title: Targeted pH-dependent fluorescent activity-based cathepsin probes.
abstract: Bifunctional, pH-activatable BODIPY dyes were developed and incorporated in mannose cluster-containing activity-based probes for cysteine proteases. Mannose receptor-dependent uptake of the probes in dendritic cells, followed by trafficking to acidic cellular compartments resulted in fluorescence as seen by live-cell imaging, and subsequent cathepsin inhibition.
authors.affiliation: Leiden Institute of Chemistry, Leiden University, P.O. Box 9052, 2300 RA Leiden, The Netherlands.
authors.forename: Sascha
authors.initials: S
authors.lastname: Hoogendoorn
authors.forename: Kim L
authors.initials: KL
authors.lastname: Habets
authors.forename: Solène
authors.initials: S
authors.lastname: Passemard
authors.forename: Johan
authors.initials: J
authors.lastname: Kuiper
authors.forename: Gijsbert A
authors.initials: GA
authors.lastname: van der Marel
authors.forename: Bogdan I
authors.initials: BI
authors.lastname: Florea
authors.forename: Herman S
authors.initials: HS
authors.lastname: Overkleeft
mesh_terms: D000818:Animals; D001896:Boron Compounds / Q000737:chemistry*; D002403:Cathepsins / Q000378:metabolism*; D003713:Dendritic Cells / Q000378:metabolism; D005456:Fluorescent Dyes / Q000737:chemistry*; D006863:Hydrogen-Ion Concentration; D007930:Leucine / Q000031:analogs & derivatives / Q000737:chemistry; D008358:Mannose / Q000737:chemistry; D051379:Mice; D008856:Microscopy, Fluorescence
chemical_list: C095489:4,4-difluoro-4-bora-3a,4a-diaza-s-indacene; D001896:Boron Compounds; C419228:DCG 04; D005456:Fluorescent Dyes; D002403:Cathepsins; D007930:Leucine; D008358:Mannose