Angiotensin II signal transduction: an update on mechanisms of physiology and pathophysiology

SJ Forrester, GW Booz, CD Sigmund… - Physiological …, 2018 - journals.physiology.org
The renin-angiotensin-aldosterone system plays crucial roles in cardiovascular physiology
and pathophysiology. However, many of the signaling mechanisms have been unclear. The …

Molecular signatures of G-protein-coupled receptors

AJ Venkatakrishnan, X Deupi, G Lebon, CG Tate… - Nature, 2013 - nature.com
G-protein-coupled receptors (GPCRs) are physiologically important membrane proteins that
sense signalling molecules such as hormones and neurotransmitters, and are the targets of …

Crystal structure of the β2 adrenergic receptor–Gs protein complex

SGF Rasmussen, BT DeVree, Y Zou, AC Kruse… - Nature, 2011 - nature.com
G protein-coupled receptors (GPCRs) are responsible for the majority of cellular responses
to hormones and neurotransmitters as well as the senses of sight, olfaction and taste. The …

High-Resolution Crystal Structure of an Engineered Human β2-Adrenergic G Protein–Coupled Receptor

V Cherezov, DM Rosenbaum, MA Hanson… - science, 2007 - science.org
Heterotrimeric guanine nucleotide–binding protein (G protein)–coupled receptors constitute
the largest family of eukaryotic signal transduction proteins that communicate across the …

Structure of a nanobody-stabilized active state of the β2 adrenoceptor

SGF Rasmussen, HJ Choi, JJ Fung, E Pardon… - Nature, 2011 - nature.com
G protein coupled receptors (GPCRs) exhibit a spectrum of functional behaviours in
response to natural and synthetic ligands. Recent crystal structures provide insights into …

Structural insights into µ-opioid receptor activation

W Huang, A Manglik, AJ Venkatakrishnan… - Nature, 2015 - nature.com
Activation of the μ-opioid receptor (μOR) is responsible for the efficacy of the most effective
analgesics. To shed light on the structural basis for μOR activation, here we report a 2.1 Å X …

Crystal structure of the human β2 adrenergic G-protein-coupled receptor

SGF Rasmussen, HJ Choi, DM Rosenbaum… - Nature, 2007 - nature.com
Structural analysis of G-protein-coupled receptors (GPCRs) for hormones and
neurotransmitters has been hindered by their low natural abundance, inherent structural …

Impact of GPCR structures on drug discovery

M Congreve, C de Graaf, NA Swain, CG Tate - Cell, 2020 - cell.com
Structures of 70 unique G protein-coupled receptors (GPCRs) have been determined, with
over 370 structures in total bound to different ligands and the receptors in various …

Activation and allosteric modulation of a muscarinic acetylcholine receptor

AC Kruse, AM Ring, A Manglik, J Hu, K Hu, K Eitel… - Nature, 2013 - nature.com
Despite recent advances in crystallography and the availability of G-protein-coupled
receptor (GPCR) structures, little is known about the mechanism of their activation process …

Adenosine receptors as drug targets—what are the challenges?

JF Chen, HK Eltzschig, BB Fredholm - Nature reviews Drug discovery, 2013 - nature.com
Adenosine signalling has long been a target for drug development, with adenosine itself or
its derivatives being used clinically since the 1940s. In addition, methylxanthines such as …