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

ABCC8 (Q09428) - Overview - Molecular Target Synopsis

Protein


ABCC8, ATP-binding cassette sub-family C member 8
UniProt Q09428

Also Known as ABCC8_HUMAN, ABCC8, HRINS, SUR, SUR1

Subunit of the beta-cell ATP-sensitive potassium channel (KATP). Regulator of ATP-sensitive K(+) channels and insulin release. Interacts with KCNJ11.

6C3O
CRYO-EM STRUCTURE OF HUMAN KATP BOUND TO ATP AND ADP IN QUATREFOIL FORM
RCSB/PDB
Inspect Structure
See all 3D Structures for ABCC8

Isoforms / Transcripts (Protein Coding)


Drugs


ABCC8 is targeted by Approved Drugs Nateglinide, Procainamide, Glipizide, Acetohexamide, Chlorpropamide, Tolbutamide, Tolazamide, Glimepiride, Repaglinide , Glyburide. (see details)
Nateglinide
Procainamide
Glipizide
Acetohexamide
Chlorpropamide
Tolbutamide
Tolazamide
Glimepiride
Repaglinide
Glyburide

Sub-cellular localization


UniProt: ABCC8 is active in the following subcellular-locations: cell membrane.
GO terms: ABCC8 is active in the following subcellular-locations: inward rectifying potassium channel, membrane, mitochondrion, plasma membrane, sarcolemma, synaptic vesicle membrane.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project ABCC8 has gain in 0 cell-lines, loss in 3 cell-lines and no signal in 1002 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: SK_OV_3, TK_10, MCF7

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: SK-N-DZ, MDA-MB-134-VI, NCI-H1092

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 ABCC8 there are:
2 structures (8 chains) solved
2 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


ABCC8 has been screened with 386 compounds (861 bioactivities), 117 compounds have bioactivities that show binding affinity of <= 500nM (174 bioactivities). (see details)