TY - JOUR
T1 - Heterodimers of G protein-coupled receptors as novel and distinct drug targets
AU - Rozenfeld, Raphael
AU - Décaillot, Fabien M.
AU - IJzerman, Adriaan P.
AU - Devi, Lakshmi A.
N1 - Funding Information:
We would like to thank Dr. Ivone Gomes for critically reading the article and Dr. Paramjit Arora (NYU) for help with Fig. 2 . This work was supported by the NIH grants DA08863, NS053751 & DA019521 (to L.A.D.).
PY - 2006/6
Y1 - 2006/6
N2 - G protein-coupled receptors (GPCRs) exist as homodimers and also associate with other GPCRs to form heterodimers. This association may alter the function of both receptors, yielding a distinct functional unit with novel properties. The multiple combinations of GPCR heterodimers, the tissue-selective expression of these complexes and their differential activation offer an exciting perspective for the development of tissue- and receptor-subtype-selective drugs. In this review, we will discuss the evidence available till date for the occurrence of GPCR heterodimerization, particularly in vivo, and describe strategies that can be used for the development of heterodimer-selective ligands.
AB - G protein-coupled receptors (GPCRs) exist as homodimers and also associate with other GPCRs to form heterodimers. This association may alter the function of both receptors, yielding a distinct functional unit with novel properties. The multiple combinations of GPCR heterodimers, the tissue-selective expression of these complexes and their differential activation offer an exciting perspective for the development of tissue- and receptor-subtype-selective drugs. In this review, we will discuss the evidence available till date for the occurrence of GPCR heterodimerization, particularly in vivo, and describe strategies that can be used for the development of heterodimer-selective ligands.
UR - http://www.scopus.com/inward/record.url?scp=33846148639&partnerID=8YFLogxK
U2 - 10.1016/j.ddstr.2006.11.001
DO - 10.1016/j.ddstr.2006.11.001
M3 - Review article
AN - SCOPUS:33846148639
SN - 1740-6773
VL - 3
SP - 437
EP - 443
JO - Drug Discovery Today: Therapeutic Strategies
JF - Drug Discovery Today: Therapeutic Strategies
IS - 4
ER -