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

ABCB1 (P08183) - Overview - Molecular Target Synopsis

Protein


ABCB1, Multidrug resistance protein 1
Enzyme Classification 7.6.2.2
UniProt P08183

Also Known as MDR1_HUMAN, ABCB1, MDR1, PGY1

Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells. Interacts with PSMB5. Finds in a complex with ABCB1, TFPI2 and PPP2R3C; leading to the dephosphorylation of ABCB1.

6QEX
NANODISC RECONSTITUTED HUMAN ABCB1 IN COMPLEX WITH UIC2 FAB AND TAXOL
RCSB/PDB
Inspect Structure
See all 3D Structures for ABCB1

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: ABCB1 is active in the following subcellular-locations: cell membrane.
GO terms: ABCB1 is active in the following subcellular-locations: apical plasma membrane, cell surface, extracellular exosome, integral component of membrane, membrane, plasma membrane.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project ABCB1 has gain in 10 cell-lines, loss in 1 cell-lines and no signal in 994 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: NCI_ADR_RES, HCT_15, CAKI_1

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: CW-2, LS1034, DMS 53

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 ABCB1 there are:
4 structures (4 chains) solved
4 are solved in complex with at least one small molecule ligand
1 are solved with an approved drug

ABCB1 is solved in complex with the approved drug(s):

TA1/PACLITAXEL (6QEX_A),
CLR/CHOLESTEROL (6QEX_A).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


ABCB1 has been screened with 3745 compounds (8764 bioactivities), 426 compounds have bioactivities that show binding affinity of <= 500nM (583 bioactivities). (see details)