Development of tricyanofuran-based activity probes for sulfatase assay in live cells
DC Field | Value | Language |
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dc.contributor.author | Yoon, Hey Young | - |
dc.contributor.author | Lee, Jung Hoon | - |
dc.contributor.author | Bin Park, Seung | - |
dc.contributor.author | Choi, Sang-Hyun | - |
dc.contributor.author | Lee, Jun-Seok | - |
dc.contributor.author | Hong, Jong-In | - |
dc.date.accessioned | 2022-08-10T09:41:11Z | - |
dc.date.available | 2022-08-10T09:41:11Z | - |
dc.date.created | 2022-08-10 | - |
dc.date.issued | 2022-09 | - |
dc.identifier.issn | 0143-7208 | - |
dc.identifier.uri | https://scholar.korea.ac.kr/handle/2021.sw.korea/142724 | - |
dc.description.abstract | Sulfatase plays a pivotal role in the regulation of biologically active metabolites associated with various diseases. In particular, the up-regulation of steroid sulfatase activity has a positive correlation with breast cancer due to the increment of estrone levels via the desulfation reaction of estron 3-sulfate. Despite the high association between sulfatase activity and disease occurrence, there has been little progress in the discovery of sulfatase inhibitors, possibly due to the lack of robust activity-based assays. To design a sulfatase activity probe, we examined the binding between four fluorophores (coumarin, BODIPY, rhodol, and tricyanofuran [TCF]) and three isoforms of sulfatase using docking simulations and found that the rhodol and TCF scaffolds exhibited stable binding. To avoid the charge-driven organelle accumulation bias, we chose TCF as the core structure and designed two probes containing sulfate (TCF-OSulf and TCF-NCOO-OSulf). The TCF probes showed clear colorimetric response and 2.7-fold and 5-fold fluorescence enhancements in vitro. In addition, the probes detected the inhibition of the enzyme by estrone-O-sulfamate (EMATE) in a time-dependent manner. Since cell -based screening has many advantages over the traditional high-throughput assay in vitro, we further examined TCF probes for the inhibitor assay for sulfatase activity in live cells. Based on our observations, TCF-NCOO-OSulf could be used to monitor sulfatase activity in live cells at a concentration of 5 mu M. This is the first sulfatase activity-based probe that can visualize activity and inhibition in live cell conditions. | - |
dc.language | English | - |
dc.language.iso | en | - |
dc.publisher | ELSEVIER SCI LTD | - |
dc.subject | STEROID SULFATASE | - |
dc.subject | ESTRONE SULFATASE | - |
dc.subject | POTENT INHIBITORS | - |
dc.subject | FLUOROPHORES | - |
dc.subject | ENZYME | - |
dc.title | Development of tricyanofuran-based activity probes for sulfatase assay in live cells | - |
dc.type | Article | - |
dc.contributor.affiliatedAuthor | Lee, Jun-Seok | - |
dc.identifier.doi | 10.1016/j.dyepig.2022.110517 | - |
dc.identifier.scopusid | 2-s2.0-85132860486 | - |
dc.identifier.wosid | 000830055400003 | - |
dc.identifier.bibliographicCitation | DYES AND PIGMENTS, v.205 | - |
dc.relation.isPartOf | DYES AND PIGMENTS | - |
dc.citation.title | DYES AND PIGMENTS | - |
dc.citation.volume | 205 | - |
dc.type.rims | ART | - |
dc.type.docType | Article | - |
dc.description.journalClass | 1 | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
dc.relation.journalResearchArea | Chemistry | - |
dc.relation.journalResearchArea | Engineering | - |
dc.relation.journalResearchArea | Materials Science | - |
dc.relation.journalWebOfScienceCategory | Chemistry, Applied | - |
dc.relation.journalWebOfScienceCategory | Engineering, Chemical | - |
dc.relation.journalWebOfScienceCategory | Materials Science, Textiles | - |
dc.subject.keywordPlus | STEROID SULFATASE | - |
dc.subject.keywordPlus | ESTRONE SULFATASE | - |
dc.subject.keywordPlus | POTENT INHIBITORS | - |
dc.subject.keywordPlus | FLUOROPHORES | - |
dc.subject.keywordPlus | ENZYME | - |
dc.subject.keywordAuthor | Fluorescent probe | - |
dc.subject.keywordAuthor | Sulfatase activity | - |
dc.subject.keywordAuthor | Live cell image -based inhibitor screening | - |
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