Literature DB >> 18513963

Design, synthesis and evaluation of potent thymidylate synthase X inhibitors.

F Esra Onen1, Yap Boum, Claire Jacquement, Maria Vittoria Spanedda, Nada Jaber, Daniel Scherman, Hannu Myllykallio, Jean Herscovici.   

Abstract

Three synthesized series of compounds based on a thiazolidine core allowed identification of potent inhibitors of thymidylate synthase X. The evaluation of the catalytic activity of the enzyme in the presence of these molecules revealed two distinct classes of compounds that inhibit ThyX with submicromolar concentrations, which could lead, after optimization, to effective inhibitors with potential biomedical interest.

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Year:  2008        PMID: 18513963     DOI: 10.1016/j.bmcl.2008.04.080

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


  13 in total

1.  Crystal structure and enzymatic characterization of thymidylate synthase X from Helicobacter pylori strain SS1.

Authors:  Kuifeng Wang; Qi Wang; Jing Chen; Lili Chen; Hualiang Jiang; Xu Shen
Journal:  Protein Sci       Date:  2011-07-06       Impact factor: 6.725

2.  Trapping of an intermediate in the reaction catalyzed by flavin-dependent thymidylate synthase.

Authors:  Tatiana V Mishanina; Eric M Koehn; John A Conrad; Bruce A Palfey; Scott A Lesley; Amnon Kohen
Journal:  J Am Chem Soc       Date:  2012-02-24       Impact factor: 15.419

3.  Biochemistry: Anchors away.

Authors:  Maria Paola Costi; Stefania Ferrari
Journal:  Nature       Date:  2009-04-16       Impact factor: 49.962

4.  Flavin-Dependent Thymidylate Synthase as a Drug Target for Deadly Microbes: Mutational Study and a Strategy for Inhibitor Design.

Authors:  Irimpan I Mathews
Journal:  J Bioterror Biodef       Date:  2013-04-20

Review 5.  Mechanisms and inhibition of uracil methylating enzymes.

Authors:  Tatiana V Mishanina; Eric M Koehn; Amnon Kohen
Journal:  Bioorg Chem       Date:  2011-11-27       Impact factor: 5.275

6.  Flavin-dependent thymidylate synthase: a novel pathway towards thymine.

Authors:  Eric M Koehn; Amnon Kohen
Journal:  Arch Biochem Biophys       Date:  2009-07-28       Impact factor: 4.013

7.  Targeting of Helicobacter pylori thymidylate synthase ThyX by non-mitotoxic hydroxy-naphthoquinones.

Authors:  Stéphane Skouloubris; Kamel Djaout; Isabelle Lamarre; Jean-Christophe Lambry; Karine Anger; Julien Briffotaux; Ursula Liebl; Hilde de Reuse; Hannu Myllykallio
Journal:  Open Biol       Date:  2015-06       Impact factor: 6.411

8.  Mechanism of Naphthoquinone Selectivity of Thymidylate Synthase ThyX.

Authors:  Hannu Myllykallio; Hubert F Becker; Alexey Aleksandrov
Journal:  Biophys J       Date:  2020-11-18       Impact factor: 4.033

9.  Mechanistic and structural basis for inhibition of thymidylate synthase ThyX.

Authors:  Tamara Basta; Yap Boum; Julien Briffotaux; Hubert F Becker; Isabelle Lamarre-Jouenne; Jean-Christophe Lambry; Stephane Skouloubris; Ursula Liebl; Marc Graille; Herman van Tilbeurgh; Hannu Myllykallio
Journal:  Open Biol       Date:  2012-10       Impact factor: 6.411

Review 10.  Flavin-Dependent Thymidylate Synthase as a New Antibiotic Target.

Authors:  Michael Choi; Kalani Karunaratne; Amnon Kohen
Journal:  Molecules       Date:  2016-05-20       Impact factor: 4.411

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