Edda S. F. Matthees

Cell-based and isoform-selective G protein-coupled receptor kinase assays for comprehensive inhibitor evaluation

Nina Kathleen Blum, Manuela C. Kiefer, Angelika Decker, Laura Klement et autres

G protein-coupled receptor (GPCR) signaling is regulated by four ubiquitously expressed GPCR kinase isoforms (GRKs), namely GRK2, GRK3, GRK5, and GRK6. Overexpression of individual GRKs occurs in diseases like cancer and heart failure, prompting a search for potent GRK inhibitors. While various …

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Novel atypical G protein-coupled receptor (GPCR)-arrestin complexes: a structural snapshot of the barcode hypothesis

Jenny C. Filor, Edda S. F. Matthees, Carsten Hoffmann

In a recent study published in Nature by Chen et al . , six novel cryo-EM structures of atypical chemokine receptor 3 (ACKR3) complexes with Arrestin2 (Arr2, also known as β-arrestin1) and Arrestin3 (Arr3, also known as β-arrestin2) were resolved using a …

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Helix-bundle and C-terminal GPCR domains differentially influence GRK-specific functions and β-arrestin-mediated regulation

Edda S. F. Matthees, Raphael Silvanus Haider, Laura Klement, Mona Reichel et autres

G protein-coupled receptors (GPCRs) orchestrate diverse physiological responses via signaling through G proteins, GPCR kinases (GRKs), and arrestins. While most G protein functions are well-established, the contributions of GRKs and arrestins remain incompletely understood. Here, we investigate the influence of β-arrestin-interacting GPCR …

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GPCR kinases phosphorylate GPCR C-terminal peptides in a hierarchical manner

Arnelle Löbbert, Nils Lorz, Edda S. F. Matthees, Philip Rößler et autres

Responses from G protein-coupled receptors (GPCRs) are downregulated in a precisely orchestrated process called desensitization. This process consists of two major steps: phosphorylation of the receptor by GPCR kinases (GRKs), predominantly on its C-terminus, and recruitment of arrestin, resulting in different signaling …

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GRKs phosphorylate GPCR C-terminal peptides in a hierarchical manner

Arnelle Löbbert, Nils Lorz, Edda S. F. Matthees, Philip Rößler et autres

Abstract Responses from G protein-coupled receptors (GPCRs) are downregulated in a precisely orchestrated process called desensitization. This process consists of two major steps: phosphorylation of the receptor by GPCR kinases (GRKs), predominantly on its C-terminus, and recruitment of arrestin, resulting in different …

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Isoprenaline shows unique kinase dependencies in stimulating β1AR–β-arrestin2 interaction compared to endogenous catecholamines

Edda S. F. Matthees, Luca E Kletzin, Arnelle Löbbert, Jana S Hoffmann et autres

AR regulation, emphasizing the need to consider these differences when translating molecular insights into physiological contexts. SIGNIFICANCE STATEMENT: Our findings reveal mechanistic differences in β1-adrenergic receptor-mediated catalytic activation of β-arrestin2 by synthetic and endogenous agonists, driven by distinct G protein-coupled receptor kinases …

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DGPT news: Fritz Külz Award 2024

Edda S. F. Matthees

Keywords G protein-coupled receptors • Signaling regulation • Biased agonism G protein-coupled receptors (GPCRs) are prominent drug targets, due to their high accessibility at the plasma membrane and broad involvement in physiological processes (Hauser et al. 2017).As this family of receptors lack …

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Relating GPCR Domains with Functionality: Receptor Helix-Bundle and C-Terminus Differentially Influence GRK-Specific Functions and β-Arrestin-Mediated Regulation (Abstract ID: 159808)

Edda S. F. Matthees, Raphael Silvanus Haider, Laura Klement, Mona Reichel et autres

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Relating GPCR domains with functionality: receptor helix-bundle and C-terminus differentially influence GRK-specific functions and β-arrestin-mediated regulation

Edda S. F. Matthees, Raphael Silvanus Haider, Laura Klement, Mona Reichel et autres

Abstract 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 contributions of GRKs and arrestins remain incompletely understood. Here, we …

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The Ca2+-sensing receptor and the pocketome: comparing nature’s complexity with human intervention in receptor modulation

Edda S. F. Matthees, Carsten Hoffmann

In a recent paper published in Nature, 1 the relatively understudied Ca 2+ -sensing receptor (CaSR) within the G protein-coupled receptor (GPCR) family C, gained attention due to pioneering research led by Georgios Skiniotis from Stanford University, with four shared first authors. …

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GRK specificity and Gβγ dependency determines the potential of a GPCR for arrestin-biased agonism

Edda S. F. Matthees, Jenny C. Filor, Natasha Jaiswal, Mona Reichel et autres

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 subfamilies. GRK2/3 interact with activated G protein βγ-subunits to translocate to the membrane. Yet, …

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Gαs is dispensable for β-arrestin coupling but dictates GRK selectivity and is predominant for gene expression regulation by β2-adrenergic receptor

Valeria Burghi, Justine S. Paradis, Sendi Rafael Adame-Garcia, Xingyu Wu et autres

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 approaches revealed that whereas G proteins are essential for mitogen-activated protein kinase …

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