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

CHRNB2 (P17787) - Overview - Molecular Target Synopsis

Protein


CHRNB2, Neuronal acetylcholine receptor subunit beta-2
UniProt P17787

Also Known as ACHB2_HUMAN, CHRNB2

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 permeable to sodiun ions. Neuronal AChR is composed of two different types of subunits: alpha and beta. Beta-2 subunit can be combined to alpha-2, alpha-3 or alpha-4 to give rise to functional receptors, complexes with beta-2 may be heteropentamers. Alpha-2/4:beta-2 nAChR complexes are proposed to exist in two subtypes: LS (low agonist sensitivity) with a (alpha-2/4)3:(beta-2)2 and HS (high agonist sensitivity) with a (alpha-2/4)2:(beta-2)3 stoichiometry; the subtypes differ in their subunit binding interfaces which are involved in ligand binding (PubMed:27493220, PubMed:22361591). 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 BuIA, MII, PnIA and GID (By similarity). The heteropentamer alpha-3-beta-2 interacts with the alpha-conotoxins ImI and ImII (PubMed:15609996). The heteropentamer alpha-4-beta-2 interacts with the alpha-conotoxins PnIA, GID and MII.

6CNJ
STRUCTURE OF THE 2ALPHA3BETA STIOCHIOMETRY OF THE HUMAN ALPHA4BETA2 NICOTINIC RECEPTOR
RCSB/PDB
Inspect Structure
See all 3D Structures for CHRNB2

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
502ENSG00000160716ENST00000368476ENSP00000357461P17787-1

Drugs


CHRNB2 is targeted by Approved Drug Varenicline. (see details)
Varenicline

Sub-cellular localization


Gene Copy Number Variation


In COSMIC - Cell Lines Project CHRNB2 has gain in 11 cell-lines, loss in 0 cell-lines and no signal in 993 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: HL_60, MCF7, HS578T

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: SK-N-FI, NCI-H810, NCI-H1155

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 CHRNB2 there are:
7 structures (12 chains) solved
3 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


CHRNB2 has been screened with 1423 compounds (3329 bioactivities), 544 compounds have bioactivities that show binding affinity of <= 500nM (873 bioactivities). (see details)