Activation of the muscarinic M1 receptor is a promising approach to improve cognitive deficits associated with cholinergic dysfunction in Alzheimer's disease, dementia with Lewy bodies, and schizophrenia.
Emi Kurimoto +3 more
doaj +1 more source
Autoradiography helps to determine the distribution and density of muscarinic receptor (MR) binding sites in the brain. However, it relies on the selectivity of radioligands toward their target.
Paulina Valuskova +4 more
doaj +1 more source
New strategic insights into managing fungal biofilms [PDF]
Fungal infections have dramatically increased in the last decades in parallel with an increase of populations with impaired immunity, resulting from medical conditions such as cancer, transplantation or other chronic diseases.
Borghi, Elisa +6 more
core +4 more sources
Virtual Affinity Fingerprints for Target Fishing: A New Application of Drug Profile Matching [PDF]
We recently introduced Drug Profile Matching (DPM), a novel virtual affinity fingerprinting bioactivity prediction method. DPM is based on the docking profiles of ca.
Czobor, P. +6 more
core +1 more source
Induction of Anti-Hebbian LTP in CA1 Stratum Oriens Interneurons: Interactions between Group I Metabotropic Glutamate Receptors and M1 Muscarinic Receptors [PDF]
An anti-Hebbian form of LTP is observed at excitatory synapses made with some hippocampal interneurons. LTP induction is facilitated when postsynaptic interneurons are hyperpolarized, presumably because Ca(2+) entry through Ca(2+)-permeable glutamate ...
Kullmann, DM +3 more
core +1 more source
Assessment of the molecular mechanisms of action of novel 4-phenylpyridine-2-one and 6-phenylpyrimidin-4-one allosteric modulators at the M1 muscarinic acetylcholine receptors [PDF]
Positive allosteric modulators (PAMs) that target the M1 muscarinic acetylcholine (ACh) receptor (M1 mAChR) are potential treatments for cognitive deficits in conditions such as Alzheimer's disease and schizophrenia.
Andrew B. Tobin +15 more
core +2 more sources
Mechanistic insights into allosteric structure-function relationships at the M1 muscarinic acetylcholine receptor [PDF]
Background: Selective and potent positive allosteric modulators (PAMs) of the M1 mAChR have been recently described. Results: Use of structural analogues and mutagenic mapping identified the mechanistic basis for increased PAM activity.
Abdul-Ridha +42 more
core +2 more sources
Spatial intensity distribution analysis: studies of G Protein-coupled receptor oligomerization [PDF]
Spatial intensity distribution analysis (SpIDA) is a recently developed approach for determining quaternary structure information on fluorophore-labelled proteins of interest in situ. It can be applied to live or fixed cells and native tissue.
Marsango, Sara +3 more
core +1 more source
The microtubule associated protein tau is mainly found in the cell’s cytosol but recently it was also shown in the extracellular space. In neurodegenerative diseases, like Alzheimer’s disease (AD), pathological tau spreads from neuron to neuron enhancing
Viktoriya Morozova +10 more
doaj +1 more source
Cholinergic receptor alterations in the cerebral cortex of spinal cord injured rat
Many areas of the cerebral cortex process sensory information or coordinate motor output necessary for control of movement. Disturbances in cortical cholinergic system can affect locomotor coordination.
R. Chinthu, T.R. Anju, C.S. Paulose
doaj +1 more source

