Results 11 to 20 of about 28,292 (196)
Affinity chromatography of the muscarinic acetylcholine receptor.
Journal of Biological Chemistry, 1983 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
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Evolution of the Muscarinic Acetylcholine Receptors in Vertebrates [PDF]
eneuro, 2018 The family of muscarinic acetylcholine receptors (mAChRs) consists of five members in mammals, encoded by the CHRM1-5 genes. The mAChRs are G-protein-coupled receptors, which can be divided into the following two subfamilies: M2 and M4 receptors coupling to Gi/o; and M1, M3, and M5 receptors coupling to Gq/11.
Julia E. Pedersen +2 more
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Allosteric Modulation of Muscarinic Acetylcholine Receptors [PDF]
Pharmaceuticals, 2010 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.g., acetylcholine).
Esam E. El-Fakahany, Jan Jakubík
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Allosteric Modulation of Muscarinic Acetylcholine Receptors [PDF]
Current Neuropharmacology, 2007 Muscarinic acetylcholine receptors (mAChRs) are prototypical Family A G protein coupled-receptors. The five mAChR subtypes are widespread throughout the periphery and the central nervous system and, accordingly, are widely involved in a variety of both physiological and pathophysiological processes.
Arthur Christopoulos +2 more
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Trafficking of M2 Muscarinic Acetylcholine Receptors [PDF]
Journal of Biological Chemistry, 1999 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
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Muscarinic Acetylcholine Receptors in the Retina—Therapeutic Implications [PDF]
International Journal of Molecular Sciences, 2021 Muscarinic acetylcholine receptors (mAChRs) belong to the superfamily of G-protein-coupled receptors (GPCRs). The family of mAChRs is composed of five subtypes, M1, M2, M3, M4 and M5, which have distinct expression patterns and functions. In the eye and its adnexa, mAChRs are widely expressed and exert multiple functions, such as modulation of tear ...
Yue Ruan +3 more
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FEBS Open Bio, EarlyView.Representation of the suggested mode of action of lactoferrin (Lf) in nonsmall cell lung cancer (NSCLC) A549 cells. Lf induces activation of caspase‐3 by activating p53 and AChE leading to decreased ACh concentrations. In turn, ACh signaling leads to activation of VEGF and AKT and blocking of caspase‐3.
Stuti Goel +9 more
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Advanced Healthcare Materials, EarlyView.Despite significant efforts in developing novel biomaterials to regenerate tissue, only a few of them have successfully reached clinical use. It has become clear that the next generation of biomaterials must be multifunctional. Smart biomaterials can respond to environmental or external stimuli, interact in a spatial‐temporal manner, and trigger ...
Sonya Ghanavati +12 more
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From Design to Outcome: The Role of Bi‐ and Multifunctional Ligands in Modern Therapeutics
Advanced Therapeutics, EarlyView.This review highlights the innovative use of bi‐ and multifunctional ligands for precision therapeutics. From strategic linker design to bioorthogonal conjugation and nanoscaffold integration, these approaches enable precise targeting, high‐resolution receptor mapping, and enhanced drug delivery.
Célia Bouacha +2 more
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Neuro‐Cancer Interactions Shape Glioma Intratumoral Heterogeneity
Advanced Science, EarlyView.This review proposes a conceptual framework for understanding glioma intratumoral heterogeneity shaped by neuro‐cancer interactions: functional patterns and transcriptional states. Functional patterns manifest as three major neural‐like adaptations with spatial and potentially hierarchical relationships, including neurogliomal synapses, glioma networks,
Tong Wu +8 more
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