Artículo
Positional scanning synthesis of a Peptoid library yields new inducers of apoptosis that target Karyopherins and Tubulin
Vendrell Navarro, Gloria; Rúa, Federico
; Bujons, Jordi; Brockmeyer, Andreas; Janning, Petra; Ziegler, Slava; Messeguer, Angel; Waldmann, Herbert
Fecha de publicación:
07/2015
Editorial:
Wiley VCH Verlag
Revista:
Chembiochem
e-ISSN:
1439-7633
Idioma:
Inglés
Tipo de recurso:
Artículo publicado
Clasificación temática:
Resumen
We describe the synthesis of a library of 11 638 N-alkylglycine peptoid trimers in a positional scanning format with adjustment of reaction conditions to account for different reactivities of the monomer building blocks. Evaluation of the library by high-content phenotypic screening for modulators of the cytoskeleton and mitosis resulted in the identification of two apoptosis-inducing peptoids, which, despite their structural similarity, target different proteins and cellular mechanisms. Whereas one peptoid binds to karyopherins, which mediate nuclear transport, the other N-alkylglycine trimer binds tubulin at the vinca alkaloid binding site.
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Articulos(CCT - ROSARIO)
Articulos de CTRO.CIENTIFICO TECNOL.CONICET - ROSARIO
Articulos de CTRO.CIENTIFICO TECNOL.CONICET - ROSARIO
Citación
Vendrell Navarro, Gloria; Rúa, Federico; Bujons, Jordi; Brockmeyer, Andreas; Janning, Petra ; et al.; Positional scanning synthesis of a Peptoid library yields new inducers of apoptosis that target Karyopherins and Tubulin; Wiley VCH Verlag; Chembiochem; 16; 11; 7-2015; 1580-1587
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