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 …

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 …

Positive allosteric mechanisms of adenosine A1 receptor-mediated analgesia

CJ Draper-Joyce, R Bhola, J Wang, A Bhattarai… - Nature, 2021 - nature.com
The adenosine A1 receptor (A1R) is a promising therapeutic target for non-opioid analgesic
agents to treat neuropathic pain,. However, development of analgesic orthosteric A1R …

Mitochondrial remodeling and ischemic protection by G protein–coupled receptor 35 agonists

GA Wyant, W Yu, IIP Doulamis, RS Nomoto, MY Saeed… - Science, 2022 - science.org
Kynurenic acid (KynA) is tissue protective in cardiac, cerebral, renal, and retinal ischemia
models, but the mechanism is unknown. KynA can bind to multiple receptors, including the …

Yeast surface display platform for rapid discovery of conformationally selective nanobodies

C McMahon, AS Baier, R Pascolutti… - Nature structural & …, 2018 - nature.com
Camelid single-domain antibody fragments ('nanobodies') provide the remarkable specificity
of antibodies within a single 15-kDa immunoglobulin VHH domain. This unique feature has …

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 …

Nanodiscs in membrane biochemistry and biophysics

IG Denisov, SG Sligar - Chemical reviews, 2017 - ACS Publications
Membrane proteins play a most important part in metabolism, signaling, cell motility,
transport, development, and many other biochemical and biophysical processes which …

Multiscale simulations of biological membranes: the challenge to understand biological phenomena in a living substance

G Enkavi, M Javanainen, W Kulig, T Róg… - Chemical …, 2019 - ACS Publications
Biological membranes are tricky to investigate. They are complex in terms of molecular
composition and structure, functional over a wide range of time scales, and characterized by …

Structural insights into G-protein-coupled receptor allostery

DM Thal, A Glukhova, PM Sexton, A Christopoulos - Nature, 2018 - nature.com
G-protein-coupled receptors (GPCRs) are key cell-surface proteins that transduce external
environmental cues into biochemical signals across the membrane. GPCRs are intrinsically …

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 …