Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
Bioorg Med Chem Lett
; 21(14): 4332-6, 2011 Jul 15.
Article
em En
| MEDLINE
| ID: mdl-21680182
ABSTRACT
We report the systematic rational design and synthesis of new monovalent Smac mimetics that bind preferentially to the BIR2 domain of the anti-apoptotic protein XIAP. Characterization of compounds in vitro (including 9i; ML101) led to the determination of key structural requirements for BIR2 binding affinity. Compounds 9h and 9j sensitized TRAIL-resistant breast cancer cells to apoptotic cell death, highlighting the value of these probe compounds as tools to investigate the biology of XIAP.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Proteínas Mitocondriais
/
Proteínas Reguladoras de Apoptose
/
Proteínas Inibidoras de Apoptose Ligadas ao Cromossomo X
Tipo de estudo:
Prognostic_studies
Limite:
Humans
Idioma:
En
Ano de publicação:
2011
Tipo de documento:
Article