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

ADRB2 (P07550) - Overview - Molecular Target Synopsis

Protein


ADRB2, Beta-2 adrenergic receptor
UniProt P07550

Also Known as ADRB2_HUMAN, ADRB2, ADRB2R, B2AR

Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. The beta-2-adrenergic receptor binds epinephrine with an approximately 30-fold greater affinity than it does norepinephrine. Binds SLC9A3R1 and GPRASP1. Interacts with ARRB1 and ARRB2. Interacts with SRC, USP20 and USP33. Interacts with VHL; the interaction, which is increased on hydroxylation of ADRB2, ubiquitinates ADRB2 leading to its degradation. Interacts with EGLN3; the interaction hydroxylates ADRB2 facilitating VHL-E3 ligase-mediated ubiquitination. Interacts (via PDZ-binding motif) with SNX27 (via PDZ domain); the interaction is required when endocytosed to prevent degradation in lysosomes and promote recycling to the plasma membrane. Interacts with CNIH4 (PubMed:24405750). Interacts with ARRDC3 (PubMed:20559325, PubMed:25220262).

6N48
STRUCTURE OF BETA2 ADRENERGIC RECEPTOR BOUND TO BI167107, NANOBODY 6B9, AND A POSITIVE ALLOSTERIC MODULATOR
RCSB/PDB
Inspect Structure
See all 3D Structures for ADRB2

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
496ENSG00000169252ENST00000305988ENSP00000305372
413P07550-1

Drugs


ADRB2 is targeted by Approved Drugs Bitolterol, Sotalol, Isoetharine, Penbutolol, Pirbuterol, Oxprenolol, Epinephrine Bitartrate, Levobunolol, Pseudoephedrine, Levosalbutamol, Timolol, Arformoterol, Dipivefrin, Metaproterenol, Mephentermine, Terbutaline, Pindolol, Propranolol, Epinephrine, Metipranolol, Ritodrine, Albuterol, Isoproterenol, Carvedilol, Salmeterol, Carteolol, Esmolol, Nadolol, Dobutamine. (see details)
Bitolterol
Sotalol
Isoetharine
Penbutolol
Pirbuterol
Oxprenolol
Epinephrine Bitartrate
Levobunolol
Pseudoephedrine
Levosalbutamol
Timolol
Arformoterol
Dipivefrin
Metaproterenol
Mephentermine
Terbutaline
Pindolol
Propranolol
Epinephrine
Metipranolol
Ritodrine
Albuterol
Isoproterenol
Carvedilol
Salmeterol
Carteolol
Esmolol
Nadolol
Dobutamine

Sub-cellular localization


UniProt: ADRB2 is active in the following subcellular-locations: cell membrane, early endosome.
GO terms: ADRB2 is active in the following subcellular-locations: apical plasma membrane, clathrin-coated vesicle membrane, early endosome, endosome, endosome membrane, integral component of plasma membrane, lysosome, membrane, nucleus, plasma membrane, receptor complex.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project ADRB2 has gain in 1 cell-lines, loss in 1 cell-lines and no signal in 1003 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: MDA_MB_231, ACHN, OVCAR_8

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: ME-180, BHY, BICR 22

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: NHEK, HMEC, CD14-positive monocyte

(see details)

3D Structures


For ADRB2 there are:
24 structures (26 chains) solved
21 are solved in complex with at least one small molecule ligand
11 are solved with an approved drug

ADRB2 is solved in complex with the approved drug(s):

CLR/CHOLESTEROL (2RH1_A, 3D4S_A, 3NY8_A, 3NY9_A, 3NYA_A, 3PDS_A, 5D5A_A, 5D5B_A, 5D6L_A, 5JQH_A, 5JQH_B, 5X7D_A),
TIM/TIMOLOL (3D4S_A).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


ADRB2 has been screened with 4321 compounds (7651 bioactivities), 1247 compounds have bioactivities that show binding affinity of <= 500nM (1914 bioactivities). (see details)