Molecular mechanisms of metabotropic GABAB receptor function

H Shaye, B Stauch, C Gati, V Cherezov - Science advances, 2021 - science.org
Metabotropic γ-aminobutyric acid G protein–coupled receptors (GABAB) represent one of
the two main types of inhibitory neurotransmitter receptors in the brain. These receptors act …

Sampling alternative conformational states of transporters and receptors with AlphaFold2

D Del Alamo, D Sala, HS Mchaourab, J Meiler - Elife, 2022 - elifesciences.org
Equilibrium fluctuations and triggered conformational changes often underlie the functional
cycles of membrane proteins. For example, transporters mediate the passage of molecules …

Structural basis of GPCR coupling to distinct signal transducers: implications for biased signaling

M Seyedabadi, M Gharghabi, EV Gurevich… - Trends in biochemical …, 2022 - cell.com
Three classes of G-protein-coupled receptor (GPCR) partners–G proteins, GPCR kinases,
and arrestins–preferentially bind active GPCRs. Our analysis suggests that the structures of …

[HTML][HTML] Understanding the molecular mechanisms of odorant binding and activation of the human OR52 family

C Choi, J Bae, S Kim, S Lee, H Kang, J Kim… - Nature …, 2023 - nature.com
Structural and mechanistic studies on human odorant receptors (ORs), key in olfactory
signaling, are challenging because of their low surface expression in heterologous cells …

Conformational rearrangement during activation of a metabotropic glutamate receptor

BW Liauw, HS Afsari, R Vafabakhsh - Biophysical Journal, 2021 - cell.com
The ability to sense external stimuli and dynamically respond lies at the core of cellular
homeostasis. G protein-coupled receptors (GPCRs), the largest family of membrane proteins …

Allosteric coupling and biased agonism in G protein‐coupled receptors

A Bock, M Bermudez - The FEBS Journal, 2021 - Wiley Online Library
G protein‐coupled receptors (GPCRs) are essential cell membrane signaling molecules and
represent the most important class of drug targets. Some signaling pathways downstream of …

Cryo–electron microscopy structure of the antidiuretic hormone arginine-vasopressin V2 receptor signaling complex

J Bous, H Orcel, N Floquet, C Leyrat, J Lai-Kee-Him… - Science …, 2021 - science.org
The antidiuretic hormone arginine-vasopressin (AVP) forms a signaling complex with the V2
receptor (V2R) and the Gs protein, promoting kidney water reabsorption. Molecular …

[HTML][HTML] Molecular interaction of HIC, an agonist of P2Y1 receptor, and its role in prostate cancer apoptosis

HTT Le, A Murugesan, T Ramesh, O Yli-Harja… - International journal of …, 2021 - Elsevier
Prostate cancer is a heterogeneous, slow growing asymptomatic cancer that predominantly
affects man. A purinergic G-protein coupled receptor, P2Y1R, is targeted for its therapeutic …

Allosteric communication regulates ligand‐specific GPCR activity

N Ma, AK Nivedha, N Vaidehi - The FEBS journal, 2021 - Wiley Online Library
G protein‐coupled receptors (GPCRs) are membrane‐bound proteins that are ubiquitously
expressed in many cell types and take part in mediating multiple signaling pathways …

[HTML][HTML] Allosteric Modulators of Dopamine D2 Receptors for Fine-Tuning of Dopaminergic Neurotransmission in CNS Diseases: Overview, Pharmacology, Structural …

AA Kaczor, TM Wróbel, D Bartuzi - Molecules, 2022 - mdpi.com
Allosteric modulation of G protein-coupled receptors (GPCRs) is nowadays a hot topic in
medicinal chemistry. Allosteric modulators, ie, compounds which bind in a receptor site …