Ultrasensitive small molecule fluorogenic probe for human heparanase
Jun Liu, Kelton A. Schleyer, Tyrel L. Bryan, Changjian Xie, Gustavo Seabra, Yongmei Xu, Arjun Kafle, Chao Cui, Ying Wang, Kunlun Yin, Benjamin Fetrow, Paul K. P. Henderson, Peter Zannes Fatland, Jian Liu, Chenglong Li, Hua Guo, Lina Cui
Abstract
tuning the electronic effect of the substrate. The probe exhibits a 756-fold fluorescence turn-on response in the presence of human heparanase, allowing one-step detection of heparanase activity in real-time with a picomolar detection limit. The high sensitivity and robustness of the probe are exemplified in a high-throughput screening assay for heparanase inhibitors.
Topics & Concepts
HeparanaseSmall moleculeChemistryMoleculeComputational biologyNanotechnologyCombinatorial chemistryBiophysicsBiochemistryBiologyMaterials scienceOrganic chemistryCellHeparan sulfateProteoglycans and glycosaminoglycans researchCarbohydrate Chemistry and SynthesisGlycosylation and Glycoproteins Research