Carina Halleskog

3032-LB: ß2-Adrenergic Receptor Modulators Improve Insulin Sensitivity in Obese and PI3K-Mutant Mice

ANASTASIA KALINOVICH, Muhammad Hamza Bokhari, JASPER DE JONG, Nodi Dehvari et autres

Introduction and Objective: Skeletal muscle is a pivotal regulator of whole-body metabolism, as it accounts for a substantial proportion of postprandial insulin-stimulated glucose disposal and is a major contributor to total energy expenditure. In this context, activation of β2adrenergic receptors (β2AR) in …

GRK-biased adrenergic agonists for the treatment of type 2 diabetes and obesity

Aikaterini Motso, Benjamin Pelcman, Anastasia Kalinovich, Nour Aldin Kahlous et autres

(Cell 188, 5142–5156.e1–e23; September 18, 2025)In the original online version of the article, the predicted binding modes for compounds 15 and 21 were mislabeled as 21 and 15, respectively, in Figure 3C. The template and mutant constructs of β2AR were incorrectly referred …

GRK-biased adrenergic agonists for the treatment of type 2 diabetes and obesity

Aikaterini Motso, Benjamin Pelcman, Anastasia Kalinovich, Nour Aldin Kahlous et autres

Biased agonism of G protein-coupled receptors (GPCRs) offers potential for safer medications. Current efforts have explored the balance between G proteins and β-arrestin; however, other transducers like GPCR kinases (GRKs) remain understudied. GRK2 is essential for β 2 adrenergic receptor (β 2 …

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The novel adrenergic agonist ATR-127 targets skeletal muscle and brown adipose tissue to tackle diabesity and steatohepatitis

Emanuela Talamonti, Jelena Davegardh, Anastasia Kalinovich, Sten M. M. van Beek et autres

OBJECTIVE: Simultaneous activation of β2- and β3-adrenoceptors (ARs) improves whole-body metabolism via beneficial effects in skeletal muscle and brown adipose tissue (BAT). Nevertheless, high-efficacy agonists simultaneously targeting these receptors whilst limiting activation of β1-ARs - and thus inducing cardiovascular complications - are …

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Development of novel β2-adrenergic receptor agonists for the stimulation of glucose uptake – The importance of chirality and ring size of cyclic amines

Krista Jaunsleine, Linda Supe, Jana Spura, Sten van Beek et autres

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Use of Isothermal Microcalorimetry to Measure Cellular Heat Production in Thermogenic Adipocytes

Muhammad Hamza Bokhari, Carina Halleskog, Irina G. Shabalina, Tore Bengtsson

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Development of Novel Β2-Adrenergic Receptor Agonists for the Stimulation of Glucose Uptake - the Importance of Chirality and Ring Size of Cyclic Amines

Krista Jaunsleine, Linda Supe, Jana Spura, Sten van Beek et autres

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Isothermal microcalorimetry measures UCP1-mediated thermogenesis in mature brite adipocytes

Muhammad Hamza Bokhari, Carina Halleskog, Alice Åslund, Nathalie Boulet et autres

Abstract The activation of thermogenesis in adipose tissue has emerged as an important target for the development of novel anti-obesity therapies. Using multi-well isothermal microcalorimetry, we have demonstrated that mature murine brown and brite adipocytes produce quantifiable heat upon β3-AR stimulation, independently …

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Treatment with a β-2-adrenoceptor agonist stimulates glucose uptake in skeletal muscle and improves glucose homeostasis, insulin resistance and hepatic steatosis in mice with diet-induced obesity

Anastasia Kalinovich, Nodi Dehvari, Alice Åslund, Sten van Beek et autres

Abstract Aims/hypothesis Chronic stimulation of β2-adrenoceptors, opposite to acute treatment, was reported to reduce blood glucose levels, as well as to improve glucose and insulin tolerance in rodent models of diabetes by essentially unknown mechanisms. We recently described a novel pathway that …

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WNT signaling in microglia : WNTs as novel regulators of microglia

Carina Halleskog

Microglia, the immunocompetent cells of the central nervous system (CNS) and the brain’s own macrophages are the most motile cells in the CNS and those with highest plasticity, as they rapidly move their projections to actively screen their environment for any type …

WNT ‐3A and WNT ‐5A counteract lipopolysaccharide‐induced pro‐inflammatory changes in mouse primary microglia

Carina Halleskog, Gunnar Schulte

Surveying microglia, the resident macrophage-like cells in the central nervous system, continuously screen their surroundings to sense imbalance in tissue homeostasis. Their activity is tightly regulated in both a pro- and anti-inflammatory manner. We have previously shown that the lipoglycoproteins WNT-3A and …

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WNT SIGNALING IN MICROGLIA

Carina Halleskog