Uncovering GPCR heteromer-biased ligands

Sanam Mustafa; Mohammed Akli Ayoub; Kevin D.G. Pfleger

doi:10.1016/j.ddtec.2010.06.003

Uncovering GPCR heteromer-biased ligands

Sanam Mustafa
, Mohammed Akli Ayoub
, Kevin D.G. Pfleger

Research output: Contribution to journal › Review article › peer-review

17 Citations (Scopus)

Abstract

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.

Original language	English
Pages (from-to)	e77-e85
Journal	Drug Discovery Today: Technologies
Volume	7
Issue number	1
DOIs	https://doi.org/10.1016/j.ddtec.2010.06.003
Publication status	Published - 2010
Externally published	Yes

ASJC Scopus subject areas

Molecular Medicine
Drug Discovery

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10.1016/j.ddtec.2010.06.003

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title = "Uncovering GPCR heteromer-biased ligands",

abstract = "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.",

author = "Sanam Mustafa and Ayoub, \{Mohammed Akli\} and Pfleger, \{Kevin D.G.\}",

note = "Funding Information: The authors{\textquoteright} 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.",

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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.

UR - https://www.scopus.com/pages/publications/78649907124

UR - https://www.scopus.com/pages/publications/78649907124#tab=citedBy

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 -

Uncovering GPCR heteromer-biased ligands

Abstract

ASJC Scopus subject areas

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