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

HTR3E (A5X5Y0) - Overview - Molecular Target Synopsis

Protein


HTR3E, 5-hydroxytryptamine receptor 3E
UniProt A5X5Y0

Also Known as 5HT3E_HUMAN, HTR3E

This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. This receptor is a ligand-gated ion channel, which when activated causes fast, depolarizing responses. It is a cation-specific, but otherwise relatively nonselective, ion channel. Forms a pentaheteromeric complex with HTR3A. Not functional as a homomeric complex.

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: HTR3E is active in the following subcellular-locations: cell membrane.
GO terms: HTR3E is active in the following subcellular-locations: integral component of plasma membrane, neuron projection, plasma membrane, synapse.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project HTR3E has gain in 11 cell-lines, loss in 1 cell-lines and no signal in 993 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are:

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: SJCRH30, 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 35% identity similarity to HTR3E there are:
8 structures (40 chains) solved
8 are solved in complex with at least one small molecule ligand
1 are solved with an approved drug

HTR3E is solved in complex with the approved drug(s):

TKT/TROPISETRON (6HIS_A, 6HIS_B, 6HIS_C, 6HIS_D, 6HIS_E).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


HTR3E has been screened with 480 compounds (667 bioactivities), 218 compounds have bioactivities that show binding affinity of <= 500nM (288 bioactivities). (see details)