Literature DB >> 19041239

Novel fluorinated pseudopeptides as proteasome inhibitors.

Lucia Formicola1, Xavier Maréchal, Nicolas Basse, Michelle Bouvier-Durand, Danièle Bonnet-Delpon, Thierry Milcent, Michèle Reboud-Ravaux, Sandrine Ongeri.   

Abstract

We have designed novel small inhibitors of rabbit 20S proteasome using a trifluoromethyl-beta-hydrazino acid scaffold. Structural variations influenced their inhibition of the three types of active sites. Proteasome inhibition at the micromolar level was selective, calpain I and cathepsin B were not inhibited.

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Year:  2008        PMID： 19041239     DOI： 10.1016/j.bmcl.2008.11.012

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  5 in total

1.  Oxadiazole-isopropylamides as potent and noncovalent proteasome inhibitors.

Authors:  Sevil Ozcan; Aslamuzzaman Kazi; Frank Marsilio; Bin Fang; Wayne C Guida; John Koomen; Harshani R Lawrence; Saïd M Sebti
Journal:  J Med Chem       Date:  2013-05-13       Impact factor: 7.446

2.  Incorporation of fluorinated phenylalanine generates highly specific inhibitor of proteasome's chymotrypsin-like sites.

Authors:  Paul P Geurink; Nora Liu; Michiel P Spaans; Sondra L Downey; Adrianus M C H van den Nieuwendijk; Gijsbert A van der Marel; Alexei F Kisselev; Bogdan I Florea; Herman S Overkleeft
Journal:  J Med Chem       Date:  2010-03-11       Impact factor: 7.446

3.  Novel synthesis of pseudopeptides bearing a difluoromethyl group by Ugi reaction and desulfanylation.

Authors:  Jingjing Wu; Hui Li; Song Cao
Journal:  Beilstein J Org Chem       Date:  2011-08-08       Impact factor: 2.883

4.  Interplay between Structure and Charge as a Key to Allosteric Modulation of Human 20S Proteasome by the Basic Fragment of HIV-1 Tat Protein.

Authors:  Przemysław Karpowicz; Paweł A Osmulski; Julia Witkowska; Emilia Sikorska; Małgorzata Giżyńska; Agnieszka Belczyk-Ciesielska; Maria E Gaczynska; Elżbieta Jankowska
Journal:  PLoS One       Date:  2015-11-17       Impact factor: 3.240

5.  Inhibition of human and yeast 20S proteasome by analogues of trypsin inhibitor SFTI-1.

Authors:  Dawid Dębowski; Michał Pikuła; Marta Lubos; Paulina Langa; Piotr Trzonkowski; Adam Lesner; Anna Łęgowska; Krzysztof Rolka
Journal:  PLoS One       Date:  2014-02-25       Impact factor: 3.240
  5 in total

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