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

THRA (P10827) - Overview - Molecular Target Synopsis

Protein


THRA, Thyroid hormone receptor alpha
UniProt P10827

Also Known as THA_HUMAN, THRA, EAR7, ERBA1, NR1A1, THRA1, THRA2

Isoform Alpha-1: Nuclear hormone receptor that can act as a repressor or activator of transcription. High affinity receptor for thyroid hormones, including triiodothyronine and thyroxine., Isoform Alpha-2: Does not bind thyroid hormone and functions as a weak dominant negative inhibitor of thyroid hormone action. Binds DNA as a dimer; homodimer and heterodimer with RXRB. Interacts with NCOA3 and NCOA6 coactivators, leading to a strong increase of transcription of target genes. Probably interacts with SFPQ. Interacts with C1D. Interacts with AKAP13. Interacts with TP53INP2. Interacts with PER2.

4LNW
CRYSTAL STRUCTURE OF TR-ALPHA BOUND TO T3 IN A SECOND SITE
RCSB/PDB
Inspect Structure
See all 3D Structures for THRA

Isoforms / Transcripts (Protein Coding)


Drugs


THRA is targeted by Approved Drugs Liothyronine, Dextrothyroxine, Levothyroxine. (see details)
Liothyronine
Dextrothyroxine
Levothyroxine

Sub-cellular localization


UniProt: THRA is active in the following subcellular-locations: nucleus.
GO terms: THRA is active in the following subcellular-locations: cytosol, nucleoplasm, nucleus, RNA polymerase II transcription factor complex.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project THRA has gain in 16 cell-lines, loss in 3 cell-lines and no signal in 985 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: HCC_2998, HCT_116, RPMI_8226

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: RPMI 2650, HM7, UACC-893

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: NHLF, BJ, IMR-90

(see details)

3D Structures


For THRA there are:
8 structures (8 chains) solved
8 are solved in complex with at least one small molecule ligand
4 are solved with an approved drug

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

T3/LIOTHYRONINE (2H77_A, 2H79_A, 4LNW_A, 4LNX_A),
T44/LEVOTHYROXINE (4LNX_A).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


THRA has been screened with 630 compounds (1102 bioactivities), 214 compounds have bioactivities that show binding affinity of <= 500nM (387 bioactivities). (see details)