Carsten Hoffmann
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View article: Multi-faceted roles of β-arrestins in G protein-coupled receptor endocytosis
Multi-faceted roles of β-arrestins in G protein-coupled receptor endocytosis Open
The internalization of G protein-coupled receptors (GPCRs) is a key process limiting cell surface receptor activity, and possibly promoting their intracellular signaling. Dysregulation of this process has been implicated in various disease…
View article: GRK phosphorylation drives β-arrestin-independent internalization of chemokine receptor CXCR5
GRK phosphorylation drives β-arrestin-independent internalization of chemokine receptor CXCR5 Open
G protein-coupled receptor (GPCR) kinases (GRKs) and β-arrestins act in concert to regulate GPCR signaling and trafficking. Previously, we showed that β-arrestins are essential for desensitization, but not internalization, of the chemokine…
View article: Advancing influenza virus treatment: in vitro and ex vivo studies of PI3K inhibitor-loaded lipid nanoparticles
Advancing influenza virus treatment: in vitro and ex vivo studies of PI3K inhibitor-loaded lipid nanoparticles Open
Influenza A viruses (IAVs) remain a significant global health concern, causing seasonal outbreaks and pandemics with substantial morbidity and mortality, particularly among vulnerable groups. Annual vaccination serves as the primary preven…
View article: Evaluating the Antiviral Efficacy of Encapsulated PKC Inhibitor BIM‐I against influenza A Virus Infection
Evaluating the Antiviral Efficacy of Encapsulated PKC Inhibitor BIM‐I against influenza A Virus Infection Open
Influenza A virus (IAV) infections remain a major global health threat, as current vaccines and antivirals often lose efficacy due to frequent viral mutation and resistance development. This underscores the urgent need for novel therapeuti…
View article: Poly(2‐Oxazoline)‐Based Polyphotoacids: Synthesis, Solution Behavior, and Cellular Uptake of Multi‐Responsive Intracellular Transporters
Poly(2‐Oxazoline)‐Based Polyphotoacids: Synthesis, Solution Behavior, and Cellular Uptake of Multi‐Responsive Intracellular Transporters Open
This work describes the first polymeric photoacids based on poly(2‐oxazoline)s. The presence of 1‐hydroxypyrene units—a photoacid that can increase its acidity upon blue light irradiation through excited‐state proton transfer—allows remote…
View article: Dynamic pharmacophores unveil binding mode ensembles for classical partial agonists at the M<sub>2</sub> receptor
Dynamic pharmacophores unveil binding mode ensembles for classical partial agonists at the M<sub>2</sub> receptor Open
For the prototypic M 2 receptor it has been previously demonstrated that dualsteric partial agonists can stabilize both, active and inactive receptor states, but it remains unclear whether orthosteric partial agonists have a similar mechan…
View article: High-fat diet impairs microbial metabolite production and aggravates influenza A infection
High-fat diet impairs microbial metabolite production and aggravates influenza A infection Open
Background Alterations in the gut microbiom can significantly impact various regions in the human body, including the pulmonary tract. This study investigates alterations in the gut microbiome during a high-fat diet (HFD), particularly sho…
View article: Non-canonical internalization mechanisms of mGlu receptors
Non-canonical internalization mechanisms of mGlu receptors Open
Cell surface G protein-coupled receptors (GPCRs) are tightly regulated through constitutive and agonist-induced internalization. While the mechanisms of constitutive internalization remain elusive, agonist-induced internalization very ofte…
View article: Identification of a regulatory sequence within the third intracellular loop that governs β-arrestin binding to the muscarinic M5 receptor
Identification of a regulatory sequence within the third intracellular loop that governs β-arrestin binding to the muscarinic M5 receptor Open
The M5 muscarinic acetylcholine receptor (M5R) is selectively expressed in dopaminergic neurons and although accounts for <2 % of the total muscarinic receptor population, plays critical roles in many physiological and pathophysiological p…
View article: Cytoplasmic tail composition modulates the G protein and arrestin-3 signaling bias of the adhesion GPCR LPHN2
Cytoplasmic tail composition modulates the G protein and arrestin-3 signaling bias of the adhesion GPCR LPHN2 Open
The class B2 Adhesion GPCRs (aGPCRs) combine cell adhesion with GPCR signaling to control diverse developmental and physiological processes. How aGPCRs interact with and integrate distinct groups of effectors including G proteins, arrestin…
View article: Non-canonical internalization mechanisms of mGlu receptors
Non-canonical internalization mechanisms of mGlu receptors Open
Cell surface density of G protein-coupled receptors (GPCRs) is tightly regulated through constitutive and agonist-induced internalization. Whereas the mechanisms of constitutive internalization remain elusive, agonist-induced internalizati…
View article: GRK5 regulates endocytosis of FPR2 independent of β-arrestins
GRK5 regulates endocytosis of FPR2 independent of β-arrestins Open
The formyl-peptide receptor 2 (FPR2) is a G-protein-coupled receptor that responds to pathogen-derived peptides and regulates both proinflammatory and proresolution cellular processes. While ligand selectivity and G-protein signaling of FP…
View article: Constitutive activity of an atypical chemokine receptor revealed by inverse agonistic nanobodies
Constitutive activity of an atypical chemokine receptor revealed by inverse agonistic nanobodies Open
Chemokine stimulation of atypical chemokine receptor 3 (ACKR3) does not activate G proteins but recruits arrestins. It is a chemokine scavenger that indirectly influences responses by restricting the availability of CXCL12, an agonist shar…
View article: Relating GPCR domains with functionality: receptor helix-bundle and C-terminus differentially influence GRK-specific functions and β-arrestin-mediated regulation
Relating GPCR domains with functionality: receptor helix-bundle and C-terminus differentially influence GRK-specific functions and β-arrestin-mediated regulation Open
G protein-coupled receptors (GPCRs) orchestrate diverse physiological responses via intracellular signaling through G proteins, GPCR kinases (GRKs), and arrestins. While the role of G proteins in receptor signaling is well-established, the…
View article: GRK specificity and Gβγ dependency determines the potential of a GPCR for arrestin-biased agonism
GRK specificity and Gβγ dependency determines the potential of a GPCR for arrestin-biased agonism Open
G protein-coupled receptors (GPCRs) are mainly regulated by GPCR kinase (GRK) phosphorylation and subsequent β-arrestin recruitment. The ubiquitously expressed GRKs are classified into cytosolic GRK2/3 and membrane-tethered GRK5/6 subfamil…
View article: Rapid elucidation of agonist-driven regulation of the neurokinin 1 receptor using a GPCR phosphorylation immunoassay
Rapid elucidation of agonist-driven regulation of the neurokinin 1 receptor using a GPCR phosphorylation immunoassay Open
Agonist-induced phosphorylation is a crucial step in the activation/deactivation cycle of G protein-coupled receptors (GPCRs), but direct determination of individual phosphorylation events has remained a major challenge. We have recently d…
View article: S1PR3 agonism and S1P lyase inhibition rescue mice in the severe state of experimental sepsis
S1PR3 agonism and S1P lyase inhibition rescue mice in the severe state of experimental sepsis Open
Sepsis is characterized as life-threatening organ dysfunction caused by a dysregulated host response to an infection. Despite numerous clinical trials that addressed this syndrome, there is still no causative treatment available to dampen …
View article: Microbially conjugated bile salts found in human bile activate the bile salt receptors TGR5 and FXR
Microbially conjugated bile salts found in human bile activate the bile salt receptors TGR5 and FXR Open
Background: Bile salts of hepatic and microbial origin mediate interorgan cross talk in the gut-liver axis. Here, we assessed whether the newly discovered class of microbial bile salt conjugates (MBSCs) activate the main host bile salt rec…
View article: Multi-faceted roles of β-arrestins in G protein-coupled receptors endocytosis
Multi-faceted roles of β-arrestins in G protein-coupled receptors endocytosis Open
Internalization plays a crucial role in regulating the density of cell surface receptors and has been demonstrated to regulate intracellular signaling. Dysregulation of this process has been implicated in various diseases. The vast majorit…
View article: Gαs is dispensable for β-arrestin coupling but dictates GRK selectivity and is predominant for gene expression regulation by β2-adrenergic receptor
Gαs is dispensable for β-arrestin coupling but dictates GRK selectivity and is predominant for gene expression regulation by β2-adrenergic receptor Open
β-arrestins play a key role in G protein-coupled receptor (GPCR) internalization, trafficking, and signaling. Whether β-arrestins act independently of G protein-mediated signaling has not been fully elucidated. Studies using genome-editing…