Molecular Target Synopsis
Overview
Domains and Structures
Drugs and Clinical Candidates
Druggability
Chemistry
Ligand Efficiency Plot
Pathways
Family Cladogram
Interaction Network
Gene Expression
Gene Copy Number Variation
RNAi
Mutations
Germline Genetics

CHRNA10 (Q9GZZ6) - Overview - Molecular Target Synopsis

Protein


CHRNA10, Neuronal acetylcholine receptor subunit alpha-10
UniProt Q9GZZ6

Also Known as ACH10_HUMAN, CHRNA10, NACHRA10

Ionotropic receptor with a probable role in the modulation of auditory stimuli. Agonist binding may induce an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane. The channel is permeable to a range of divalent cations including calcium, the influx of which may activate a potassium current which hyperpolarizes the cell membrane. In the ear, this may lead to a reduction in basilar membrane motion, altering the activity of auditory nerve fibers and reducing the range of dynamic hearing. This may protect against acoustic trauma. Forms heterooligomeric channels in conjunction with CHRNA9. The native outer hair cell receptor may be composed of CHRNA9-CHRNA10 heterooligomers. Interacts with the conotoxin GeXXA (PubMed:26395518). Interacts with the alpha-conotoxin RgIA.

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: CHRNA10 is active in the following subcellular-locations: cell junction, cell membrane, postsynaptic cell membrane, synapse.
GO terms: CHRNA10 is active in the following subcellular-locations: axon, cell junction, cholinergic synapse, integral component of plasma membrane, integral component of postsynaptic specialization membrane, membrane, neuron projection, perikaryon, synapse.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project CHRNA10 has gain in 1 cell-lines, loss in 2 cell-lines and no signal in 1002 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: SNB_19, LOXIMVI, HCT_15

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: Hs 746T, NCI-H209, GTL-16

In Array Express (RNA-seq of long poly adenylated RNA and long non poly adenylated RNA from ENCODE cell lines), the highest expressing cell lines are: NHLF, HSMM, HMEC

(see details)

3D Structures


At greater than 50% identity similarity to CHRNA10 there are:
3 structures (5 chains) solved
3 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


CHRNA10 has been screened with 45 compounds (53 bioactivities), 8 compounds have bioactivities that show binding affinity of <= 500nM (8 bioactivities). (see details)