title: Controlling the intracellular localization of fluorescent polyamide analogues in cultured cells.
abstract: The intracellular distribution of fluorescent-labeled polyamides was examined in live cells. We showed that BODIPY-labeled polyamides accumulate in acidic vesicles, mainly lysosomes, in the cytoplasm of HCT116 colon cancer cells and human rheumatoid synovial fibroblasts (RSF). Verapamil blocked vesicular accumulation and led to nuclear accumulation of the BODIPY-labeled polyamide in RSFs. We infer that the basic amine group commonly found at the end of synthetic polyamide chains is responsible for their accumulation in cytoplasmic vesicles in mammalian cells. Modifying the charge on a polyamide by replacing the BODIPY moiety with a fluorescein moiety on the amine tail allowed the polyamide to localize in the nucleus of the cell and bypass the cytoplasmic vesicles in HCT116 cells.
authors.affiliation: Pharmacia Corporation, 700 Chesterfield Parkway North, Chesterfield, MO 63198, USA. kathleen.s.crowley@pharmacia.com
authors.forename: Kathleen S
authors.initials: KS
authors.lastname: Crowley
authors.forename: Dennis P
authors.initials: DP
authors.lastname: Phillion
authors.forename: Scott S
authors.initials: SS
authors.lastname: Woodard
authors.forename: Barbara A
authors.initials: BA
authors.lastname: Schweitzer
authors.forename: Megh
authors.initials: M
authors.lastname: Singh
authors.forename: Hossein
authors.initials: H
authors.lastname: Shabany
authors.forename: Barry
authors.initials: B
authors.lastname: Burnette
authors.forename: Paul
authors.initials: P
authors.lastname: Hippenmeyer
authors.forename: Monique
authors.initials: M
authors.lastname: Heitmeier
authors.forename: James K
authors.initials: JK
authors.lastname: Bashkin
mesh_terms: D001896:Boron Compounds; D002467:Cell Nucleus / Q000378:metabolism; D002478:Cells, Cultured; D005453:Fluorescence; D005456:Fluorescent Dyes; D006801:Humans; D042541:Intracellular Space / Q000378:metabolism; D009757:Nylons / Q000378:metabolism*; D014700:Verapamil / Q000494:pharmacology
chemical_list: C095489:4,4-difluoro-4-bora-3a,4a-diaza-s-indacene; D001896:Boron Compounds; D005456:Fluorescent Dyes; D009757:Nylons; D014700:Verapamil