Thioamide-based fluorescent sensors for dipeptidyl peptidase 4

Dipeptidyl peptidase 4 (DPP-4) is a promising biomarker for cancer and metabolic diseases. We demonstrate the design of novel fluorescent DPP-4 probes based on the protease's native substrates using a thioamide as a quencher for measuring in vitro kinetics, inhibition with sitagliptin, and DPP-...

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Veröffentlicht in:	Chemical communications (Cambridge, England) England), 2024-11, Vol.6 (89), p.1375-1378
Hauptverfasser:	Phan, Hoang Anh T, Chang, Yanan, Eaton, Samuel A, Petersson, E. James
Format:	Artikel
Sprache:	eng
Schlagworte:	Biomarkers Chemistry Dipeptidyl Peptidase 4 - analysis Dipeptidyl Peptidase 4 - metabolism Dipeptidyl-Peptidase IV Inhibitors - chemistry Fluorescence Fluorescent Dyes - chemistry Humans Kinetics Metabolic disorders Molecular Structure Peptidases Saliva - chemistry Sitagliptin Phosphate - chemistry Spectrometry, Fluorescence Substrate inhibition Thioamides - chemistry
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Beschreibung
Zusammenfassung:	Dipeptidyl peptidase 4 (DPP-4) is a promising biomarker for cancer and metabolic diseases. We demonstrate the design of novel fluorescent DPP-4 probes based on the protease's native substrates using a thioamide as a quencher for measuring in vitro kinetics, inhibition with sitagliptin, and DPP-4 activity in saliva samples. Thioamide sensors detect DPP-4 activity in human saliva.
ISSN:	1359-7345 1364-548X 1364-548X
DOI:	10.1039/d4cc03309d