Sep 2, 2014

Ultrasensitive small molecule fluorogenic probe for human heparanase

bioRxiv
Christina ZakasLina Cui

Abstract

Heparanase is a critical enzyme involved in the remodeling of the extracellular matrix (ECM), and its elevated expression has been linked with diseases such as cancer and inflammation. The detection of heparanase enzymatic activity holds tremendous value in the study of the cellular microenvironment, and search of molecular therapeutics targeting heparanase, however, assays developed for this enzyme so far have suffered prohibitive drawbacks. Here we present an ultrasensitive fluorogenic small-molecule probe for heparanase enzymatic activity. 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.

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Mentioned in this Paper

Study
Size
Genetic Analysis
Genetic Screening Method
Larva
Genetic Inheritance
Streblospio benedicti
Analysis
Genotype Determination
Population Group

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