Format

Send to

Choose Destination
Biochem Pharmacol. 2013 Jan 15;85(2):147-52. doi: 10.1016/j.bcp.2012.08.021. Epub 2012 Sep 10.

Opportunities for functional selectivity in GPCR antibodies.

Author information

1
Department of Molecular Biology, The Scripps Research Institute, La Jolla, CA 92037, USA. dwebb@scripps.edu

Abstract

Monoclonal antibodies (mAbs) have been used for decades as tools to probe the biology and pharmacology of receptors in cells and tissues. They are also increasingly being developed for clinical purposes against a broad range of targets, albeit to a lesser extent for G-protein-coupled receptors (GPCRs) relative to other therapeutic targets. Recent pharmacological, structural and biophysical data have provided a great deal of new insight into the molecular details, complexity and regulation of GPCR function. Whereas GPCRs used to be viewed as having either "on" or "off" conformational states, it is now recognized that their structures may be finely tuned by ligands and other interacting proteins, leading to the selective activation of specific signaling pathways. This information coupled with new technologies for the selection of mAbs targeting GPCRs will be increasingly deployed for the development of highly selective mAbs that recognize conformational determinants leading to novel therapeutics.

PMID:
22975405
PMCID:
PMC3729224
DOI:
10.1016/j.bcp.2012.08.021
[Indexed for MEDLINE]
Free PMC Article

Supplemental Content

Full text links

Icon for Elsevier Science Icon for PubMed Central
Loading ...
Support Center