Literature DB >> 25131411

Defining the biology component of the drug discovery strategy for malaria eradication.

Didier Leroy1, Brice Campo2, Xavier C Ding2, Jeremy N Burrows2, Stéphanie Cherbuin2.   

Abstract

Malaria is still considered a deadly scourge in Africa, Asia, and South America despite improved vector control and curative treatments with new antimalarial combinations. The next challenge is to work towards disease eradication. To achieve this goal it is crucial to develop, validate, and integrate biological assays into test cascades that align with the key target product profiles. For anti-relapse, a parent molecule should kill hypnozoites or cause activation of Plasmodium vivax liver stages. For transmission blocking, dual equal-activity antimalarials killing both the asexual and the sexual parasite stages in human blood are favored. Finally, by assessing cross resistance and generating drug resistance in the laboratory, it is expected that new medicines with acceptable resistance profiles will be forthcoming.
Copyright © 2014 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  anti-relapse drugs; drug resistance; malaria; transmission blocking

Mesh:

Substances:

Year:  2014        PMID: 25131411     DOI: 10.1016/j.pt.2014.07.004

Source DB:  PubMed          Journal:  Trends Parasitol        ISSN: 1471-4922


  19 in total

1.  Luciferase-Based, High-Throughput Assay for Screening and Profiling Transmission-Blocking Compounds against Plasmodium falciparum Gametocytes.

Authors:  Leonardo Lucantoni; David A Fidock; Vicky M Avery
Journal:  Antimicrob Agents Chemother       Date:  2016-03-25       Impact factor: 5.191

2.  Interrogating alkyl and arylalkylpolyamino (bis)urea and (bis)thiourea isosteres as potent antimalarial chemotypes against multiple lifecycle forms of Plasmodium falciparum parasites.

Authors:  Bianca K Verlinden; Marna de Beer; Boobalan Pachaiyappan; Ethan Besaans; Warren A Andayi; Janette Reader; Jandeli Niemand; Riette van Biljon; Kiplin Guy; Timothy Egan; Patrick M Woster; Lyn-Marie Birkholtz
Journal:  Bioorg Med Chem       Date:  2015-01-28       Impact factor: 3.641

Review 3.  Killing the hypnozoite--drug discovery approaches to prevent relapse in Plasmodium vivax.

Authors:  Brice Campo; Omar Vandal; David L Wesche; Jeremy N Burrows
Journal:  Pathog Glob Health       Date:  2015-04-18       Impact factor: 2.894

4.  Small-molecule xenomycins inhibit all stages of the Plasmodium life cycle.

Authors:  Jessey Erath; Julio Gallego-Delgado; Wenyue Xu; Grasiella Andriani; Scott Tanghe; Katerina V Gurova; Andrei Gudkov; Andrei Purmal; Elena Rydkina; Ana Rodriguez
Journal:  Antimicrob Agents Chemother       Date:  2014-12-15       Impact factor: 5.191

5.  Identification and deconvolution of cross-resistance signals from antimalarial compounds using multidrug-resistant Plasmodium falciparum strains.

Authors:  Monika Chugh; Christian Scheurer; Sibylle Sax; Elizabeth Bilsland; Donelly A van Schalkwyk; Kathryn J Wicht; Natalie Hofmann; Anil Sharma; Sridevi Bashyam; Shivendra Singh; Stephen G Oliver; Timothy J Egan; Pawan Malhotra; Colin J Sutherland; Hans-Peter Beck; Sergio Wittlin; Thomas Spangenberg; Xavier C Ding
Journal:  Antimicrob Agents Chemother       Date:  2014-12-08       Impact factor: 5.191

6.  Efficient Synthesis of 1,9-Substituted Benzo[h][1,6]naphthyridin-2(1H)-ones and Evaluation of their Plasmodium falciparum Gametocytocidal Activities.

Authors:  Hao Li; Wei Sun; Xiuli Huang; Xiao Lu; Paresma R Patel; Myunghoon Kim; Meghan J Orr; Richard M Fisher; Takeshi Q Tanaka; John C McKew; Anton Simeonov; Philip E Sanderson; Wei Zheng; Kim C Williamson; Wenwei Huang
Journal:  ACS Comb Sci       Date:  2017-10-27       Impact factor: 3.784

Review 7.  Assessing risks of Plasmodium falciparum resistance to select next-generation antimalarials.

Authors:  Maëlle Duffey; Benjamin Blasco; Jeremy N Burrows; Timothy N C Wells; David A Fidock; Didier Leroy
Journal:  Trends Parasitol       Date:  2021-05-14

8.  Morphological and Molecular Descriptors of the Developmental Cycle of Babesia divergens Parasites in Human Erythrocytes.

Authors:  Ingrid Rossouw; Christine Maritz-Olivier; Jandeli Niemand; Riette van Biljon; Annel Smit; Nicholas A Olivier; Lyn-Marie Birkholtz
Journal:  PLoS Negl Trop Dis       Date:  2015-05-08

Review 9.  The malaria parasite cation ATPase PfATP4 and its role in the mechanism of action of a new arsenal of antimalarial drugs.

Authors:  Natalie Jane Spillman; Kiaran Kirk
Journal:  Int J Parasitol Drugs Drug Resist       Date:  2015-08-27       Impact factor: 4.077

10.  Characterization of Novel Antimalarial Compound ACT-451840: Preclinical Assessment of Activity and Dose-Efficacy Modeling.

Authors:  Amélie Le Bihan; Ruben de Kanter; Iñigo Angulo-Barturen; Christoph Binkert; Christoph Boss; Reto Brun; Ralf Brunner; Stephan Buchmann; Jeremy Burrows; Koen J Dechering; Michael Delves; Sonja Ewerling; Santiago Ferrer; Christoph Fischli; Francisco Javier Gamo-Benito; Nina F Gnädig; Bibia Heidmann; María Belén Jiménez-Díaz; Didier Leroy; Maria Santos Martínez; Solange Meyer; Joerg J Moehrle; Caroline L Ng; Rintis Noviyanti; Andrea Ruecker; Laura María Sanz; Robert W Sauerwein; Christian Scheurer; Sarah Schleiferboeck; Robert Sinden; Christopher Snyder; Judith Straimer; Grennady Wirjanata; Jutta Marfurt; Ric N Price; Thomas Weller; Walter Fischli; David A Fidock; Martine Clozel; Sergio Wittlin
Journal:  PLoS Med       Date:  2016-10-04       Impact factor: 11.069

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