{"doi":"10.1101/2020.03.26.008730","title":"Ultrasensitive small molecule fluorogenic probe for human heparanase","abstract":"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.","journal":"bioRxiv (Cold Spring Harbor Laboratory)","year":2020,"id":124735,"datarank":0.0,"base_score":0.0,"endowment":0.0,"self_citation_contribution":0.0,"citation_network_contribution":0.0,"self_endowment_contribution":0.0,"citer_contribution":0.0,"corpus_percentile":null,"corpus_rank":null,"citation_count":2,"citer_count":0,"citers_with_citation_signal":0,"citers_with_endowment":0,"datacite_reuse_total":0,"is_dataset":false,"is_dataset_confidence":0.9562,"is_data_producer":false,"deposit_databanks":null,"is_oa":true,"file_count":0,"downloads":0,"has_version_chain":false,"published_date":"2020-01-01","fair_score":null,"fair_percentile":null,"algorithm_id":"datarank_citation_only_1hop_v6","ranking_scope":"data_only","authors":[{"id":371028,"name":"Kelton A. Schleyer","orcid":"0000-0001-5385-8850","position":1,"is_corresponding":false},{"id":372677,"name":"Tyrel L. Bryan","orcid":null,"position":2,"is_corresponding":false},{"id":371029,"name":"Changjian Xie","orcid":"0000-0002-2062-430X","position":3,"is_corresponding":false},{"id":371030,"name":"Gustavo Seabra","orcid":"0000-0002-1303-4483","position":4,"is_corresponding":false},{"id":288975,"name":"Yongmei Xu","orcid":"0000-0002-3756-581X","position":5,"is_corresponding":false},{"id":371031,"name":"Arjun Kafle","orcid":"0000-0001-5510-8391","position":6,"is_corresponding":false},{"id":371032,"name":"Chao Cui","orcid":"0000-0003-1154-0929","position":7,"is_corresponding":false},{"id":236249,"name":"Ying Wang","orcid":"0000-0002-1444-5778","position":8,"is_corresponding":false},{"id":372678,"name":"Kunlun Yin","orcid":null,"position":9,"is_corresponding":false},{"id":372679,"name":"Benjamin Fetrow","orcid":null,"position":10,"is_corresponding":false},{"id":372680,"name":"Paul K. P. Henderson","orcid":null,"position":11,"is_corresponding":false},{"id":372681,"name":"Peter Zannes Fatland","orcid":null,"position":12,"is_corresponding":false},{"id":569950,"name":"Jian Liu","orcid":"0000-0001-9208-6814","position":13,"is_corresponding":false},{"id":292728,"name":"Chenglong Li","orcid":"0000-0001-9460-3168","position":14,"is_corresponding":false},{"id":371033,"name":"Hua Guo","orcid":"0000-0001-9901-053X","position":15,"is_corresponding":false},{"id":371034,"name":"Lina Cui","orcid":"0000-0002-8149-5206","position":16,"is_corresponding":false},{"id":371027,"name":"Jun Liu","orcid":"0000-0002-5002-6183","position":0,"is_corresponding":true}],"reference_count":46,"raw_metadata":null,"created_at":"2026-07-18T23:15:11.632153Z","pmid":null,"pmcid":null,"fwci":null,"citation_percentile":null,"influential_citations":0,"oa_status":null,"license":null,"views":0,"total_file_size_bytes":0,"version_count":0,"fair_f":null,"fair_a":null,"fair_i":null,"fair_r":null,"fair_zscore":null,"fair_rationale":null,"fair_model":null,"fair_agent_version":null,"fair_fulltext_source":null,"fair_has_llm":null,"fair_computed_at":null,"clinical_trials":[],"software_tools":[],"db_accessions":[],"linked_datasets":[],"topics":[]}