The use of a diversity oriented synthesis (DOS) approach on a series of Ugi-derived oxabicyclic peptidomimetics resulted in the generation of a set of libraries of compounds presenting novel structural cores. These chemical cores have been employed to design potential antagonists of the antiapoptotic protein Bcl-xL through reiterated steps of molecular docking calculations followed by experimental verification of binding. Our data suggest that the DOS approach is suitable to generate novel scaffolds, which can be employed to target protein-protein interactions.

Identification of Lead Compounds As Antagonists of Protein Bcl-xL with a Diversity-Oriented Multidisciplinary Approach

RIVA, RENATA;BASSO, ANDREA;
2009-01-01

Abstract

The use of a diversity oriented synthesis (DOS) approach on a series of Ugi-derived oxabicyclic peptidomimetics resulted in the generation of a set of libraries of compounds presenting novel structural cores. These chemical cores have been employed to design potential antagonists of the antiapoptotic protein Bcl-xL through reiterated steps of molecular docking calculations followed by experimental verification of binding. Our data suggest that the DOS approach is suitable to generate novel scaffolds, which can be employed to target protein-protein interactions.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11567/250508
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