| Summary: | The concept that 7 transmembrane receptors (7TMRs) exist and function as independent monomers has facilitated a therapeutic approach of selective targeting of receptors. However, oligomerisation of 7TMRs is now being recognised as an important biological phenomenon that adds a level of complexity to their signalling. In vitro , many 7TMR heterodimers display altered binding, signalling, and trafficking properties compared to their constituent monomeric units. This review discusses an emerging concept regarding the role of 7TMR heterodimerisation in vivo , and its significance to drug therapy. Studies of angiotensin receptor signalling indicate a pivotal role for heterodimerisation in the pathogenesis of human disorders. Furthermore, the occurrence of angiotensin receptor heterodimers has profound effect on the responsiveness to treatment with 7TMR blockers. Global assessment of the prevalence of different heterodimers during disease and their responsiveness to drug therapy is likely to optimise patient treatment and reduce side-effects associated with 7TMR blockers.
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