Imaging cellular distribution of Bcl inhibitors using small molecule drug conjugates.
Bioconjug Chem
; 25(11): 2081-5, 2014 Nov 19.
Article
em En
| MEDLINE
| ID: mdl-25333750
ABSTRACT
Overexpression of anti-apoptotic proteins such as Bcl-2 is a cellular mechanism to evade apoptosis; consequently, Bcl-2 inhibitors are being developed as anticancer agents. In this work, we have synthesized a fluorescent version of ABT-199 in an effort to visualize a drug surrogate by high resolution imaging. We show that this fluorescent conjugate has comparable Bcl-2 binding efficacy and cell line potency to the parent compound and can be used as an imaging agent in several cancer cell types. We anticipate that this agent will be a valuable tool for studying the single-cell distribution and pharmacokinetics of ABT-199 as well the broader group of BH3-mimetics.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Sulfonamidas
/
Compostos Bicíclicos Heterocíclicos com Pontes
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Proteínas Proto-Oncogênicas c-bcl-2
/
Imagem Molecular
/
Corantes Fluorescentes
Limite:
Humans
Idioma:
En
Ano de publicação:
2014
Tipo de documento:
Article