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

GABRR1 (P24046) - Overview - Molecular Target Synopsis

Protein


GABRR1, Gamma-aminobutyric acid receptor subunit rho-1
UniProt P24046

Also Known as GBRR1_HUMAN, GABRR1

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. Rho-1 GABA receptor could play a role in retinal neurotransmission. Generally pentameric. There are five types of GABA(A) receptor chains: alpha, beta, gamma, delta, and rho. Interacts with SQSTM1.

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: GABRR1 is active in the following subcellular-locations: cell junction, cell membrane, postsynaptic cell membrane, synapse.
GO terms: GABRR1 is active in the following subcellular-locations: cell junction, chloride channel complex, GABA-A receptor complex, GABA-ergic synapse, glutamatergic synapse, integral component of plasma membrane, neuron projection, plasma membrane, postsynaptic membrane, synapse.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project GABRR1 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: MCF7, SK_OV_3, HL_60

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: NCI-H716, Hs 746T, NCI-H209

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


At greater than 50% identity similarity to GABRR1 there are:
4 structures (10 chains) solved
2 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


GABRR1 has been screened with 126 compounds (196 bioactivities), 3 compounds have bioactivities that show binding affinity of <= 500nM (7 bioactivities). (see details)