A fluorescent light-up probe as an inhibitor of intracellular β-tryptase.
A pyrene-functionalized peptidic inhibitor binds to and inhibits β-tryptase in a non-competitive and reversible manner even in cells. Upon protein binding a fluorescence increase of the two pyrene fluorophores is observed which allows using as a fluorescent light-up probe for this enzyme.
College of Public Health, Nantong University, 9 Seyuan Road, Nantong, 226019, China.
Qi
Q
Wang
Xiuyin
X
Shi
Xiaoxia
X
Zhu
Martin
M
Ehlers
Junchen
J
Wu
Carsten
C
Schmuck
D016923:Cell Death / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D005456:Fluorescent Dyes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D008027:Light; D008407:Mast Cells; D008958:Models, Molecular; D008968:Molecular Conformation; D015842:Serine Proteinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D053802:Tryptases / Q000037:antagonists & inhibitors* / Q000378:metabolism
D005456:Fluorescent Dyes; D015842:Serine Proteinase Inhibitors; D053802:Tryptases