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Synthesis and biological effect of lysosome-targeting fluorescent anion transporters with enhanced anionophoric activity
Hong,Xiao Qiao1; He,Xiang Yu1; Tam,Kin Yip3; Chen,Wen Hua1,2
2020-10-01
Source PublicationBioorganic and Medicinal Chemistry Letters
ISSN0960-894X
Volume30Issue:19
AbstractTwo lysosome-targeting fluorescent anion transporters derived from coumarins, trifluoromethylated arylsquaramides and morpholines were synthesized, and their specificity and efficiency to target and alkalize lysosomes were investigated. They are able to target lysosomes specifically. Compared with the previous analogue without trifluoromethyl substituents, these two conjugates, in particular the one having a 3,5-bis(trifluoromethyl) substituent, exhibit significantly higher ability to facilitate the transport of chloride anions, alkalize lysosomes and reduce the activity of lysosomal Cathepsin B enzyme. The present finding suggests that improving the anionophoric activity of lysosome-targeting fluorescent anion transporters is favorable to the efficiency to alkalize lysosomes and deactivate lysosomal Cathepsin B enzyme.
KeywordCathepsin B enzyme Fluorescent anion transporter Lysosomal alkalization Lysosome targeting
DOI10.1016/j.bmcl.2020.127461
URLView the original
Language英语
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Cited Times [WOS]:1   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionUniversity of Macau
Affiliation1.School of Pharmaceutical Sciences,Southern Medical University,Guangzhou,510515,China
2.School of Biotechnology and Health Sciences,International Healthcare Innovation Institute (Jiangmen),Wuyi University,Jiangmen,529020,China
3.Cancer Centre,Faculty of Health Sciences,University of Macau,Taipa,China
Recommended Citation
GB/T 7714
Hong,Xiao Qiao,He,Xiang Yu,Tam,Kin Yip,et al. Synthesis and biological effect of lysosome-targeting fluorescent anion transporters with enhanced anionophoric activity[J]. Bioorganic and Medicinal Chemistry Letters,2020,30(19).
APA Hong,Xiao Qiao,He,Xiang Yu,Tam,Kin Yip,&Chen,Wen Hua.(2020).Synthesis and biological effect of lysosome-targeting fluorescent anion transporters with enhanced anionophoric activity.Bioorganic and Medicinal Chemistry Letters,30(19).
MLA Hong,Xiao Qiao,et al."Synthesis and biological effect of lysosome-targeting fluorescent anion transporters with enhanced anionophoric activity".Bioorganic and Medicinal Chemistry Letters 30.19(2020).
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