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

CHRNA3 (P32297) - Overview - Molecular Target Synopsis

Protein


CHRNA3, Neuronal acetylcholine receptor subunit alpha-3
UniProt P32297

Also Known as ACHA3_HUMAN, CHRNA3, NACHRA3

After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane. Neuronal AChR is composed of two different types of subunits: alpha and beta. Alpha-3 subunit can be combined to beta-2 or beta-4 to give rise to functional receptors. Interacts with RIC3; which is required for proper folding and assembly (PubMed:16120769). Interacts with LYPD6 (PubMed:27344019). The heteropentamer alpha-3-beta-2 interacts with alpha-conotoxins ImI and ImII (PubMed:15609996). The heteropentamer alpha-3-beta-2 interacts with alpha-conotoxins ImI, ImII, PnIA, GID and MII (By similarity). The heteropentamer alpha-3-beta-4 interacts with the alpha-conotoxin ImI (PubMed:15609996).

5TVC
CRYSTAL STRUCTURE OF A CHIMERIC ACETYLCHOLINE BINDING PROTEIN FROM APLYSIA CALIFORNICA (AC-ACHBP) CONTAINING LOOP C FROM THE HUMAN ALPHA 3 NICOTINIC ACETYLCHOLINE RECEPTOR IN COMPLEX WITH (E,2S)-N-METHYL-5- (5-PHENOXY-3-PYRIDYL)PENT-4-EN-2-AMINE (TI-5312)
RCSB/PDB
Inspect Structure
See all 3D Structures for CHRNA3

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: CHRNA3 is active in the following subcellular-locations: cell junction, cell membrane, postsynaptic cell membrane, synapse.
GO terms: CHRNA3 is active in the following subcellular-locations: acetylcholine-gated channel complex, cell junction, dendrite, integral component of membrane, integral component of plasma membrane, neuron projection, neuronal cell body, plasma membrane, plasma membrane raft, postsynaptic density, postsynaptic membrane, synapse.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project CHRNA3 has gain in 0 cell-lines, loss in 2 cell-lines and no signal in 1003 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: CCRF_CEM, OVCAR_8, MOLT_4

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: SK-N-DZ, KELLY, SK-N-FI

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: SK-N-SH_RA, SK-N-SH, NHLF

(see details)

3D Structures


For CHRNA3 there are:
3 structures (15 chains) solved
3 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


CHRNA3 has been screened with 1009 compounds (2228 bioactivities), 242 compounds have bioactivities that show binding affinity of <= 500nM (378 bioactivities). (see details)