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

CHRNA2 (Q15822) - Overview - Molecular Target Synopsis

Protein


CHRNA2, Neuronal acetylcholine receptor subunit alpha-2
UniProt Q15822

Also Known as ACHA2_HUMAN, CHRNA2

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 seems to be composed of two different types of subunits: alpha and non-alpha (beta). Alpha-2 subunit can be combined to beta-2 or beta-4 to give rise to functional receptors. The alpha-2:beta-2 nAChR complex is proposed to be a heteropentamer with two subtypes: LS (low agonist sensitivity) with a (alpha-2)3:(beta-2)2 and HS (high agonist sensitivity) with a (alpha-2)2:(beta-2)3 stoichiometry; the subtypes differ in their subunit binding interfaces which are involved in ligand binding.

5FJV
CRYSTAL STRUCTURE OF THE EXTRACELLULAR DOMAIN OF ALPHA2 NICOTINIC ACETYLCHOLINE RECEPTOR IN PENTAMERIC ASSEMBLY
RCSB/PDB
Inspect Structure
See all 3D Structures for CHRNA2

Isoforms / Transcripts (Protein Coding)


Drugs


CHRNA2 is targeted by Approved Drugs Metocurine, Pipecuronium, Suxamethonium, Ethopropazine, Rapacuronium, Cycrimine, Nicotine, Vecuronium, Decamethonium, Trihexyphenidyl, Tubocurarine, Mecamylamine, Oxyphenonium, Rocuronium, Cisatracurium, Atracurium, Carbachol, Pancuronium, Pentolinium, Benztropine, Mivacurium, Trimethaphan. (see details)
Metocurine
Pipecuronium
Suxamethonium
Ethopropazine
Rapacuronium
Cycrimine
Nicotine
Vecuronium
Decamethonium
Trihexyphenidyl
Tubocurarine
Mecamylamine
Oxyphenonium
Rocuronium
Cisatracurium
Atracurium
Carbachol
Pancuronium
Pentolinium
Benztropine
Mivacurium
Trimethaphan

Sub-cellular localization


UniProt: CHRNA2 is active in the following subcellular-locations: cell junction, cell membrane, postsynaptic cell membrane, synapse.
GO terms: CHRNA2 is active in the following subcellular-locations: acetylcholine-gated channel complex, cell junction, integral component of membrane, integral component of plasma membrane, neuron projection, plasma membrane, postsynaptic membrane, synapse.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project CHRNA2 has gain in 0 cell-lines, loss in 10 cell-lines and no signal in 995 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: HL_60, MCF7, HOP_92

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

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, NHLF, HSMM

(see details)

3D Structures


For CHRNA2 there are:
1 structures (5 chains) solved
1 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


CHRNA2 has been screened with 39 compounds (77 bioactivities), 6 compounds have bioactivities that show binding affinity of <= 500nM (11 bioactivities). (see details)