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Literature DB >> 16595339

Constitutive activity of muscarinic acetylcholine receptors.

Abstract

We review the literature describing constitutive activity of the five muscarinic acetylcholine receptors in native and recombinant systems and discuss the effect of constitutive activity on muscarinic pharmacology in the context of modern models of receptor activation. We include a summary of mutations found to cause constitutive activity and discuss the implications of these data for the structure, function, and activation mechanism of muscarinic receptors. Finally, we discuss the possible physiological significance of constitutive activity of muscarinic receptors, incorporating information provided by targeted deletion of each of the muscarinic subtypes.

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Year: 2006 PMID： 16595339 DOI： 10.1080/10799890600567349

Source DB: PubMed Journal: J Recept Signal Transduct Res ISSN： 1079-9893 Impact factor: 2.092

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Cited

18 in total

1. Allosteric effects of sodium ion binding on activation of the m3 muscarinic g-protein-coupled receptor.

Authors: Yinglong Miao; Alisha D Caliman; J Andrew McCammon
Journal: Biophys J Date: 2015-04-07 Impact factor: 4.033

2. Mapping of allosteric druggable sites in activation-associated conformers of the M2 muscarinic receptor.

Authors: Yinglong Miao; Sara E Nichols; J Andrew McCammon
Journal: Chem Biol Drug Des Date: 2013-10-30 Impact factor: 2.817

3. Cardiac resynchronization therapy restores sympathovagal balance in the failing heart by differential remodeling of cholinergic signaling.

Authors: Deeptankar DeMazumder; David A Kass; Brian O'Rourke; Gordon F Tomaselli
Journal: Circ Res Date: 2015-03-02 Impact factor: 17.367

4. Two distinct conformations of helix 6 observed in antagonist-bound structures of a beta1-adrenergic receptor.

Authors: Rouslan Moukhametzianov; Tony Warne; Patricia C Edwards; Maria J Serrano-Vega; Andrew G W Leslie; Christopher G Tate; Gebhard F X Schertler
Journal: Proc Natl Acad Sci U S A Date: 2011-05-03 Impact factor: 11.205

5. A constitutively active G protein-coupled acetylcholine receptor regulates motility of larval Schistosoma mansoni.

Authors: Kevin MacDonald; Michael J Kimber; Tim A Day; Paula Ribeiro
Journal: Mol Biochem Parasitol Date: 2015-09-10 Impact factor: 1.759

Review 6. Cholinergic and glutamatergic alterations beginning at the early stages of Alzheimer disease: participation of the phospholipase A2 enzyme.

Authors: Evelin L Schaeffer; Wagner F Gattaz
Journal: Psychopharmacology (Berl) Date: 2008-02-19 Impact factor: 4.530

Constitutive activity of muscarinic acetylcholine receptors.

1. Allosteric effects of sodium ion binding on activation of the m3 muscarinic g-protein-coupled receptor.

2. Mapping of allosteric druggable sites in activation-associated conformers of the M2 muscarinic receptor.

3. Cardiac resynchronization therapy restores sympathovagal balance in the failing heart by differential remodeling of cholinergic signaling.

4. Two distinct conformations of helix 6 observed in antagonist-bound structures of a beta1-adrenergic receptor.

5. A constitutively active G protein-coupled acetylcholine receptor regulates motility of larval Schistosoma mansoni.

Review 6. Cholinergic and glutamatergic alterations beginning at the early stages of Alzheimer disease: participation of the phospholipase A2 enzyme.

7. Activation and dynamic network of the M2 muscarinic receptor.

8. Mechanism of the G-protein mimetic nanobody binding to a muscarinic G-protein-coupled receptor.

9. Divergence of allosteric effects of rapacuronium on binding and function of muscarinic receptors.

Review 10. Accelerated molecular dynamics simulations of ligand binding to a muscarinic G-protein-coupled receptor.