Journal
BIOCHEMICAL PHARMACOLOGY
Volume 85, Issue 2, Pages 147-152Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bcp.2012.08.021
Keywords
GPCR; Ligand induced conformation; Biased signaling; Monoclonal antibody; Therapeutic antibody
Categories
Funding
- National Institutes of Health/National Institute of General Medical Sciences [U54 GM094618, U01 GM094612, R21 AI101687]
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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. (C) 2012 Elsevier Inc. All rights reserved.
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