Literature DB >> 21707314

Development of novel drugs for human African trypanosomiasis.

Reto Brun1, Robert Don, Robert T Jacobs, Michael Zhuo Wang, Michael P Barrett.   

Abstract

Human African trypanosomiasis (HAT) or 'sleeping sickness' is a neglected tropical disease caused by the parasite Trypanosoma brucei. Novel models for funding pharmaceutical development against HAT are beginning to yield results. The Drugs for Neglected Diseases initiative (DNDi) rediscovered a nitroimidazole, fexinidazole, which is currently in Phase I clinical trials. Novel benzoxaboroles, discovered by Anacor, Scynexis and DNDi, have good pharmacokinetic properties in plasma and in the brain and are curative in a murine model of stage two HAT with brain infection. The Consortium for Parasitic Drug Development (CPDD) has identified a series of dicationic compounds that can cure a monkey model of stage two HAT. With other screening programs yielding hits, the pipeline for new HAT drugs might finally begin to fill.
© 2011 Future Medicine Ltd

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Year:  2011        PMID: 21707314     DOI: 10.2217/fmb.11.44

Source DB:  PubMed          Journal:  Future Microbiol        ISSN: 1746-0913            Impact factor:   3.165


  51 in total

1.  Characterization of a melamino nitroheterocycle as a potential lead for the treatment of human african trypanosomiasis.

Authors:  Federica Giordani; Annamaria Buschini; Alessandro Baliani; Marcel Kaiser; Reto Brun; Michael P Barrett; Claudia Pellacani; Paola Poli; Ian H Gilbert
Journal:  Antimicrob Agents Chemother       Date:  2014-07-14       Impact factor: 5.191

2.  Genetic validation of aminoacyl-tRNA synthetases as drug targets in Trypanosoma brucei.

Authors:  Savitha Kalidas; Igor Cestari; Severine Monnerat; Qiong Li; Sandesh Regmi; Nicholas Hasle; Mehdi Labaied; Marilyn Parsons; Kenneth Stuart; Margaret A Phillips
Journal:  Eukaryot Cell       Date:  2014-02-21

Review 3.  Recent developments in drug discovery for leishmaniasis and human African trypanosomiasis.

Authors:  Advait S Nagle; Shilpi Khare; Arun Babu Kumar; Frantisek Supek; Andriy Buchynskyy; Casey J N Mathison; Naveen Kumar Chennamaneni; Nagendar Pendem; Frederick S Buckner; Michael H Gelb; Valentina Molteni
Journal:  Chem Rev       Date:  2014-11-03       Impact factor: 60.622

4.  Designed compounds for recognition of 10 base pairs of DNA with two at binding sites.

Authors:  Yang Liu; Yun Chai; Arvind Kumar; Richard R Tidwell; David W Boykin; W David Wilson
Journal:  J Am Chem Soc       Date:  2012-03-09       Impact factor: 15.419

5.  Substituted 2-phenylimidazopyridines: a new class of drug leads for human African trypanosomiasis.

Authors:  Hari Babu Tatipaka; J Robert Gillespie; Arnab K Chatterjee; Neil R Norcross; Matthew A Hulverson; Ranae M Ranade; Pendem Nagendar; Sharon A Creason; Joshua McQueen; Nicole A Duster; Advait Nagle; Frantisek Supek; Valentina Molteni; Tanja Wenzler; Reto Brun; Richard Glynne; Frederick S Buckner; Michael H Gelb
Journal:  J Med Chem       Date:  2014-01-15       Impact factor: 7.446

6.  In vitro and in vivo evaluation of 28DAP010, a novel diamidine for treatment of second-stage African sleeping sickness.

Authors:  Tanja Wenzler; Sihyung Yang; Donald A Patrick; Olivier Braissant; Mohamed A Ismail; Richard R Tidwell; David W Boykin; Michael Zhuo Wang; Reto Brun
Journal:  Antimicrob Agents Chemother       Date:  2014-05-27       Impact factor: 5.191

7.  A novel protein kinase is essential in bloodstream Trypanosoma brucei.

Authors:  Bryan C Jensen; Nick Booster; Rama Subba Rao Vidadala; Dustin J Maly; Marilyn Parsons
Journal:  Int J Parasitol       Date:  2016-03-23       Impact factor: 3.981

8.  Pharmacokinetics, Trypanosoma brucei gambiense efficacy, and time of drug action of DB829, a preclinical candidate for treatment of second-stage human African trypanosomiasis.

Authors:  Tanja Wenzler; Sihyung Yang; Olivier Braissant; David W Boykin; Reto Brun; Michael Zhuo Wang
Journal:  Antimicrob Agents Chemother       Date:  2013-08-19       Impact factor: 5.191

9.  Induced resistance to methionyl-tRNA synthetase inhibitors in Trypanosoma brucei is due to overexpression of the target.

Authors:  Ranae M Ranade; J Robert Gillespie; Sayaka Shibata; Christophe L M J Verlinde; Erkang Fan; Wim G J Hol; Frederick S Buckner
Journal:  Antimicrob Agents Chemother       Date:  2013-04-15       Impact factor: 5.191

10.  Trypanosoma brucei S-adenosylmethionine decarboxylase N terminus is essential for allosteric activation by the regulatory subunit prozyme.

Authors:  Nahir Velez; Chad A Brautigam; Margaret A Phillips
Journal:  J Biol Chem       Date:  2013-01-03       Impact factor: 5.157

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