Literature DB >> 16304196

Interaction of monobenzamidine-linked trypanocides with the Trypanosoma brucei P2 aminopurine transporter.

Mhairi L Stewart1, Cyrille Boussard, Reto Brun, Ian H Gilbert, Michael P Barrett.   

Abstract

Single benzamidine group-carrying compounds were shown to interact with the Trypanosoma brucei P2 aminopurine transporter. Replacement of the amidine with a guanidine group decreased affinity. Trypanocidal activity was evident, but compounds were equally toxic against trypanosomes lacking the P2 transporter, which indicates additional uptake routes for monobenzamidine-derived compounds.

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Year:  2005        PMID: 16304196      PMCID: PMC1315980          DOI: 10.1128/AAC.49.12.5169-5171.2005

Source DB:  PubMed          Journal:  Antimicrob Agents Chemother        ISSN: 0066-4804            Impact factor:   5.191


  19 in total

1.  An approach to use an unusual adenosine transporter to selectively deliver polyamine analogues to trypanosomes.

Authors:  C K Tye; G Kasinathan; M P Barrett; R Brun; V E Doyle; A H Fairlamb; R Weaver; I H Gilbert
Journal:  Bioorg Med Chem Lett       Date:  1998-04-07       Impact factor: 2.823

2.  Continuous cultivation of Trypanosoma brucei blood stream forms in a medium containing a low concentration of serum protein without feeder cell layers.

Authors:  H Hirumi; K Hirumi
Journal:  J Parasitol       Date:  1989-12       Impact factor: 1.276

3.  A nucleoside transporter from Trypanosoma brucei involved in drug resistance.

Authors:  P Mäser; C Sütterlin; A Kralli; R Kaminsky
Journal:  Science       Date:  1999-07-09       Impact factor: 47.728

4.  Adenosine transporters in bloodstream forms of Trypanosoma brucei brucei: substrate recognition motifs and affinity for trypanocidal drugs.

Authors:  H P de Koning; S M Jarvis
Journal:  Mol Pharmacol       Date:  1999-12       Impact factor: 4.436

5.  Arsenical-resistant trypanosomes lack an unusual adenosine transporter.

Authors:  N S Carter; A H Fairlamb
Journal:  Nature       Date:  1993-01-14       Impact factor: 49.962

6.  The Alamar Blue assay to determine drug sensitivity of African trypanosomes (T.b. rhodesiense and T.b. gambiense) in vitro.

Authors:  B Räz; M Iten; Y Grether-Bühler; R Kaminsky; R Brun
Journal:  Acta Trop       Date:  1997-11       Impact factor: 3.112

7.  Design, synthesis and evaluation of potential inhibitors of HIV gp120-CD4 interactions.

Authors:  Cyrille Boussard; Thomas Klimkait; Naheed Mahmood; Martin Pritchard; Ian H Gilbert
Journal:  Bioorg Med Chem Lett       Date:  2004-05-17       Impact factor: 2.823

8.  The trypanocide diminazene aceturate is accumulated predominantly through the TbAT1 purine transporter: additional insights on diamidine resistance in african trypanosomes.

Authors:  Harry P de Koning; Laura F Anderson; Mhairi Stewart; Richard J S Burchmore; Lynsey J M Wallace; Michael P Barrett
Journal:  Antimicrob Agents Chemother       Date:  2004-05       Impact factor: 5.191

9.  A diamidine-resistant Trypanosoma equiperdum clone contains a P2 purine transporter with reduced substrate affinity.

Authors:  M P Barrett; Z Q Zhang; H Denise; C Giroud; T Baltz
Journal:  Mol Biochem Parasitol       Date:  1995-07       Impact factor: 1.759

10.  Uptake of diamidine drugs by the P2 nucleoside transporter in melarsen-sensitive and -resistant Trypanosoma brucei brucei.

Authors:  N S Carter; B J Berger; A H Fairlamb
Journal:  J Biol Chem       Date:  1995-11-24       Impact factor: 5.157

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Journal:  Bioorg Med Chem Lett       Date:  2006-12-03       Impact factor: 2.823

2.  Predictive computational models of substrate binding by a nucleoside transporter.

Authors:  Catharine J Collar; Mohammed I Al-Salabi; Mhairi L Stewart; Michael P Barrett; W David Wilson; Harry P de Koning
Journal:  J Biol Chem       Date:  2009-10-05       Impact factor: 5.157

3.  New insights in staging and chemotherapy of African trypanosomiasis and possible contribution of medicinal plants.

Authors:  Paul F Seke Etet; M Fawzi Mahomoodally
Journal:  ScientificWorldJournal       Date:  2012-04-19

4.  A luciferase based viability assay for ATP detection in 384-well format for high throughput whole cell screening of Trypanosoma brucei brucei bloodstream form strain 427.

Authors:  Melissa L Sykes; Vicky M Avery
Journal:  Parasit Vectors       Date:  2009-11-12       Impact factor: 3.876

  4 in total

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