Anionic phospholipids control mechanisms of GPCR-G protein recognition

N Thakur, AP Ray, L Sharp, B Jin, A Duong… - Nature …, 2023 - nature.com
G protein-coupled receptors (GPCRs) are embedded in phospholipids that strongly
influence drug-stimulated signaling. Anionic lipids are particularly important for GPCR …

Dynamics and mechanistic underpinnings to pharmacology of class A GPCRs: an NMR perspective

SK Huang, RS Prosser - American Journal of Physiology …, 2022 - journals.physiology.org
One-third of current pharmaceuticals target G protein-coupled receptors (GPCRs), the
largest receptor superfamily in humans and mediators of diverse physiological processes …

Single-Molecule Imaging of Integral Membrane Protein Dynamics and Function

A Modak, Z Kilic, K Chattrakun, DS Terry… - Annual Review of …, 2024 - annualreviews.org
Integral membrane proteins (IMPs) play central roles in cellular physiology and represent
the majority of known drug targets. Single-molecule fluorescence and fluorescence …

Dual mechanisms of cholesterol-GPCR interactions that depend on membrane phospholipid composition

AP Ray, N Thakur, NG Pour, MT Eddy - Structure, 2023 - cell.com
Cholesterol is a critical component of mammalian cell membranes and an allosteric
modulator of G protein-coupled receptors (GPCRs), but divergent views exist on the …

Single-molecule visualization of human A2A adenosine receptor activation by a G protein and constitutively activating mutations

S Wei, NG Pour, S Tiruvadi-Krishnan, AP Ray… - Communications …, 2023 - nature.com
Mutations that constitutively activate G protein-coupled receptors (GPCRs), known as
constitutively activating mutations (CAMs), modify cell signaling and interfere with drugs …

Unravelling the mechanism of neurotensin recognition by neurotensin receptor 1

K Asadollahi, S Rajput, LA de Zhang, CS Ang… - Nature …, 2023 - nature.com
The conformational ensembles of G protein-coupled receptors (GPCRs) include inactive and
active states. Spectroscopy techniques, including NMR, show that agonists, antagonists and …

Single-molecule analysis reveals that a glucagon-bound extracellular domain of the glucagon receptor is dynamic

T Liu, S Khanal, GD Hertslet, R Lamichhane - Journal of Biological …, 2023 - ASBMB
Dynamic information is vital to understanding the activation mechanism of G protein-coupled
receptors (GPCRs). Despite the availability of high-resolution structures of different …

Global insights into the fine tuning of human A2AAR conformational dynamics in a ternary complex with an engineered G protein viewed by NMR

G Ferré, K Anazia, LO Silva, N Thakur, AP Ray… - Cell reports, 2022 - cell.com
G protein-coupled receptor (GPCR) conformational plasticity enables formation of ternary
signaling complexes with intracellular proteins in response to binding extracellular ligands …

[HTML][HTML] Minute-timescale free-energy calculations reveal a pseudo-active state in the adenosine A2A receptor activation mechanism

VM D'Amore, P Conflitti, L Marinelli, V Limongelli - Chem, 2024 - cell.com
G protein-coupled receptors (GPCRs) are membrane proteins targeted by over one-third of
marketed drugs. Understanding their activation mechanism is essential for precise …

Sub-millisecond conformational dynamics of the A2A adenosine receptor revealed by single-molecule FRET

I Maslov, O Volkov, P Khorn, P Orekhov… - Communications …, 2023 - nature.com
The complex pharmacology of G-protein-coupled receptors (GPCRs) is defined by their multi-
state conformational dynamics. Single-molecule Förster Resonance Energy Transfer …