selectivity, placed it within a
theoretical framework, and provided a mechanistic basis for the
phenomenon. This exciting, comprehensive, and future-oriented
volume includes chapters that focus on theoretical and
mechanistic aspects of functional selectivity and that cut across
subfamilies of GPCRs. Additional chapters focus on subfamilies of
therapeutically relevant receptors where there is considerable
evidence of ligand functional selectivity. Accessible and
authoritative, Functional Selectivity of G Protein-Coupled
Receptors is a valuable educational tool and reference source for
students and scientists interested in drug development, chemical
biology, and GPCR function.
Functional selectivity refers to the ability of different ligands
acting at one receptor subtype to activate multiple signaling
pathways in unique combinations; that is, one drug can be an
agonist at pathway A and an antagonist or partial agonist at
pathway B, and another drug can have the reverse profile.
Functional selectivity has profound implications for drug
development, for chemical biology, and for the design of
experiments to characterize receptor function. In Functional
Selectivity of G Protein-Coupled Receptors expert neuroscientists
and pharmacologists review the work that demonstrated the
existence of functional selectivity, placed it within a
theoretical framework, and provided a mechanistic basis for the
phenomenon. This exciting, comprehensive, and future-oriented
volume includes chapters that focus on theoretical and
mechanistic aspects of functional selectivity and that cut across
subfamilies of GPCRs. Additional chapters focus on subfamilies of
therapeutically relevant receptors where there is considerable
evidence of ligand functional selectivity. Accessible and
authoritative, Functional Selectivity of G Protein-Coupled
Receptors is a valuable educational tool and reference source for
students and scientists interested in drug development, chemical
biology, and GPCR function.
