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α- and β-hydrazino acid-based pseudopeptides inhibit the chymotrypsin-like activity of the eukaryotic 20S proteasome.

Abstract：

:We describe the synthesis of a library of new pseudopeptides and their inhibitory activity of the rabbit 20S proteasome chymotrypsin-like (ChT-L) activity. We replaced a natural α-amino acid by an α- or a β-hydrazino acid and obtained inhibitors of proteasome up to a submicromolar range (0.7 μM for molecule 24b). Structural variations influenced the inhibition of the ChT-L activity. Models of inhibitor/20S proteasome complexes corroborated the inhibition efficacies obtained by kinetic studies.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Bordessa A,Keita M,Maréchal X,Formicola L,Lagarde N,Rodrigo J,Bernadat G,Bauvais C,Soulier JL,Dufau L,Milcent T,Crousse B,Reboud-Ravaux M,Ongeri S

doi

10.1016/j.ejmech.2013.09.059

subject

Has Abstract

pub_date

2013-01-01 00:00:00

pages

505-24

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(13)00640-5

journal_volume

70

pub_type

杂志文章

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