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

TTR (P02766) - Overview - Molecular Target Synopsis

Protein


TTR, Transthyretin
UniProt P02766

Also Known as TTHY_HUMAN, TTR, PALB

Thyroid hormone-binding protein. Probably transports thyroxine from the bloodstream to the brain. Homotetramer. Dimer of dimers. In the homotetramer, subunits assemble around a central channel that can accommodate two ligand molecules. Interacts with RBP4.

6FZL
CRYSTAL STRUCTURE OF HUMAN TRANSTHYRETIN DOUBLE MUTANT K35T/T119M
RCSB/PDB
Inspect Structure
See all 3D Structures for TTR

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
147ENSG00000118271ENST00000237014ENSP00000237014P02766-1

Drugs


TTR is targeted by Approved Drug Tafamidis. (see details)
Tafamidis

Sub-cellular localization


UniProt: TTR is active in the following subcellular-locations: cytoplasm, secreted.
GO terms: TTR is active in the following subcellular-locations: azurophil granule lumen, extracellular exosome, extracellular region, extracellular space, protein-containing complex.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project TTR has gain in 5 cell-lines, loss in 12 cell-lines and no signal in 988 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: SW_620, MDA_MB_435, RPMI_8226

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: HuH-7, JHH-7, JHH-5

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: HepG2, SK-N-SH, NHLF

(see details)

3D Structures


For TTR there are:
307 structures (675 chains) solved
191 are solved in complex with at least one small molecule ligand
27 are solved with an approved drug

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

TCW/TOLCAPONE (4D7B_A, 4D7B_B, 5A6I_A),
9CR/ALITRETINOIN (1TYR_A, 1TYR_B),
T44/LEVOTHYROXINE (1ETA_1, 1ETA_2, 1ETB_1, 1ETB_2, 1F86_A, 1F86_B, 1ICT_C, 1ICT_D, 2ROX_A, 2ROX_B, 3OZK_A, 3OZK_B, 5CR1_A),
DIF/DICLOFENAC (1DVX_B, 3CFQ_A, 3CFQ_B),
3MI/TAFAMIDIS (3TCT_A, 3TCT_B, 4HIS_A, 6FFT_A, 6FFT_B),
4TX/GEMFIBROZIL (5BOJ_A, 5BOJ_B),
1FL/DIFLUNISAL (3D2T_A, 3D2T_B, 4I89_A, 4I89_B),
MIL/MILRINONE (1TLM_A, 1TLM_B),
FLF/FLUFENAMIC ACID (1BM7_A, 1BM7_B, 3OZL_A, 3OZL_B),
LUR/LUMIRACOXIB (4IIZ_A, 4IIZ_B, 4IK6_A, 4IK6_B),
IMN/INDOMETHACIN (4IK7_A, 4IK7_B, 4IKI_A, 4IKI_B),
DES/DIETHYLSTILBESTROL (1TT6_A, 1TT6_B, 1TZ8_B, 1TZ8_C, 1TZ8_D).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


TTR has been screened with 576 compounds (1273 bioactivities), 23 compounds have bioactivities that show binding affinity of <= 500nM (26 bioactivities). (see details)