Literature DB >> 11392545

A new structural class of selective and non-covalent inhibitors of the chymotrypsin-like activity of the 20S proteasome.

C García-Echeverría1, P Imbach, D France, P Fürst, M Lang, A M Noorani, D Scholz, J Zimmermann, P Furet.   

Abstract

We describe the identification and in vitro characterization of a series of 2-aminobenzylstatine derivatives that inhibit non-covalently the chymotrypsin-like activity of the 20S proteasome. Our initial SAR data demonstrate that the 2-aminobenzylstatine core structure can effectively serve as the basis for designing potent, selective and non-covalent inhibitors of the chymotrypsin-like activity of the 20S proteasome.

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Year:  2001        PMID: 11392545     DOI: 10.1016/s0960-894x(01)00205-0

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


  4 in total

1.  Scytonemides A and B, cyclic peptides with 20S proteasome inhibitory activity from the cultured cyanobacterium Scytonema hofmanii.

Authors:  Aleksej Krunic; Armelle Vallat; Shunyan Mo; Daniel D Lantvit; Steven M Swanson; Jimmy Orjala
Journal:  J Nat Prod       Date:  2010-11-08       Impact factor: 4.050

Review 2.  Proteasome inhibition: a new anti-inflammatory strategy.

Authors:  Peter J Elliott; Thomas Matthias Zollner; Wolf-Henning Boehncke
Journal:  J Mol Med (Berl)       Date:  2003-03-26       Impact factor: 4.599

3.  Characterization of a new series of non-covalent proteasome inhibitors with exquisite potency and selectivity for the 20S beta5-subunit.

Authors:  Christopher Blackburn; Kenneth M Gigstad; Paul Hales; Khristofer Garcia; Matthew Jones; Frank J Bruzzese; Cynthia Barrett; Jane X Liu; Teresa A Soucy; Darshan S Sappal; Nancy Bump; Edward J Olhava; Paul Fleming; Lawrence R Dick; Christopher Tsu; Michael D Sintchak; Jonathan L Blank
Journal:  Biochem J       Date:  2010-09-15       Impact factor: 3.857

4.  Peptide and Peptide-Like Modulators of 20S Proteasome Enzymatic Activity in Cancer Cells.

Authors:  Carlos García-Echeverría
Journal:  Int J Pept Res Ther       Date:  2006-03-04       Impact factor: 1.931

  4 in total

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