Literature DB >> 9871688

Inhibitors of the chymotrypsin-like activity of proteasome based on di- and tri-peptidyl alpha-keto aldehydes (glyoxals).

J F Lynas1, P Harriott, A Healy, M A McKervey, B Walker.   

Abstract

A series of peptidyl alpha-keto aldehydes (glyoxals) have been synthesised as putative inhibitors of the chymotryptic-like activity of proteasome. The most potent peptides, Cbz-Leu-Leu-Tyr-COCHO and Bz-Leu-Leu-Leu-COCHO, function as slow-binding reversible inhibitors, exhibiting final Ki values of approximately 3.0 nM. These are among the lowest values so far reported for (tri)peptide-based aldehyde-related inhibitors.

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Year:  1998        PMID： 9871688     DOI： 10.1016/s0960-894x(98)00030-4

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


  9 in total

Review 1.  The ubiquitin-proteasome pathway and proteasome inhibitors.

Authors:  J Myung; K B Kim; C M Crews
Journal:  Med Res Rev       Date:  2001-07       Impact factor: 12.944

2.  Antitrypanosomal activities of proteasome inhibitors.

Authors:  Njinkeng Joseph Nkemngu; Joseph Nkemgu-Njinkeng; Vera Rosenkranz; Michael Wink; Dietmar Steverding
Journal:  Antimicrob Agents Chemother       Date:  2002-06       Impact factor: 5.191

Review 3.  Proteasome inhibitors: an expanding army attacking a unique target.

Authors:  Alexei F Kisselev; Wouter A van der Linden; Herman S Overkleeft
Journal:  Chem Biol       Date:  2012-01-27

4.  13C-NMR study of the inhibition of delta-chymotrypsin by a tripeptide-glyoxal inhibitor.

Authors:  Aleksandra Djurdjevic-Pahl; Chandralal Hewage; J Paul G Malthouse
Journal:  Biochem J       Date:  2002-03-01       Impact factor: 3.857

5.  Epoxomicin, a potent and selective proteasome inhibitor, exhibits in vivo antiinflammatory activity.

Authors:  L Meng; R Mohan; B H Kwok; M Elofsson; N Sin; C M Crews
Journal:  Proc Natl Acad Sci U S A       Date:  1999-08-31       Impact factor: 11.205

6.  Proteasome-mediated effects on amyloid precursor protein processing at the gamma-secretase site.

Authors:  Fiona Flood; Suzanne Murphy; Richard F Cowburn; Lars Lannfelt; Brian Walker; Janet A Johnston
Journal:  Biochem J       Date:  2005-01-15       Impact factor: 3.857

7.  Metals in anticancer therapy: copper(II) complexes as inhibitors of the 20S proteasome.

Authors:  Sarmad Sahiel Hindo; Michael Frezza; Dajena Tomco; Mary Jane Heeg; Lew Hryhorczuk; Bruce R McGarvey; Q Ping Dou; Cláudio N Verani
Journal:  Eur J Med Chem       Date:  2009-05-24       Impact factor: 6.514

8.  A 13C-NMR study of the inhibition of papain by a dipeptide-glyoxal inhibitor.

Authors:  Jonathan Lowther; Aleksandra Djurdjevic-Pahl; Chandralal Hewage; J Paul G Malthouse
Journal:  Biochem J       Date:  2002-09-15       Impact factor: 3.857

9.  Natural product scaffolds as inspiration for the design and synthesis of 20S human proteasome inhibitors.

Authors:  Grace E Hubbell; Jetze J Tepe
Journal:  RSC Chem Biol       Date:  2020-09-16
  9 in total

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