Literature DB >> 18636690

Structural basis for the potent calpain inhibitory activity of peptidyl alpha-ketoacids.

Isaac O Donkor1, Haregewein Assefa, Jiuyu Liu.   

Abstract

A series of peptidyl alpha-ketoacids and alpha-ketoesters was synthesized and studied as mu-calpain inhibitors. Docking studies revealed that the mu-calpain inhibitory activity of the compounds is influenced by hydrogen bonding interactions and the potential for ionic interaction with active site residues as well as placement of a planar N-terminal capping group into the S 3 pocket of the enzyme.

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Year:  2008        PMID： 18636690      PMCID： PMC2643072          DOI： 10.1021/jm800182c

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  13 in total

Review 1.  A survey of calpain inhibitors.

Authors:  I O Donkor
Journal:  Curr Med Chem       Date:  2000-12       Impact factor: 4.530

2.  A Ca(2+) switch aligns the active site of calpain.

Authors:  Tudor Moldoveanu; Christopher M Hosfield; Daniel Lim; John S Elce; Zongchao Jia; Peter L Davies
Journal:  Cell       Date:  2002-03-08       Impact factor: 41.582

Review 3.  Calcium-activated neutral protease (calpain) system: structure, function, and regulation.

Authors:  D E Croall; G N DeMartino
Journal:  Physiol Rev       Date:  1991-07       Impact factor: 37.312

Review 4.  Calpains and disease.

Authors:  Mayana Zatz; Alessandra Starling
Journal:  N Engl J Med       Date:  2005-06-09       Impact factor: 91.245

5.  The graphical determination of K m and K i .

Authors:  M Dixon
Journal:  Biochem J       Date:  1972-08       Impact factor: 3.857

6.  Calpain inhibition by alpha-ketoamide and cyclic hemiacetal inhibitors revealed by X-ray crystallography.

Authors:  D Cuerrier; T Moldoveanu; J Inoue; P L Davies; R L Campbell
Journal:  Biochemistry       Date:  2006-06-20       Impact factor: 3.162

7.  The synthesis of ketomethylene pseudopeptide analogues of dipeptide aldehyde inhibitors of calpain.

Authors:  M R Angelastro; A L Marquart; S Mehdi; J R Koehl; R J Vaz; P Bey; N P Peet
Journal:  Bioorg Med Chem Lett       Date:  1999-01-18       Impact factor: 2.823

8.  Peptide alpha-keto ester, alpha-keto amide, and alpha-keto acid inhibitors of calpains and other cysteine proteases.

Authors:  Z Li; G S Patil; Z E Golubski; H Hori; K Tehrani; J E Foreman; D D Eveleth; R T Bartus; J C Powers
Journal:  J Med Chem       Date:  1993-10-29       Impact factor: 7.446

9.  Stereospecific synthesis of peptidyl alpha-keto amides as inhibitors of calpain.

Authors:  S L Harbeson; S M Abelleira; A Akiyama; R Barrett; R M Carroll; J A Straub; J N Tkacz; C Wu; G F Musso
Journal:  J Med Chem       Date:  1994-09-02       Impact factor: 7.446

10.  Cleavage of the plasma membrane Na+/Ca2+ exchanger in excitotoxicity.

Authors:  Daniele Bano; Kenneth W Young; Christopher J Guerin; Ros Lefeuvre; Nancy J Rothwell; Luigi Naldini; Rosario Rizzuto; Ernesto Carafoli; Pierluigi Nicotera
Journal:  Cell       Date:  2005-01-28       Impact factor: 41.582
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  2 in total

1.  Peptidyl alpha-ketoamides with nucleobases, methylpiperazine, and dimethylaminoalkyl substituents as calpain inhibitors.

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Journal:  J Med Chem       Date:  2010-09-09       Impact factor: 7.446

2.  Mechanism of action of thalassospiramides, a new class of calpain inhibitors.

Authors:  Liang Lu; Michael J Meehan; Shuo Gu; Zhilong Chen; Weipeng Zhang; Gen Zhang; Lingli Liu; Xuhui Huang; Pieter C Dorrestein; Ying Xu; Bradley S Moore; Pei-Yuan Qian
Journal:  Sci Rep       Date:  2015-03-05       Impact factor: 4.379
  2 in total

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