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

HTR3A (P46098) - Overview - Molecular Target Synopsis

Protein


HTR3A, 5-hydroxytryptamine receptor 3A
UniProt P46098

Also Known as 5HT3A_HUMAN, HTR3A, 5HT3R, HTR3

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 in neurons. It is a cation-specific, but otherwise relatively nonselective, ion channel. Forms pentahomomeric complex as well as pentaheteromeric complex with HTR3B or HTR3C or HTR3D or HTR3E; homomeric complex is functional but exhibits low conductance with modified voltage dependence, and decreased agonist and antagonist affinity. Interacts with RIC3.

Isoforms / Transcripts (Protein Coding)


Drugs


HTR3A is targeted by Approved Drugs Amoxapine, Mirtazapine, Granisetron, Ondansetron, Metoclopramide, Alosetron. (see details)
Amoxapine
Mirtazapine
Granisetron
Ondansetron
Metoclopramide
Alosetron

Sub-cellular localization


Gene Copy Number Variation


In COSMIC - Cell Lines Project HTR3A has gain in 1 cell-lines, loss in 9 cell-lines and no signal in 995 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: RXF_393, MOLT_4, MCF7

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: SK-N-FI, OCI-LY-3, SU-DHL-16

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 75% identity similarity to HTR3A 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

HTR3A 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


HTR3A has been screened with 1405 compounds (1894 bioactivities), 523 compounds have bioactivities that show binding affinity of <= 500nM (680 bioactivities). (see details)