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

ESRRA (P11474) - Overview - Molecular Target Synopsis

Protein


ESRRA, Steroid hormone receptor ERR1
UniProt P11474

Also Known as ERR1_HUMAN, ESRRA, ERR1, ESRL1, NR3B1

Binds to an ERR-alpha response element (ERRE) containing a single consensus half-site, 5'-TNAAGGTCA-3'. Can bind to the medium-chain acyl coenzyme A dehydrogenase (MCAD) response element NRRE-1 and may act as an important regulator of MCAD promoter. Binds to the C1 region of the lactoferrin gene promoter. Requires dimerization and the coactivator, PGC-1A, for full activity. The ERRalpha/PGC1alpha complex is a regulator of energy metabolism. Induces the expression of PERM1 in the skeletal muscle. Binds DNA as a monomer or a homodimer. Interacts (via the AF2 domain) with coactivator PPARGC1A (via the L3 motif); the interaction greatly enhances transcriptional activity of genes involved in energy metabolism. Interacts with PIAS4; the interaction enhances sumoylation. Interacts with MAPK15; promotes re-localization of ESRRA to the cytoplasm through a XPO1-dependent mechanism then inhibits ESRRA transcriptional activity.

3K6P
ESTROGEN RELATED RECEPTOR ALPHA IN COMPLEX WITH AN ETHER BASED LIGAND
RCSB/PDB
Inspect Structure
See all 3D Structures for ESRRA

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: ESRRA is active in the following subcellular-locations: cytoplasm, nucleus.
GO terms: ESRRA is active in the following subcellular-locations: cytoplasm, fibrillar center, intercellular bridge, microtubule cytoskeleton, nucleoplasm, nucleus.



UniProt
GO terms

Gene Copy Number Variation


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

Gene Expression


In NCI60, the highest expressing cell lines are: HCC_2998, MDA_N, KM12

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: DMS 53, CAL 27, SW 1463

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, HeLa-S3, A549

(see details)

3D Structures


For ESRRA there are:
4 structures (6 chains) solved
2 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


ESRRA has been screened with 234 compounds (387 bioactivities), 75 compounds have bioactivities that show binding affinity of <= 500nM (85 bioactivities). (see details)