The path to the G protein‐coupled receptor structural landscape: Major milestones and future directions
MM Kogut‐Günthel, Z Zara, A Nicoli… - British Journal of …, 2024 - Wiley Online Library
G protein‐coupled receptors (GPCRs) play a crucial role in cell function by transducing
signals from the extracellular environment to the inside of the cell. They mediate the effects …
signals from the extracellular environment to the inside of the cell. They mediate the effects …
Molecular Biophysics of Class AG Protein Coupled Receptors–Lipids Interactome at a Glance—Highlights from the A2A Adenosine Receptor
E Tzortzini, A Kolocouris - Biomolecules, 2023 - mdpi.com
G protein-coupled receptors (GPCRs) are embedded in phospholipid membrane bilayers
with cholesterol representing 34% of the total lipid content in mammalian plasma …
with cholesterol representing 34% of the total lipid content in mammalian plasma …
Dual mechanisms of cholesterol-GPCR interactions that depend on membrane phospholipid composition
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 …
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
Mutations that constitutively activate G protein-coupled receptors (GPCRs), known as
constitutively activating mutations (CAMs), modify cell signaling and interfere with drugs …
constitutively activating mutations (CAMs), modify cell signaling and interfere with drugs …
Fully activated structure of the sterol-bound Smoothened GPCR-Gi protein complex
ADP Vo, SK Kim, MY Yang… - Proceedings of the …, 2023 - National Acad Sciences
Smoothened (SMO) is an oncoprotein and signal transducer in the Hedgehog signaling
pathway that regulates cellular differentiation and embryogenesis. As a member of the …
pathway that regulates cellular differentiation and embryogenesis. As a member of the …
Lipid Trolling to Optimize A3 Adenosine Receptor-Positive Allosteric Modulators (PAMs)
A3 adenosine receptor (A3AR) positive allosteric modulators (PAMs)(2, 4-disubstituted-1 H-
imidazo [4, 5-c] quinolin-4-amines) allosterically increase the E max of A3AR agonists, but …
imidazo [4, 5-c] quinolin-4-amines) allosterically increase the E max of A3AR agonists, but …
Integrative residue-intuitive machine learning and MD Approach to Unveil Allosteric Site and Mechanism for β2AR
X Chen, K Wang, J Chen, C Wu, J Mao, Y Song… - Nature …, 2024 - nature.com
Allosteric drugs offer a new avenue for modern drug design. However, the identification of
cryptic allosteric sites presents a formidable challenge. Following the allostery nature of …
cryptic allosteric sites presents a formidable challenge. Following the allostery nature of …
[HTML][HTML] Membrane mimetic-dependence of GPCR energy landscapes
We leveraged variable-temperature 19 F-NMR spectroscopy to compare the conformational
equilibria of the human A 2A adenosine receptor (A 2A AR), a class AG protein-coupled …
equilibria of the human A 2A adenosine receptor (A 2A AR), a class AG protein-coupled …
[HTML][HTML] GPCRs in the round: SMA-like copolymers and SMALPs as a platform for investigating GPCRs
H Ayub, RJ Murray, GC Kuyler, F Napier-Khwaja… - Archives of Biochemistry …, 2024 - Elsevier
G-protein-coupled receptors (GPCRs) are the largest family of membrane proteins, regulate
a plethora of physiological responses and are the therapeutic target for 30–40% of clinically …
a plethora of physiological responses and are the therapeutic target for 30–40% of clinically …
Emerging modes of regulation of neuromodulatory G protein-coupled receptors
In the nervous system, G protein-coupled receptors (GPCRs) control neuronal excitability,
synaptic transmission, synaptic plasticity, and, ultimately, behavior through spatiotemporally …
synaptic transmission, synaptic plasticity, and, ultimately, behavior through spatiotemporally …