Searchable abstracts of presentations at key conferences in endocrinology
Endocrine Abstracts (2013) 32 S4.2 | DOI: 10.1530/endoabs.32.S4.2

ECE2013 Symposia New advances in GPCRs in endocrinology (3 abstracts)

Biased agonism of the AT1 receptor: perspectives in drug discovery?

J H Hansen


Novo Nordisk A/s, Diabetes Biology, Denmark.


The angiotensin II type 1 receptor (AT1R) belongs to the family of seven trans-membrane (7TM) receptors, also referred to as G-protein coupled receptors. The AT1R is the primary effector of the renin–angiotensin system, and serves as a key regulator of cardiovascular physiology. The importance of the receptor is clearly illustrated be the frequent use of AT1R blockers and ACE inhibitors in cardiovascular medicine. Upon binding of Ang II the AT1R is signals through both G protein-dependent and -independent pathways. The G protein-dependent pathways are well established and studied in detail whereas we know less about G protein-independent pathways. Pharmacological targeted activation and blocking of the signaling cascades provides novel tools to increase the understanding of how these receptors exert their cellular functions and importantly it present a new clinical potential. This so-called biased agonism (or functional selectivity) has been studied extensively for the last decade and the focus is still increasing. In this talk I will introduce the concept of AT1R mediated biased agonism, discuss the underlying complexity of the AT1R signaling transduction networks and gene regulation and present the clinical potential of AT1R biased agonists.

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