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

GABRP (O00591) - Overview - Molecular Target Synopsis

Protein


GABRP, Gamma-aminobutyric acid receptor subunit pi
UniProt O00591

Also Known as GBRP_HUMAN, GABRP

GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel. In the uterus, the function of the receptor appears to be related to tissue contractility. The binding of this pI subunit with other GABA(A) receptor subunits alters the sensitivity of recombinant receptors to modulatory agents such as pregnanolone. Generally pentameric. There are five types of GABA(A) receptor chains: alpha, beta, gamma, delta, and epsilon. A sixth class of subunit: Rho form homomeric GABA receptors that do not appear to coexist with GABA(A) receptor subunits but with GABA(C) receptor subunits. Subunit Pi can also bind this complex.

Isoforms / Transcripts (Protein Coding)


Drugs


GABRP is targeted by Approved Drugs Ethchlorvynol, Clobazam, Eszopiclone. (see details)
Ethchlorvynol
Clobazam
Eszopiclone

Sub-cellular localization


UniProt: GABRP is active in the following subcellular-locations: cell junction, cell membrane, postsynaptic cell membrane, synapse.
GO terms: GABRP is active in the following subcellular-locations: cell junction, chloride channel complex, GABA-A receptor complex, integral component of plasma membrane, neuron projection, postsynaptic membrane, synapse.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project GABRP has gain in 2 cell-lines, loss in 2 cell-lines and no signal in 1000 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: NCI_H322M, HT29, RXF_393

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: Calu-3, H322T, HCC1143

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: MCF-7, SK-N-SH, NHLF

(see details)

3D Structures


At greater than 50% identity similarity to GABRP there are:
10 structures (33 chains) solved
8 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


GABRP has been screened with 642 compounds (850 bioactivities), 267 compounds have bioactivities that show binding affinity of <= 500nM (324 bioactivities). (see details)