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

ABCG2 (Q9UNQ0) - Overview - Molecular Target Synopsis

Protein


ABCG2, ATP-binding cassette sub-family G member 2
UniProt Q9UNQ0

Also Known as ABCG2_HUMAN, ABCG2, ABCP, BCRP, BCRP1, MXR

High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both from mitochondria to cytosol and from cytosol to extracellular space, and cellular export of hemin, and heme. Xenobiotic transporter that may play an important role in the exclusion of xenobiotics from the brain. Appears to play a major role in the multidrug resistance phenotype of several cancer cell lines. Implicated in the efflux of numerous drugs and xenobiotics: mitoxantrone, the photosensitizer pheophorbide, camptothecin, methotrexate, azidothymidine (AZT), and the anthracyclines daunorubicin and doxorubicin. Monomer under reducing conditions, the minimal functional units is a homodimer; disulfide-linked, but the major oligomeric form in plasma membranes is a homotetramer with possibility of higher order oligomerization up to homododecamers.

6HZM
CRYO-EM STRUCTURE OF THE ABCG2 E211Q MUTANT BOUND TO ATP AND MAGNESIUM (ALTERNATIVE PLACEMENT OF MAGNESIUM INTO THE CRYO-EM DENSITY)
RCSB/PDB
Inspect Structure
See all 3D Structures for ABCG2

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: ABCG2 is active in the following subcellular-locations: cell membrane, mitochondrion membrane.
GO terms: ABCG2 is active in the following subcellular-locations: integral component of membrane, mitochondrial membrane, nucleus, plasma membrane.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project ABCG2 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: RPMI_8226, HCC_2998, A549

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: OUMS-23, RMUG-S, HCC-15

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: A549, SK-N-SH, HSMM

(see details)

3D Structures


For ABCG2 there are:
9 structures (18 chains) solved
9 are solved in complex with at least one small molecule ligand
1 are solved with an approved drug

ABCG2 is solved in complex with the approved drug(s):

CLR/CHOLESTEROL (6HIJ_A, 6HIJ_B).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


ABCG2 has been screened with 862 compounds (1873 bioactivities), 108 compounds have bioactivities that show binding affinity of <= 500nM (169 bioactivities). (see details)