Publications

Activation of adenosine A(1) receptors (A(1)R) in the brain causes sedation, reduces anxiety, inhibits seizures, and promotes neuroprotection. Cerebral A(1)R can be visualized using 8-dicyclopropylmethyl-1-(11)C-methyl-3-propyl-xanthine ((11)C-MPDX) and PET. This study aims to test whether (11)C-MPDX can be used for quantitative studies of cerebral A1R in rodents. Methods: (11)C-MPDX was injected (intravenously) into isoflurane-anesthetized male ...

We report the design, synthesis, and validation of the novel compound photocaged N6-cyclopentyladenosine (cCPA) to achieve precisely localized and timed release of the parent adenosine A1 receptor agonist CPA using 405 nm light. Gi protein-coupled A1 receptors (A1Rs) modulate neurotransmission via pre- and post-synaptic routes. The dynamics of the CPA-mediated effect on neurotransmission, characterized by fast activation and slow recovery, make ...

Background and purpose: Many G protein-coupled receptors (GPCRs) can be allosterically modulated by small molecule ligands. This modulation is best understood in terms of the kinetics of the ligand-receptor interaction. However, many current kinetic assays require at least the (radio-) labeling of the orthosteric ligand, which is impractical for studying a range of ligands. Here we describe the application of a so-called competition association ...

Up to 30 % of epilepsy patients suffer from drug-resistant epilepsy (DRE). The search for innovative therapies is therefore important to close the existing treatment gap in these patients. The adenosinergic system possesses potent anticonvulsive effects, mainly through the adenosine A1 receptor (A1R). However, clinical application of A1R agonists is hindered by severe systemic side effects. To achieve local modulation of A1Rs, we employed a ...

OBJECTIVES: To investigate serum lipid profile in early, treatment-naïve psoriatic arthritis (PsA) and to determine whether changes in classical lipids or apolipoproteins are specific to PsA. METHODS: Total cholesterol, non-high-density lipoprotein cholesterol (non-HDL-c), low-density lipoprotein cholesterol (LDL-c), HDL-c, triglycerides, apolipoprotein B (ApoB) and apolipoprotein A1 (ApoA1) were compared in newly diagnosed untreated PsA ...

Background: InformationTumor stroma remodeling is a key feature of malignant tumors and can promote cancer progression. Laminins are major constituents of basement membranes that physically separate the epithelium from the underlying stroma. Results: By employing mouse models expressing high and low levels of the laminin 1 chain (LM1), we highlighted its implication in a tumor-stroma crosstalk, thus leading to increased colon tumor incidence, ...

To measure the diameter and the transsectional area of the internal carotid arteries (ICA) on CT Angiography (CTA) in patients with aplasia of the A1-segment of the ACA (A1) and in patients with symmetrical A1, the mean diameter and area of the ICA on both sides were measured at a level of 2 cm below the skull base with a commercially available CT software in 41 consecutive patients with aplasia of A1 observed during a 12-month period on ...

© 2018 Gouwy, De Buck, Abouelasrar Salama, Vandooren, Knoops, Pörtner, Vanbrabant, Berghmans, Opdenakker, Proost, Van Damme and Struyf. Serum amyloid A1 (SAA1) is a prototypic acute phase protein, induced to extremely high levels by physical insults, including inflammation and infection. Human SAA and its NH 2 -terminal part have been studied extensively in the context of amyloidosis. By contrast, little is known about COOH-terminal fragments of ...

Casein kinase 2 (CK2) is a ubiquitous pleiotropic enzyme that is highly conserved across eukaryotic kingdoms. CK2 is singular amongst kinases as it is highly rigid and constitutively active. Arabidopsis thaliana is widely used as a model system in molecular plant research; the biological functions of A. thaliana CK2 are well studied in vivo and many of its substrates have been identified. Here, crystal structures of the alpha subunit of A. ...

Infection, sterile injury, and chronic inflammation trigger the acute phase response in order to re-establish homeostasis. This response includes production of positive acute phase proteins in the liver, such as members of the serum amyloid A (SAA) family. In humans the major acute phase SAAs comprise a group of closely related variants of SAA1 and SAA2. SAA1 was proven to be chemotactic for several leukocyte subtypes through activation of the G ...