Literature DB >> 11425595

Evaluation of novel dipeptide-bound alpha,beta-unsaturated amides and epoxides as irreversible inhibitors of guinea pig liver transglutaminase.

C Marrano1, P de Macédo, J W Keillor.   

Abstract

Herein, we report the results of irreversible inhibition of guinea pig liver transglutaminase (TGase) by a series of 24 novel dipeptides containing either an alpha,beta-unsaturated amide or an epoxide functional group. Their inactivation rate constants were measured using a direct continuous spectrophotometric method and were found to vary between 421 x 10(3) and 3000 x 10(3)M(-1)min(-1).

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Year:  2001        PMID： 11425595     DOI： 10.1016/s0968-0896(01)00101-8

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN： 0968-0896            Impact factor:   3.641


  12 in total

Review 1.  Role of transglutaminase 2 in celiac disease pathogenesis.

Authors:  Cornelius Klöck; Thomas R Diraimondo; Chaitan Khosla
Journal:  Semin Immunopathol       Date:  2012-03-22       Impact factor: 9.623

2.  Structure-activity relationship analysis of the selective inhibition of transglutaminase 2 by dihydroisoxazoles.

Authors:  R Edward Watts; Mathew Siegel; Chaitan Khosla
Journal:  J Med Chem       Date:  2006-12-14       Impact factor: 7.446

3.  SAR Development of Lysine-Based Irreversible Inhibitors of Transglutaminase 2 for Huntington's Disease.

Authors:  John Wityak; Michael E Prime; Frederick A Brookfield; Stephen M Courtney; Sayeh Erfan; Siw Johnsen; Peter D Johnson; Marie Li; Richard W Marston; Laura Reed; Darshan Vaidya; Sabine Schaertl; Anna Pedret-Dunn; Maria Beconi; Douglas Macdonald; Ignacio Muñoz-Sanjuan; Celia Dominguez
Journal:  ACS Med Chem Lett       Date:  2012-10-04       Impact factor: 4.345

Review 4.  Regulation of the activities of the mammalian transglutaminase family of enzymes.

Authors:  Cornelius Klöck; Chaitan Khosla
Journal:  Protein Sci       Date:  2012-11-09       Impact factor: 6.725

5.  Acylideneoxoindoles: a new class of reversible inhibitors of human transglutaminase 2.

Authors:  Cornelius Klöck; Xi Jin; Kihang Choi; Chaitan Khosla; Peter B Madrid; Andrew Spencer; Brian C Raimundo; Paul Boardman; Guido Lanza; John H Griffin
Journal:  Bioorg Med Chem Lett       Date:  2010-12-16       Impact factor: 2.823

6.  Structure-activity relationships of hydrophobic alkyl acrylamides as tissue transglutaminase inhibitors.

Authors:  Alana M M Rangaswamy; Pauline Navals; Eric W J Gates; Sammir Shad; Sarah K I Watt; Jeffrey W Keillor
Journal:  RSC Med Chem       Date:  2022-01-26

7.  Structure-Activity Relationships of Potent, Targeted Covalent Inhibitors That Abolish Both the Transamidation and GTP Binding Activities of Human Tissue Transglutaminase.

Authors:  Abdullah Akbar; Nicole M R McNeil; Marie R Albert; Viviane Ta; Gautam Adhikary; Karine Bourgeois; Richard L Eckert; Jeffrey W Keillor
Journal:  J Med Chem       Date:  2017-09-14       Impact factor: 7.446

8.  Structure-based design of alpha-amido aldehyde containing gluten peptide analogues as modulators of HLA-DQ2 and transglutaminase 2.

Authors:  Matthew Siegel; Jiang Xia; Chaitan Khosla
Journal:  Bioorg Med Chem       Date:  2007-06-13       Impact factor: 3.641

Review 9.  Transglutaminase 2 inhibitors and their therapeutic role in disease states.

Authors:  Matthew Siegel; Chaitan Khosla
Journal:  Pharmacol Ther       Date:  2007-05-13       Impact factor: 12.310

10.  Transglutaminase activation in neurodegenerative diseases.

Authors:  Thomas M Jeitner; Nancy A Muma; Kevin P Battaile; Arthur Jl Cooper
Journal:  Future Neurol       Date:  2009-07-01
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