A5028074293- Receptor Mechanisms and Signaling
- Mast cells and histamine
- Ion channel regulation and function
- Cellular transport and secretion
- Erythrocyte Function and Pathophysiology
- Protein Kinase Regulation and GTPase Signaling
- Neuropeptides and Animal Physiology
- Nitric Oxide and Endothelin Effects
- Regulation of Appetite and Obesity
- Monoclonal and Polyclonal Antibodies Research
- Protein Structure and Dynamics
- Neuroscience and Neuropharmacology Research
- Adenosine and Purinergic Signaling
- Fibroblast Growth Factor Research
- Parathyroid Disorders and Treatments
- Mass Spectrometry Techniques and Applications
- Chemical Synthesis and Analysis
- Biochemical Analysis and Sensing Techniques
- Advanced Biosensing Techniques and Applications
- Coagulation, Bradykinin, Polyphosphates, and Angioedema
- Asthma and respiratory diseases
University of Copenhagen
2021-2024
Vrije Universiteit Amsterdam
2016-2023
Monash University
2023
The human histamine H3 receptor (hH3R) is predominantly expressed in the CNS, where it regulates synthesis and release of other neurotransmitters. Due to its neuromodulatory role, hH3R has been associated with various CNS disorders, including Alzheimer's Parkinson's disease. Markedly, gene undergoes extensive splicing, resulting 20 isoforms, which 7TM isoforms exhibit variations intracellular loop 3 (IL3) and/or C-terminal tail. Particularly, that display IL3 (e.g., hH3R-365) are shown...
Abstract The calcium-sensing receptor (CaSR) is responsible for sustaining a stable blood calcium concentration. Consequently, genetic and acquired changes in this G protein-coupled can give rise to various homeostasis disorders. Synthetic positive allosteric modulators targeting CaSR are currently used treat hypercalcemia, but their usage highly limited due the high risk of severe hypocalcemia gastrointestinal intolerance. In study, we aimed generate pharmacologically active CaSR-specific...
The histamine H
Real-time label-free techniques are used to profile G protein-coupled receptor (GPCR) signaling pathways in living cells. However, interpreting the signal responses is challenging, and previously reported methods do not reliably separate from each other. In this study, a continuous angular-scanning surface plasmon resonance (SPR) technique utilized for measuring GPCR profiles. We show how ability, up nine real-time parameters simultaneously, results more information-rich profiles different...
The histamine H3 receptor (H3R) is a neurotransmitter that primarily found in the brain, where it controls release and synthesis of histamine, as well other neurotransmitters (e.g. dopamine, serotonin). Notably, 20 H3R isoforms are differentially expressed human brain consequence alternative gene splicing. hH3R-445, -415, -365 -329 contain prototypical GPCR (7TM) structure, yet exhibit deletions third intracellular loop, structural domain pivotal for G protein-coupling, signaling regulation....
Abstract Context The human calcium-sensing receptor (CaSR) plays a key role in calcium homeostasis, and most identified CASR variants are associated with hypercalcemic hypocalcemic disorders. Objective Here we characterized the pharmacological implications of 5 heterozygous from individuals familial hypocalciuric hypercalcemia 1 (FHH1: Y63C, I81T, Q459R, W818stop) or autosomal dominant hypocalcemia (ADH1: R955stop). Methods Total cell surface expression levels wild-type (WT) variant CaSRs...
The calcium-sensing receptor (CaSR) plays a key role in calcium homeostasis, and small-molecule peptide positive allosteric modulators (PAMs) of CaSR, so-called calcimimetics, are used the treatment hyperparathyroidism hypocalcemic disorders. In this study, four monovalent nanobodies - representing distinct nanobody families with CaSR PAM activity were subjected to elaborate pharmacological profiling at receptor. While Nb5 displayed negligible all assays, Nb4, Nb10 Nb45 potently potentiated Ca