Cellular Physiology and Biochemistry, 2014 Background/ Aims: Impaired pancreatic beta cell function and insulin secretion/action are a link between obesity and type 2 diabetes, which are worldwide public health burdens.
Rosiane A. Miranda +10 more
doaj +1 more source
Molecular determinants of allosteric modulation at the M1 muscarinic acetylcholine receptor [PDF]
, 2014 Background: BQCA is a selective allosteric modulator of the M1 mAChR. Results: Residues that govern BQCA activity were identified using mutagenesis and molecular modelling.
Abdul-Ridha +57 more
core +2 more sources
Cholinergic regulation of mood: from basic and clinical studies to emerging therapeutics. [PDF]
, 2019 Mood disorders are highly prevalent and are the leading cause of disability worldwide. The neurobiological mechanisms underlying depression remain poorly understood, although theories regarding dysfunction within various neurotransmitter systems have ...
Dulawa, Stephanie C, Janowsky, David S
core
Interactions between the neuromodulatory systems and the amygdala: exploratory survey using the Allen Mouse Brain Atlas. [PDF]
, 2013 Neuromodulatory systems originate in nuclei localized in the subcortical region of the brain and control fundamental behaviors by interacting with many areas of the central nervous system.
Krichmar, Jeffrey L, Zaldivar, Andrew
core +1 more source
PLoS ONE, 2019 In early-onset generalized torsion dystonia, caused by a GAG deletion in TOR1A (DYT1), enhanced striatal cholinergic activity has been suggested to be critically involved. Previous studies have shown increased acetylcholine levels in the striatum of DYT1
Franziska Richter +3 more
doaj +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]
, 2018 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
G protein‐coupled receptor‐mediated autophagy in health and disease
British Journal of Pharmacology, Volume 182, Issue 14, Page 3151-3162, July 2025.G protein‐coupled receptors (GPCRs) constitute the largest and most diverse superfamily of mammalian transmembrane proteins. These receptors are involved in a wide range of physiological functions and are targets for more than a third of available drugs in the market. Autophagy is a cellular process involved in degrading damaged proteins and organelles
Devrim Öz‐Arslan +2 more
wiley +1 more source
Rab11a and Myosin Vb Regulate Recycling of the M4Muscarinic Acetylcholine Receptor [PDF]
The Journal of Neuroscience, 2002 Agonist-induced internalization followed by subsequent return to the cell surface regulates G-protein-coupled receptor (GPCR) activity. Because the cellular responsiveness to ligand depends on the balance between receptor degradation and recycling, it is crucial to identify the molecules involved in GPCR recovery to the cell surface.
James J. Lah +4 more
openaire +3 more sources
Frontiers in Pharmacology, 2016 Background/Aim: Muscarinic acetylcholine receptors exist in five subtypes (M1~M5), and they are widely expressed in various tissues to mediate diverse autonomic functions, including gastric secretion.
Koji Takeuchi +4 more
doaj +1 more source
Mechanistic insights into allosteric structure-function relationships at the M1 muscarinic acetylcholine receptor [PDF]
, 2014 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