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

TPSB2 (P20231) - Overview - Molecular Target Synopsis

Protein


TPSB2, Tryptase beta-2
Enzyme Classification 3.4.21.59
UniProt P20231

Also Known as TRYB2_HUMAN, TPSB2, TPS2

Tryptase is the major neutral protease present in mast cells and is secreted upon the coupled activation-degranulation response of this cell type. May play a role in innate immunity. Homotetramer. The active tetramer is converted to inactive monomers at neutral and acidic pH in the absence of heparin. Low concentrations of inactive monomers become active monomers at pH 6.0 in the presence of heparin. When the concentration of active monomers is higher, they convert to active monomers and then to active tetramers. These monomers are active and functionally distinct from the tetrameric enzyme. In contrast to the hidden active sites in the tetrameric form, the active site of the monomeric form is accessible for macromolecular proteins and inhibitors eg: fibrinogen which is a substrate for the monomeric but not for the tetrameric form. The monomeric form forms a complex with SERPINB6.

3V7T
CRYSTAL STRUCTURE OF HUMAN BETA-TRYPTASE COMPLEXED WITH A SYNTHETIC INHIBITOR WITH A TROPANYLAMIDE SCAFFOLD
RCSB/PDB
Inspect Structure
See all 3D Structures for TPSB2

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform

Sub-cellular localization


UniProt: TPSB2 is active in the following subcellular-locations: secreted.
GO terms: TPSB2 is active in the following subcellular-locations: collagen-containing extracellular matrix, extracellular space.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project TPSB2 has gain in 0 cell-lines, loss in 0 cell-lines and no signal in 0 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: LOXIMVI, NCI_H522, SK_MEL_5

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: OCI-AML5, ML-2, HEL

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


For TPSB2 there are:
10 structures (40 chains) solved
10 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


TPSB2 has been screened with 601 compounds (1436 bioactivities), 345 compounds have bioactivities that show binding affinity of <= 500nM (774 bioactivities). (see details)