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Target intelligence / Profile preview
Transmembrane protease, serine 2 (TMPRSS2)
- Target
- TMPRSS2
- Molecular classification
- Enzyme, Serine Protease, Type II Transmembrane Protein
01
Overview
Transmembrane protease serine 2 (TMPRSS2) is a type II transmembrane serine protease that plays a critical role in viral entry, particularly for coronaviruses like SARS-CoV and SARS-CoV-2, by priming viral spike proteins. It is also implicated in prostate cancer through gene fusions with ETS transcription factors. TMPRSS2 contains several domains, including a cytosolic tail, transmembrane region, LDLRA domain, SRCR domain, and a serine protease domain with a catalytic triad of His296, Asp345, and Ser441. Inhibitors like camostat mesylate (ineffective against COVID-19) and N‑0385 target its serine protease activity.
02
Mechanism of action
Serine protease inhibition
03
Biological functions
Proteolytic activation/priming of viral spike proteinsAndrogen-regulated protease activity in prostateCell membrane fusion
04
Disease associations
Viral InfectionProstate Cancer
05
Safety considerations
Potential for off-target effects due to serine protease activityResistance to inhibitors may developIncomplete understanding of long-term effects of TMPRSS2 inhibition
06
Interacting drugs
Camostat mesylate
1 more in the full profile.
07
Biomarkers
TMPRSS2-ERG gene fusion in prostate cancer
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