Tetrazine-Responsive Self-immolative Linkers.

Neumann, Kevin; Jain, Sarthak; Gambardella, Alessia; Walker, Sarah E; Valero, Elsa; Lilienkampf, Annamaria; Bradley, Mark

Neumann, Kevin; Jain, Sarthak; Gambardella, Alessia; Walker, Sarah E; Valero, Elsa; Lilienkampf, Annamaria; Bradley, Mark.

Afiliação

Neumann K; EaStCHEM School of Chemistry, University of Edinburgh, Joseph Black Building, David Brewster Road, Edinburgh, EH9 3FJ, UK.
Jain S; EaStCHEM School of Chemistry, University of Edinburgh, Joseph Black Building, David Brewster Road, Edinburgh, EH9 3FJ, UK.
Gambardella A; EaStCHEM School of Chemistry, University of Edinburgh, Joseph Black Building, David Brewster Road, Edinburgh, EH9 3FJ, UK.
Walker SE; EaStCHEM School of Chemistry, University of Edinburgh, Joseph Black Building, David Brewster Road, Edinburgh, EH9 3FJ, UK.
Valero E; EaStCHEM School of Chemistry, University of Edinburgh, Joseph Black Building, David Brewster Road, Edinburgh, EH9 3FJ, UK.
Lilienkampf A; EaStCHEM School of Chemistry, University of Edinburgh, Joseph Black Building, David Brewster Road, Edinburgh, EH9 3FJ, UK.
Bradley M; EaStCHEM School of Chemistry, University of Edinburgh, Joseph Black Building, David Brewster Road, Edinburgh, EH9 3FJ, UK.

Chembiochem ; 18(1): 91-95, 2017 Jan 03.

Article em En | MEDLINE | ID: mdl-27862818

ABSTRACT

ABSTRACT

Molecules that undergo activation or modulation following the addition of benign external small-molecule chemical stimuli have numerous applications. Here, we report the highly efficient "decaging" of a variety of moieties by activation of a "self-immolative" linker, by application of water-soluble and stable tetrazine, including the controlled delivery of doxorubicin in a cellular context.

Assuntos

Portadores de Fármacos/química; Compostos Heterocíclicos com 1 Anel/química; Apoptose/efeitos dos fármacos; Linhagem Celular Tumoral; Reação de Cicloadição; Doxorrubicina/química; Doxorrubicina/metabolismo; Doxorrubicina/toxicidade; Liberação Controlada de Fármacos; Células HEK293; Humanos; Nanopartículas/química; Polietilenoglicóis/química

Palavras-chave

Diels-Alder reaction; doxorubicin; nanoparticles; prodrugs; tetrazine

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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Portadores de Fármacos / Compostos Heterocíclicos com 1 Anel Limite: Humans Idioma: En Revista: Chembiochem Assunto da revista: BIOQUIMICA Ano de publicação: 2017 Tipo de documento: Article País de afiliação: Reino Unido

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