Publications by authors named "M Wasinska-Kalwa"
The diversity of physiological roles of the endocannabinoid system has turned it into an attractive yet elusive therapeutic target. However, chemical probes with various functionalities could pave the way for a better understanding of the endocannabinoid system at the cellular level. Notably, inverse agonists of CBR - a key receptor of the endocannabinoid system - lagged behind despite the evidence regarding the therapeutic potential of its antagonism.
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- The cannabinoid receptor type 1 (CBR) plays a key role in various bodily functions, including appetite, pain, memory, and body temperature regulation, but our understanding of its cellular signaling and dynamics is limited.
- Researchers developed new fluorescent probes for CBR by using a modular design approach that centers around a diethyl glycine-based building block, making synthesis easier and more efficient.
- Validation of these probes through various assays supports their potential use in real-time imaging studies to explore CBR's localization, movement, and effects in different diseases.
Tryptophan hydroxylases catalyze the first and rate-limiting step in the biosynthesis of serotonin, a well-known neurotransmitter that plays an important role in multiple physiological functions. A reduction of serotonin levels, especially in the brain, can cause dysregulation leading to depression or insomnia. In contrast, overproduction of peripheral serotonin is associated with symptoms like carcinoid syndrome and pulmonary arterial hypertension.
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- - The study highlights the unclear role of CBR tissue expression and signaling in various diseases, prompting new research efforts.
- - Researchers created a powerful fluorescent CBR agonist probe that combines a validated ligand with a silicon-rhodamine fluorophore for increased cell permeability.
- - This probe uniquely maintains affinity for both mouse and human CBR, facilitating CBR detection in live cells and zebrafish, which could enhance the development of CBR-related drugs.
Due to a unique mechanism that limits the possibility of hypoglycemia, the free fatty acid receptor (FFA1) is an attractive target for the treatment of type 2 diabetes. So far, however, none of the promising agonists have been able to enter the market. The most advanced clinical candidate, TAK-875, was withdrawn from phase III clinical trials due to liver safety issues.
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