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

TPSAB1 (Q15661) - Overview - Molecular Target Synopsis

Protein


TPSAB1, Tryptase alpha/beta-1
Enzyme Classification 3.4.21.59
UniProt Q15661

Also Known as TRYB1_HUMAN, TPSAB1, TPS1, TPS2, TPSB1

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. Isoform 2 cleaves large substrates, such as fibronectin, more efficiently than isoform 1, but seems less efficient toward small substrates (PubMed:18854315). 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.

5WI6
HUMAN BETA-1 TRYPTASE MUTANT ILE99CYS
RCSB/PDB
Inspect Structure
See all 3D Structures for TPSAB1

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: TPSAB1 is active in the following subcellular-locations: secreted.
GO terms: TPSAB1 is active in the following subcellular-locations: extracellular region, extracellular space.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project TPSAB1 has gain in 2 cell-lines, loss in 3 cell-lines and no signal in 1000 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: NCI_H460, LOXIMVI, RPMI_8226

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: OCI-AML5, U-937, ML-2

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 TPSAB1 there are:
14 structures (44 chains) solved
13 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


TPSAB1 has been screened with 601 compounds (1436 bioactivities), 345 compounds have bioactivities that show binding affinity of <= 500nM (774 bioactivities). (see details)