TY - JOUR
T1 - Uncovering GPCR heteromer-biased ligands
AU - Mustafa, Sanam
AU - Ayoub, Mohammed Akli
AU - Pfleger, Kevin D.G.
N1 - Funding Information:
The authors’ work on GPCR heteromerization is funded by the National Health and Medical Research Council (NHMRC) of Australia (Project Grant #566736) and Dimerix Bioscience Pty Ltd.
PY - 2010
Y1 - 2010
N2 - The formation of complexes involving different G-protein-coupled receptors (GPCRs) is now an established phenomenon, termed heteromerization. The relevance of higher order structures, in particular heteromerization, has been demonstrated by differential pharmacology displayed by GPCR heteromers compared to monomers/homomers of the respective constituent receptor units. The concepts of heteromerization and heteromer-selective/biased ligands introduce exciting opportunities for enhancing signal specificity and therefore have the potential to play a crucial role in future drug discovery.
AB - The formation of complexes involving different G-protein-coupled receptors (GPCRs) is now an established phenomenon, termed heteromerization. The relevance of higher order structures, in particular heteromerization, has been demonstrated by differential pharmacology displayed by GPCR heteromers compared to monomers/homomers of the respective constituent receptor units. The concepts of heteromerization and heteromer-selective/biased ligands introduce exciting opportunities for enhancing signal specificity and therefore have the potential to play a crucial role in future drug discovery.
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U2 - 10.1016/j.ddtec.2010.06.003
DO - 10.1016/j.ddtec.2010.06.003
M3 - Review article
C2 - 24103688
AN - SCOPUS:78649907124
SN - 1740-6749
VL - 7
SP - e77-e85
JO - Drug Discovery Today: Technologies
JF - Drug Discovery Today: Technologies
IS - 1
ER -