Literature DB >> 16962325

Identification of novel inhibitors of UDP-Glc 4'-epimerase, a validated drug target for african sleeping sickness.

Michael D Urbaniak1, Jioji N Tabudravu, Aichi Msaki, Kathy Mansfield Matera, Ruth Brenk, Marcel Jaspars, Michael A J Ferguson.   

Abstract

Novel inhibitors of Trypanosoma brucei and mammalian UDP-Glc 4'-epimerase were identified by screening a small library of natural products and commercially available drug-like molecules. The inhibitors possess low micromolar potency against the T. brucei and human enzymes in vitro, display a degree of selectivity between the two enzymes, and are cytotoxic to cultured T. brucei and mammalian cells.

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Year:  2006        PMID： 16962325     DOI： 10.1016/j.bmcl.2006.08.091

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


  17 in total

1.  In silico work flow for scaffold hopping in Leishmania.

Authors:  Barnali Waugh; Ambarnil Ghosh; Dhananjay Bhattacharyya; Nanda Ghoshal; Rahul Banerjee
Journal:  BMC Res Notes       Date:  2014-11-17

2.  Deletion of UDP-glucose pyrophosphorylase reveals a UDP-glucose independent UDP-galactose salvage pathway in Leishmania major.

Authors:  Anne-Christin Lamerz; Sebastian Damerow; Barbara Kleczka; Martin Wiese; Ger van Zandbergen; Jens Lamerz; Alexander Wenzel; Fong-Fu Hsu; John Turk; Stephen M Beverley; Françoise H Routier
Journal:  Glycobiology       Date:  2010-03-24       Impact factor: 4.313

3.  A target-based high throughput screen yields Trypanosoma brucei hexokinase small molecule inhibitors with antiparasitic activity.

Authors:  Elizabeth R Sharlow; Todd A Lyda; Heidi C Dodson; Gabriela Mustata; Meredith T Morris; Stephanie S Leimgruber; Kuo-Hsiung Lee; Yoshiki Kashiwada; David Close; John S Lazo; James C Morris
Journal:  PLoS Negl Trop Dis       Date:  2010-04-13

4.  Computer-aided identification of Trypanosoma brucei uridine diphosphate galactose 4'-epimerase inhibitors: toward the development of novel therapies for African sleeping sickness.

Authors:  Jacob D Durrant; Michael D Urbaniak; Michael A J Ferguson; J Andrew McCammon
Journal:  J Med Chem       Date:  2010-07-08       Impact factor: 7.446

5.  The aignopsanes, a new class of sesquiterpenes from selected chemotypes of the sponge Cacospongia mycofijiensis.

Authors:  Tyler A Johnson; Taro Amagata; Koneni V Sashidhara; Allen G Oliver; Karen Tenney; Teatulohi Matainaho; Kenny Kean-Hooi Ang; James H McKerrow; Phillip Crews
Journal:  Org Lett       Date:  2009-05-07       Impact factor: 6.005

6.  Sugar nucleotide pools of Trypanosoma brucei, Trypanosoma cruzi, and Leishmania major.

Authors:  Daniel C Turnock; Michael A J Ferguson
Journal:  Eukaryot Cell       Date:  2007-06-08

7.  Identification of Genes Conferring Tolerance to Lignocellulose-Derived Inhibitors by Functional Selections in Soil Metagenomes.

Authors:  Kevin J Forsberg; Sanket Patel; Evan Witt; Bin Wang; Tyler D Ellison; Gautam Dantas
Journal:  Appl Environ Microbiol       Date:  2015-11-06       Impact factor: 4.792

8.  The marine sponge Diacarnus bismarckensis as a source of peroxiterpene inhibitors of Trypanosoma brucei, the causative agent of sleeping sickness.

Authors:  Brent K Rubio; Karen Tenney; Kean-Hooi Ang; Maha Abdulla; Michelle Arkin; James H McKerrow; Phillip Crews
Journal:  J Nat Prod       Date:  2009-02-27       Impact factor: 4.050

9.  Mining the human gut microbiome for novel stress resistance genes.

Authors:  Eamonn P Culligan; Julian R Marchesi; Colin Hill; Roy D Sleator
Journal:  Gut Microbes       Date:  2012-06-12

10.  UDP-galactose 4'-epimerase from the liver fluke, Fasciola hepatica: biochemical characterization of the enzyme and identification of inhibitors.

Authors:  Veronika L Zinsser; Steffen Lindert; Samantha Banford; Elizabeth M Hoey; Alan Trudgett; David J Timson
Journal:  Parasitology       Date:  2014-08-15       Impact factor: 3.234
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