A. Inoue

OrgaMeas: A pipeline that integrates all the processes of organelle image analysis

OrgaMeas provides a high-throughput image analysis pipeline for accurate organelle morphology and dynamics measurement using deep learning tools.

Four-color single-molecule imaging system for tracking GPCR dynamics with fluorescent HiBiT peptide

The paper develops a four-color single-molecule imaging system using fluorescent HiBiT peptides to track GPCR dynamics and interactions in living cells.

Structural and Dynamic Insights into the Biased Signaling Mechanism of the Human Kappa Opioid Receptor

This study investigates the structural dynamics of the human KOR-Gi signaling complex with G-protein-biased and balanced agonists, identifying key residues involved in signaling bias.

Structural insights into sphingosine 1-phosphate receptor 4 activation

The paper determines the cryo-EM structure of activated S1PR4, revealing mechanisms of ligand recognition and Gi coupling to aid in developing safer S1PR4 agonists.

Multi-faceted roles of β-arrestins in G protein-coupled receptors endocytosis

The paper challenges the conventional view of GPCR internalization by showing multiple pathways regulate receptor internalization, with specific findings on the GLP-1R's mechanism.

Characterization of Gαs and Gαolf activation by catechol and non-catechol dopamine D1 receptor agonists

This study evaluates how different dopamine D1 receptor agonists activate Gαs and Gαolf, revealing region-specific pharmacological profiles with implications for targeted drug development.

A single domain intrabody targeting the follicle-stimulating hormone receptor (FSHR) impacts FSH-induced G protein-dependent signalling

The paper characterizes an intrabody that modulates FSHR signaling by reducing cAMP production without affecting Gs recruitment.

ArreSTick Motif is Responsible for GPCR-beta-Arrestin Binding Stability and Extends Phosphorylation-Dependent beta-arrestin Interactions to Non-Receptor Proteins

The paper identifies the arreSTick motif as a key determinant of GPCR-{beta}-arrestin binding stability and shows its presence in non-receptor proteins.

Structure of the human Duffy antigen receptor

This study determines the cryo-EM structure of the Duffy antigen receptor bound to CCL7, revealing structural features that explain its unique functional properties and lack of G protein coupling.

Cell swelling enhances canonical β-adrenergic signaling

The paper shows that osmotic swelling enhances β2-adrenergic receptor activity and downstream cAMP responses in cardiomyocytes and other cell types.

Receptor endocytosis orchestrates the spatiotemporal bias of β-arrestin signaling

The study shows that β-arrestin signaling bias is spatiotemporally determined by ligand dissociation rate and G protein activity at endosomes, not receptor conformation.

Phosphorylation barcodes direct biased chemokine signaling at CXCR3

The paper shows that CXCR3 chemokines use different phosphorylation barcodes to activate distinct signaling pathways, leading to varied physiological outcomes.

The dynamic nature of neurotensin receptor 1 (NTS1) allostery and signaling bias

This study investigates NTS1 allostery and signaling bias using NMR, showing PIP2 enhances transducer complexation through allosteric connections and β-arrestin modulates receptor conformation.

Endosomal Chemokine Receptor Signalosomes Regulate Central Mechanisms Underlying Cell Migration

This study shows endosomal chemokine receptor signaling, specifically through CCR7, enhances Rac1 activity and immune T cell chemotaxis by recruiting G protein and β-arrestin.

Ligands tune the local and global motions of neurotensin receptor 1 (NTS1): a DFT-guided solution NMR analysis

This study uses NMR and DFT to analyze sub-nanosecond motions of NTS1, showing ligands affect conformational entropy and dynamics.

Activation of the urotensin-II receptor by anti-COVID-19 drug remdesivir induces cardiomyocyte dysfunction

This study identifies remdesivir as a selective agonist of the urotensin-II receptor, linking its cardiotoxicity to receptor activation and genetic variants.

Modulation of cannabinoid receptor signaling by endocannabinoids

This study investigates how endocannabinoids modulate CB1 receptor signaling by comparing their activation of Gi1 with synthetic cannabinoids and revealing structural differences in ligand binding.

Molecular insights into intrinsic transducer-coupling bias in the CXCR4-CXCR7 system

This study characterizes the biased agonism of CXCR4 and CXCR7, revealing differences in G-protein coupling, β-arrestin recruitment, and ERK1/2 activation.

Engineered high-density lipoprotein particles that chaperone bioactive lipid mediators to combat endothelial dysfunction and thromboinflammation

This paper constructs engineered HDL-like particles that chaperone bioactive lipids to reduce inflammation and endothelial dysfunction.

The Effect of Ligands and Transducers on the Neurotensin Recep-tor 1 (NTS1) Conformational Ensemble

This study uses 19F-NMR to show ligands and transducers modulate NTS1 conformational substates, revealing dynamic behavior not captured by static structures.

Structural insights into distinct signaling profiles of the μOR activated by diverse agonists

This study compares the structural and signaling differences between two μOR agonists, lofentanil and mitragynine pseudoindoxyl, revealing how their distinct binding modes lead to different G protein and β-arrestin activation profiles.

Expression of mini-G proteins specifically halt cognate GPCR trafficking and intracellular signalling

This paper shows that mini-G proteins block GPCR trafficking and signaling by preventing receptor internalization, and proposes a nanobody-based alternative assay.

Membrane phosphoinositides stabilize GPCR-arrestin complexes and offer temporal control of complex assembly and dynamics

This study identifies membrane phosphoinositides as regulators of GPCR-arrestin complex dynamics, showing they stabilize complexes and enable temporal control of receptor signaling and recycling.

Integrative analysis of scRNAs-seq and scATAC-seq revealed transit-amplifying thymic epithelial cells expressing autoimmune regulator

The paper identifies transit-amplifying thymic epithelial cells expressing Aire and CD80 through integrative scRNA-seq and scATAC-seq analysis.

Common coupling map advances GPCR-G protein selectivity

The paper creates a common coupling map of GPCR-G protein interactions by integrating multiple datasets, revealing selectivity and co-coupling patterns.

Receptor Activity-Modifying Protein 2 (RAMP2) alters glucagon receptor trafficking in hepatocytes with functional effects on receptor signalling

This study investigates how RAMP2 affects GCGR trafficking and signaling in hepatocytes, showing it alters receptor internalization and signaling bias with limited metabolic impact.

A genetic mouse model with postnatal Nf1 and p53 loss recapitulates the histology and transcriptome of human malignant peripheral nerve sheath tumor

This paper develops a genetic mouse model of MPNST that closely mimics human tumors in genetics, histology, and transcriptome.

RAMPs regulate signalling bias and internalisation of the GIPR

This study shows RAMPs modulate GIPR signaling and internalization, with RAMP3 reducing cAMP production and promoting surface retention, while RAMP1/2 decrease Gq/11/15 activation, and RAMP1 is essential for normal glucose regulation.

Constitutive G protein coupling profiles of understudied orphan GPCRs

The paper uses BRET to determine G protein coupling profiles of 48 orphan GPCRs without ligands, identifying 48 receptor-G protein pairs, many previously unknown.

Intrinsic bias at non-canonical, β-arrestin-coupled seven transmembrane receptors

The paper identifies two non-canonical GPCRs, D6R and C5aR2, that exclusively couple to β-arrestins and exhibit distinct GRK preferences and downstream signaling.