Turning a scorpion toxin into an antitumor miniprotein.
J Am Chem Soc
; 130(41): 13546-8, 2008 Oct 15.
Article
en En
| MEDLINE
| ID: mdl-18798622
ABSTRACT
The oncoproteins MDM2 and MDMX negatively regulate the activity and stability of the tumor suppressor protein p53 and are important molecular targets for anticancer therapy. Grafting four residues of p53 critical for MDM2/MDMX binding to the N-terminal alpha-helix of BmBKTx1, a scorpion toxin isolated from the venom of the Asian scorpion Buthus martensi Karsch, converts the miniature protein into an effective inhibitor of p53 interactions with MDM2 and MDMX. Additional mutations enable the 27-residue miniprotein inhibitor to traverse the cell membrane and selectively kill tumor cells in a p53 dependent manner.
Texto completo:
1
Bases de datos:
MEDLINE
Asunto principal:
Venenos de Escorpión
/
Escorpiones
/
Antineoplásicos
Tipo de estudio:
Prognostic_studies
Límite:
Animals
Idioma:
En
Revista:
J Am Chem Soc
Año:
2008
Tipo del documento:
Article
País de afiliación:
Estados Unidos