Results 1 to 10 of about 124,416 (341)
Targeting the M1 muscarinic acetylcholine receptor in Alzheimer's disease. [PDF]
Alzheimer’s disease (AD) remains a major cause of morbidity and mortality worldwide, and despite extensive research, only a few drugs are available for management of the disease.
Dwomoh L, Tejeda GS, Tobin AB.
europepmc +2 more sources
Allosteric Modulation of Muscarinic Acetylcholine Receptors [PDF]
An allosteric modulator is a ligand that binds to an allosteric site on the receptor and changes receptor conformation to produce increase (positive cooperativity) or decrease (negative cooperativity) in the binding or action of an orthosteric agonist (e.
Esam E. El-Fakahany, Jan Jakubík
doaj +4 more sources
Muscarinic acetylcholine receptors have been implicated as potential neuroprotective targets for glaucoma. We tested the hypothesis that the lack of a single muscarinic receptor subtype leads to age-dependent neuron reduction in the retinal ganglion cell
Panagiotis Laspas+9 more
doaj +2 more sources
Flavonoids with M1 Muscarinic Acetylcholine Receptor Binding Activity
Muscarinic acetylcholine receptor-active compounds have potential for the treatment of Alzheimer’s disease. In this study, a series of natural and synthetic flavones and flavonols was assayed in vitro for their ability to inhibit radioligand binding at ...
Meyyammai Swaminathan+6 more
doaj +2 more sources
Activation and allosteric modulation of a muscarinic acetylcholine receptor [PDF]
Despite recent advances in crystallography and the availability of G-protein-coupled receptor (GPCR) structures, little is known about the mechanism of their activation process, as only the β2 adrenergic receptor (β2AR) and rhodopsin have been ...
A. Kruse+17 more
semanticscholar +5 more sources
Identification of a family of muscarinic acetylcholine receptor genes. [PDF]
Complementary DNAs for three different muscarinic acetylcholine receptors were isolated from a rat cerebral cortex library, and the cloned receptors were expressed in mammalian cells.
T. Bonner+3 more
semanticscholar +5 more sources
Affinity chromatography of the muscarinic acetylcholine receptor.
A novel compound, 3-(2'-aminobenzhydryloxy)-tropane (ABT), and an ABT-agarose gel were synthesized and used for the purification of solubilized muscarinic receptors. ABT had a high affinity with an apparent dissociation constant (Kd) of 7 nM for the muscarinic receptors solubilized from the porcine brain by digitonin. An ABT-agarose gel was prepared by
Kazuko Haga, Tatsuya Haga
openalex +4 more sources
Trafficking of M2 Muscarinic Acetylcholine Receptors [PDF]
Internalization is an important mechanism regulating the agonist-dependent responses of G-protein-coupled receptors. The internalization of the M(2) muscarinic cholinergic receptors (mAChR) in HEK293 cells has been demonstrated to occur by an unknown mechanism that is independent of arrestins and dynamin.
Aaron G. Roseberry+1 more
openalex +5 more sources
Revisiting the Endocytosis of the M2 Muscarinic Acetylcholine Receptor [PDF]
The agonist-induced endocytosis of the muscarinic acetylcholine receptor M2 is different from that of the other members of the muscarinic receptor family.
Wymke Ockenga, Ritva Tikkanen
doaj +4 more sources
Fine Tuning Muscarinic Acetylcholine Receptor Signaling Through Allostery and Bias
The M1 and M4 muscarinic acetylcholine receptors (mAChRs) are highly pursued drug targets for neurological diseases, in particular for Alzheimer’s disease and schizophrenia.
E. T. van der Westhuizen+7 more
semanticscholar +1 more source