Literature DB >> 26666915

Identification and Characterization of FTY720 for the Treatment of Human African Trypanosomiasis.

Amy J Jones1, Marcel Kaiser2, Vicky M Avery3.   

Abstract

The screening of a focused library identified FTY720 (Fingolimod; Gilenya) as a potent selective antitrypanosomal compound active against Trypanosoma brucei gambiense and T. brucei rhodesiense, the causative agents of human African trypanosomiasis (HAT). This is the first report of trypanocidal activity for FTY720, an oral drug registered for the treatment of relapsing multiple sclerosis, and the characterization of sphingolipids as a potential new class of compounds for HAT.
Copyright © 2016, American Society for Microbiology. All Rights Reserved.

Entities:  

Mesh：

Substances：

Year:  2015        PMID： 26666915      PMCID： PMC4775930          DOI： 10.1128/AAC.02116-15

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


  23 in total

Review 1.  Fingolimod (FTY720): discovery and development of an oral drug to treat multiple sclerosis.

Authors:  Volker Brinkmann; Andreas Billich; Thomas Baumruker; Peter Heining; Robert Schmouder; Gordon Francis; Shreeram Aradhye; Pascale Burtin
Journal:  Nat Rev Drug Discov       Date:  2010-10-29       Impact factor: 84.694

2.  De novo sphingolipid synthesis is essential for viability, but not for transport of glycosylphosphatidylinositol-anchored proteins, in African trypanosomes.

Authors:  Shaheen S Sutterwala; Caleb H Creswell; Sumana Sanyal; Anant K Menon; James D Bangs
Journal:  Eukaryot Cell       Date:  2007-01-12

3.  Developmentally regulated sphingolipid synthesis in African trypanosomes.

Authors:  Shaheen S Sutterwala; Fong-Fu Hsu; Elitza S Sevova; Kevin J Schwartz; Kai Zhang; Phillip Key; John Turk; Stephen M Beverley; James D Bangs
Journal:  Mol Microbiol       Date:  2008-08-11       Impact factor: 3.501

Review 4.  Screening strategies to identify new chemical diversity for drug development to treat kinetoplastid infections.

Authors:  Rob Don; Jean-Robert Ioset
Journal:  Parasitology       Date:  2013-08-28       Impact factor: 3.234

5.  Development of an Alamar Blue viability assay 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:  Am J Trop Med Hyg       Date:  2009-10       Impact factor: 2.345

6.  Antitrypanosomal activity of fexinidazole, a new oral nitroimidazole drug candidate for treatment of sleeping sickness.

Authors:  Marcel Kaiser; Michael A Bray; Monica Cal; Bernadette Bourdin Trunz; Els Torreele; Reto Brun
Journal:  Antimicrob Agents Chemother       Date:  2011-09-12       Impact factor: 5.191

7.  Formation and remodeling of inositolphosphoceramide during differentiation of Trypanosoma cruzi from trypomastigote to amastigote.

Authors:  Maria Laura Salto; Laura E Bertello; Mauricio Vieira; Roberto Docampo; Silvia N J Moreno; Rosa M de Lederkremer
Journal:  Eukaryot Cell       Date:  2003-08

8.  Molecular species analysis of phospholipids from Trypanosoma brucei bloodstream and procyclic forms.

Authors:  P K Patnaik; M C Field; A K Menon; G A Cross; M C Yee; P Bütikofer
Journal:  Mol Biochem Parasitol       Date:  1993-03       Impact factor: 1.759

9.  Fexinidazole--a new oral nitroimidazole drug candidate entering clinical development for the treatment of sleeping sickness.

Authors:  Els Torreele; Bernadette Bourdin Trunz; David Tweats; Marcel Kaiser; Reto Brun; Guy Mazué; Michael A Bray; Bernard Pécoul
Journal:  PLoS Negl Trop Dis       Date:  2010-12-21

10.  Identification of compounds with anti-proliferative activity against Trypanosoma brucei brucei strain 427 by a whole cell viability based HTS campaign.

Authors:  Melissa L Sykes; Jonathan B Baell; Marcel Kaiser; Eric Chatelain; Sarah R Moawad; Danny Ganame; Jean-Robert Ioset; Vicky M Avery
Journal:  PLoS Negl Trop Dis       Date:  2012-11-29
View more
  3 in total

Review 1.  Novel lead compounds in pre-clinical development against African sleeping sickness.

Authors:  Michael Berninger; Ines Schmidt; Alicia Ponte-Sucre; Ulrike Holzgrabe
Journal:  Medchemcomm       Date:  2017-07-31       Impact factor: 3.597

2.  Screening a Natural Product-Based Library against Kinetoplastid Parasites.

Authors:  Bilal Zulfiqar; Amy J Jones; Melissa L Sykes; Todd B Shelper; Rohan A Davis; Vicky M Avery
Journal:  Molecules       Date:  2017-10-12       Impact factor: 4.411

Review 3.  Who Needs a Contractile Actomyosin Ring? The Plethora of Alternative Ways to Divide a Protozoan Parasite.

Authors:  Tansy C Hammarton
Journal:  Front Cell Infect Microbiol       Date:  2019-11-21       Impact factor: 5.293
  3 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.