Literature DB >> 26967915

Novel drug discovery for Chagas disease.

Carolina B Moraes1, Caio H Franco1,2.   

Abstract

INTRODUCTION: Chagas disease is a chronic infection associated with long-term morbidity. Increased funding and advocacy for drug discovery for neglected diseases have prompted the introduction of several important technological advances, and Chagas disease is among the neglected conditions that has mostly benefited from technological developments. A number of screening campaigns, and the development of new and improved in vitro and in vivo assays, has led to advances in the field of drug discovery. AREAS COVERED: This review highlights the major advances in Chagas disease drug screening, and how these are being used not only to discover novel chemical entities and drug candidates, but also increase our knowledge about the disease and the parasite. Different methodologies used for compound screening and prioritization are discussed, as well as novel techniques for the investigation of these targets. The molecular mechanism of action is also discussed. EXPERT OPINION: Technological advances have been executed with scientific rigour for the development of new in vitro cell-based assays and in vivo animal models, to bring about novel and better drugs for Chagas disease, as well as to increase our understanding of what are the necessary properties for a compound to be successful in the clinic. The gained knowledge, combined with new exciting approaches toward target deconvolution, will help identifying new targets for Chagas disease chemotherapy in the future.

Entities:  

Keywords:  Chagas disease drug discovery; Trypanosoma cruzi; high content screening; target deconvolution

Mesh:

Substances:

Year:  2016        PMID: 26967915     DOI: 10.1517/17460441.2016.1160883

Source DB:  PubMed          Journal:  Expert Opin Drug Discov        ISSN: 1746-0441            Impact factor:   6.098


  5 in total

1.  A new chemotype with promise against Trypanosoma cruzi.

Authors:  Xiaofang Wang; Monica Cal; Marcel Kaiser; Frederick S Buckner; Galina I Lepesheva; Austin G Sanford; Alexander I Wallick; Paul H Davis; Jonathan L Vennerstrom
Journal:  Bioorg Med Chem Lett       Date:  2019-10-31       Impact factor: 2.823

2.  In silico structural characterization of protein targets for drug development against Trypanosoma cruzi.

Authors:  Carlyle Ribeiro Lima; Nicolas Carels; Ana Carolina Ramos Guimaraes; Pierre Tufféry; Philippe Derreumaux
Journal:  J Mol Model       Date:  2016-09-24       Impact factor: 1.810

3.  The Correlation between Chemical Structures and Antioxidant, Prooxidant, and Antitrypanosomatid Properties of Flavonoids.

Authors:  João Luiz Baldim; Bianca Gonçalves Vasconcelos de Alcântara; Olívia da Silva Domingos; Marisi Gomes Soares; Ivo Santana Caldas; Rômulo Dias Novaes; Tiago Branquinho Oliveira; João Henrique Ghilardi Lago; Daniela Aparecida Chagas-Paula
Journal:  Oxid Med Cell Longev       Date:  2017-07-02       Impact factor: 6.543

4.  Novel structural CYP51 mutation in Trypanosoma cruzi associated with multidrug resistance to CYP51 inhibitors and reduced infectivity.

Authors:  Caio H Franco; David C Warhurst; Tapan Bhattacharyya; Ho Y A Au; Hai Le; Miriam A Giardini; Bruno S Pascoalino; Ana Claudia Torrecilhas; Lavinia M D Romera; Rafael Pedro Madeira; Sergio Schenkman; Lucio H Freitas-Junior; Eric Chatelain; Michael A Miles; Carolina B Moraes
Journal:  Int J Parasitol Drugs Drug Resist       Date:  2020-06-13       Impact factor: 4.077

5.  3-pyridyl inhibitors with novel activity against Trypanosoma cruzi reveal in vitro profiles can aid prediction of putative cytochrome P450 inhibition.

Authors:  Melissa L Sykes; Vicky M Avery
Journal:  Sci Rep       Date:  2018-03-20       Impact factor: 4.379

  5 in total

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