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Fluorescent Probes of the Apoptolidins and their Utility in Cellular Localization Studies

DeGuire, Sean M. ; Earl, David C. ; Du, Yu ; Crews, Brenda A. ; Jacobs, Aaron T. ; Ustione, Alessandro ; Daniel, Cristina ; Chong, Katherine M. ; Marnett, Lawrence J. ; Piston, David W. ; Bachmann, Brian O. ; Sulikowski, Gary A.

Angewandte Chemie, 2015-01, Vol.127 (3), p.975-978 [Periódico revisado por pares]

Weinheim: WILEY-VCH Verlag

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  • Título:
    Fluorescent Probes of the Apoptolidins and their Utility in Cellular Localization Studies
  • Autor: DeGuire, Sean M. ; Earl, David C. ; Du, Yu ; Crews, Brenda A. ; Jacobs, Aaron T. ; Ustione, Alessandro ; Daniel, Cristina ; Chong, Katherine M. ; Marnett, Lawrence J. ; Piston, David W. ; Bachmann, Brian O. ; Sulikowski, Gary A.
  • Assuntos: Biotechnology ; Cellular ; Chemistry ; Cycloaddition ; Derivatives ; Fluoreszenzsonden ; Lungs ; Metabolismus ; Molecular structure ; Naturstoffe ; Panels ; Polyketide ; Position (location) ; Tumortherapeutika
  • É parte de: Angewandte Chemie, 2015-01, Vol.127 (3), p.975-978
  • Notas: Vanderbilt Chemical Biology Interface (CBI) - No. T32 GM065086
    This research was supported by the National Institutes of Health (CA 059515). S.M.D. and D.C.E. acknowledge the support of the Vanderbilt Chemical Biology Interface (CBI) training program (T32 GM065086).
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    National Institutes of Health - No. CA 059515
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    SourceType-Scholarly Journals-1
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    content type line 23
  • Descrição: Apoptolidin A has been described among the top 0.1 % most‐cell‐selective cytotoxic agents to be evaluated in the NCI 60 cell line panel. The molecular structure of apoptolidin A consists of a 20‐membered macrolide with mono‐ and disaccharide moieties. In contrast to apoptolidin A, the aglycone (apoptolidinone) shows no cytotoxicity (>10 μM) when evaluated against several tumor cell lines. Apoptolidin H, the C27 deglycosylated analogue of apoptolidin A, displayed sub‐micromolar activity against H292 lung carcinoma cells. Selective esterification of apoptolidins A and H with 5‐azidopentanoic acid afforded azido‐functionalized derivatives of potency equal to that of the parent macrolide. They also underwent strain‐promoted alkyne–azido cycloaddition reactions to provide access to fluorescent and biotin‐functionalized probes. Microscopy studies demonstrate apoptolidins A and H localize in the mitochondria of H292 human lung carcinoma cells. Ausgesprochen wählerisch: Apoptolidine zählen zu den 0.1 % zellselektivsten zytotoxischen Substanzen, die im 60‐Zelllinientest des NCI untersucht worden sind. Eine Kombination aus Gendeletion (um die Biosynthesemaschinerie zu manipulieren) und chemischer Synthese macht neue fluoreszierende Apoptolidin‐Derivate für biologische Studien zugänglich.
  • Editor: Weinheim: WILEY-VCH Verlag
  • Idioma: Inglês;Alemão
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