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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

In-Edges 7

a(MESH:Conotoxins) association complex(p(HGNC:CHRNA10), p(HGNC:CHRNA9)) View Subject | View Object

Regarding the ascending afferent excitatory pain pathway, in which nicotinic antagonists are anticipated to have analgesic effects, a newly described subtype of nAChR, α9α10, seems to be expressed on dorsal root ganglia (in addition to the inner ear) and constitutes an in vitro target for new α-conotoxins, such as vc1.1, RgiA, or it14a237–241. PubMed:19721446

a(MESH:Conotoxins) decreases act(complex(p(HGNC:CHRNA10), p(HGNC:CHRNA9))) View Subject | View Object

In vivo, these α-conotoxins display potent alleviation of allopathic pain239,242,243 (and additionally reveal an endogeneous ACh activation of lymphocytes through α9α10 nAChRs, which are inhibited by these α-conotoxins). PubMed:19721446

a(MESH:"Ganglia, Spinal") increases complex(p(HGNC:CHRNA10), p(HGNC:CHRNA9)) View Subject | View Object

α9 or a9 and α10 subunits are expressed in most immune cells, dorsal root ganglion cells, human keratinocytes and colon and breast cancer cells. PubMed:28901280

a(MESH:Acetylcholine) increases act(complex(p(HGNC:CHRNA10), p(HGNC:CHRNA9))) View Subject | View Object

α9 and α9-α10 nAChRs have a number of interesting characteristics: they are acti- vated by ACh but not by the classical agonist nicotine. Cho- line is also a potent selective agonist of the α9 subtype PubMed:28901280

a(MESH:Keratinocytes) increases complex(p(HGNC:CHRNA10), p(HGNC:CHRNA9)) View Subject | View Object

α9 or a9 and α10 subunits are expressed in most immune cells, dorsal root ganglion cells, human keratinocytes and colon and breast cancer cells. PubMed:28901280

a(MESH:Nicotine) causesNoChange act(complex(p(HGNC:CHRNA10), p(HGNC:CHRNA9))) View Subject | View Object

α9 and α9-α10 nAChRs have a number of interesting characteristics: they are acti- vated by ACh but not by the classical agonist nicotine. Cho- line is also a potent selective agonist of the α9 subtype PubMed:28901280

a(MESH:Phosphorylcholine) causesNoChange complex(p(HGNC:CHRNA10), p(HGNC:CHRNA9)) View Subject | View Object

whereas phosphocholine (PC) does not evoke ion current responses in Xenopus oocytes expressing functional ho- momeric α9 or heteromeric α9-α10 nAChRs [121]. How- ever, preincubation with PC attenuates choline-induced ion current changes, thus suggesting that PC is a silent agonist of these two subtypes PubMed:28901280

Out-Edges 5

complex(p(HGNC:CHRNA10), p(HGNC:CHRNA9)) association a(MESH:Conotoxins) View Subject | View Object

Regarding the ascending afferent excitatory pain pathway, in which nicotinic antagonists are anticipated to have analgesic effects, a newly described subtype of nAChR, α9α10, seems to be expressed on dorsal root ganglia (in addition to the inner ear) and constitutes an in vitro target for new α-conotoxins, such as vc1.1, RgiA, or it14a237–241. PubMed:19721446

complex(p(HGNC:CHRNA10), p(HGNC:CHRNA9)) increases act(a(MESH:Lymphocytes)) View Subject | View Object

In vivo, these α-conotoxins display potent alleviation of allopathic pain239,242,243 (and additionally reveal an endogeneous ACh activation of lymphocytes through α9α10 nAChRs, which are inhibited by these α-conotoxins). PubMed:19721446

complex(p(HGNC:CHRNA10), p(HGNC:CHRNA9)) increases p(MESH:"Receptors, Nicotinic") View Subject | View Object

Unlike the α9 subunit, the α10 subunit is only functional when it is co-expressed with an α9 subunit. In Xenopus oocytes, the co-injection of α9 and α10 subunits increases functional nAChR expression at least 100 times more than the injection of α9 alone. PubMed:28901280

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