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complex(p(HGNC:CHRNA3), p(HGNC:CHRNB4))

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Components

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Nicotinic acetylcholine receptor signalling: roles in Alzheimer's disease and amyloid neuroprotection. v1.0.0

Nicotinic receptors: allosteric transitions and therapeutic targets in the nervous system v1.0.0

This document contains the curation of the review article Nicotinic receptors: allosteric transitions and therapeutic targets in the nervous system by Taly et al. 2009

Chaperoning α7 neuronal nicotinic acetylcholine receptors v1.0.0

In-Edges 3

a(CHEBI:"amyloid-beta") causesNoChange act(complex(p(HGNC:CHRNA3), p(HGNC:CHRNB4))) View Subject | View Object

Abeta action on nAChRs depends on subunit composition; it has been reported to block alpha7, transiently potentiate alpha4beta2 before blocking, and to have no action on alpha3beta4 (Pym et al., 2005). However, in contrast to its reported transient enhancement when expressed in oocytes, an inhibition of alpha4beta2 has been reported when expressed in human SH-EP1 cells (Wu et al., 2004). PubMed:19293145

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a(MESH:"5-(2-azetidinylmethoxy)-2-chloropyridine") increases act(complex(p(HGNC:CHRNA3), p(HGNC:CHRNB4))) View Subject | View Object

The first nicotinic receptor ligand to undergo Phase ii clinical trials for analgesic activity was the potent Abbott compound ABT-594, a nAChR agonist that preferentially targets α4β2 (ReFS 231–235). The compound allowed for the clinical proof of concept, but could not be developed further because of adverse effects such as emesis and nausea236. As these adverse effects seemed to be attributable to the activation of the ganglionic α3β4 nAChR receptors, Abbott undertook a search for more selective α4β2 agonists, independently and in cooperation with Neurosearch. PubMed:19721446

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Annotations
Text Location
Review

p(HGNC:RIC3) decreases act(complex(p(HGNC:CHRNA3), p(HGNC:CHRNB4))) View Subject | View Object

In contrast, RIC-3 caused a marked inhibition of functional responses with hetero- meric α3β4 and α4β2 AChRs in Xenopus oocytes [109]. PubMed:22040696

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Out-Edges 2

complex(p(HGNC:CHRNA3), p(HGNC:CHRNB4)) hasComponent p(HGNC:CHRNA3) View Subject | View Object

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complex(p(HGNC:CHRNA3), p(HGNC:CHRNB4)) hasComponent p(HGNC:CHRNB4) View Subject | View Object

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About

BEL Commons is developed and maintained in an academic capacity by Charles Tapley Hoyt and Daniel Domingo-Fernández at the Fraunhofer SCAI Department of Bioinformatics with support from the IMI project, AETIONOMY. It is built on top of PyBEL, an open source project. Please feel free to contact us here to give us feedback or report any issues. Also, see our Publishing Notes and Data Protection information.

If you find BEL Commons useful in your work, please consider citing: Hoyt, C. T., Domingo-Fernández, D., & Hofmann-Apitius, M. (2018). BEL Commons: an environment for exploration and analysis of networks encoded in Biological Expression Language. Database, 2018(3), 1–11.