Publications by authors named "C C Felder"
Mitochondrial diseases are rare genetic disorders often accompanied by severe sleep disorders. We present the case of a 12-year-old boy diagnosed with a severe primary mitochondrial disease, exhibiting ataxia, spasticity, progressive external ophthalmoplegia, cardiomyopathy and severely disrupted sleep, but no cognitive impairment. Interestingly, his parents reported improved sleep during night train rides.
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- - The M muscarinic acetylcholine receptor (M mAChR) is a key target for drug development due to its role in managing psychosis, cognition, and addiction, with xanomeline showing promise in improving symptoms of schizophrenia in clinical trials.
- - Recent research revealed the cryo-EM structure of xanomeline bound to the M mAChR, showing that two xanomeline molecules can simultaneously bind to different sites on the receptor.
- - These findings suggest that xanomeline functions as both an orthosteric and allosteric ligand, enhancing our understanding of its complex pharmacology and how ligands can interact with GPCRs for therapeutic purposes.
Article Synopsis
- The selectivity of drugs for their target receptors is vital for effective treatment, but distinguishing between similar receptors poses a challenge.
- The discovery of ligands that preferentially activate target receptors over closely related ones, despite similar binding affinities, points to a phenomenon called 'efficacy-driven selectivity.'
- Using atomic-level simulations, researchers identified how the drug xanomeline interacts differently with inactive and active states of muscarinic acetylcholine receptors, paving the way for designing drugs with enhanced selectivity for important receptors.
Muscarinic acetylcholine receptors for psychotic disorders: bench-side to clinic.
Trends Pharmacol Sci
December 2022
Article Synopsis
- Interest in muscarinic acetylcholine receptor (mAChR) activators for schizophrenia surged in the 1990s due to xanomeline, an agonist initially developed for Alzheimer’s, showing unexpected antipsychotic effects.
- During that time, there were challenges in managing tolerability issues linked to the activation of peripheral mAChRs.
- Recent advancements in targeted ligands and combination treatments have improved the feasibility of mAChR activators as promising therapies for schizophrenia, with ongoing clinical development efforts.