Literature DB >> 30876846

Walking a tightrope: drug discovery in visceral leishmaniasis.

Rafael Balaña-Fouce1, M Yolanda Pérez Pertejo1, Bárbara Domínguez-Asenjo1, Camino Gutiérrez-Corbo1, Rosa M Reguera2.   

Abstract

The current commitment of the pharma industry, nongovernmental organizations and academia to find better treatments against neglected tropical diseases should end decades of challenge caused by these global scourges. The initial result of these efforts has been the introduction of enhanced combinations of drugs, currently in clinical use, or formulations thereof. Phenotypic screening based on intracellular parasite infections has been revealed as the first key tool of antileishmanial drug discovery, because most first-in-class drugs entering Phase I trials were discovered this way. The professional commitment among stakeholders has enabled the availability of a plethora of new chemical entities that fit the target product profile for these diseases. However, the rate of hit discovery in leishmaniasis is far behind that for other neglected diseases. This review defends the need to develop new screening methods that consider the part played not only by intracellular parasites but also by the host's immune system to generate disease-relevant assays and improve clinical outcomes.
Copyright © 2019 Elsevier Ltd. All rights reserved.

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Year:  2019        PMID: 30876846     DOI: 10.1016/j.drudis.2019.03.007

Source DB:  PubMed          Journal:  Drug Discov Today        ISSN: 1359-6446            Impact factor:   7.851


  9 in total

1.  Novel Linker Variants of Antileishmanial/Antitubercular 7-Substituted 2-Nitroimidazooxazines Offer Enhanced Solubility.

Authors:  Andrew M Thompson; Patrick D O'Connor; Vanessa Yardley; Louis Maes; Delphine Launay; Stephanie Braillard; Eric Chatelain; Baojie Wan; Scott G Franzblau; Zhenkun Ma; Christopher B Cooper; William A Denny
Journal:  ACS Med Chem Lett       Date:  2021-01-21       Impact factor: 4.345

2.  Virtual Screening and the In Vitro Assessment of the Antileishmanial Activity of Lignans.

Authors:  Mayara Dos Santos Maia; Joanda Paolla Raimundo E Silva; Thaís Amanda de Lima Nunes; Julyanne Maria Saraiva de Sousa; Gabriela Cristina Soares Rodrigues; Alex France Messias Monteiro; Josean Fechine Tavares; Klinger Antonio da Franca Rodrigues; Francisco Jaime B Mendonça-Junior; Luciana Scotti; Marcus Tullius Scotti
Journal:  Molecules       Date:  2020-05-12       Impact factor: 4.411

Review 3.  Marine alkaloids as bioactive agents against protozoal neglected tropical diseases and malaria.

Authors:  Andre G Tempone; Pauline Pieper; Samanta E T Borborema; Fernanda Thevenard; Joao Henrique G Lago; Simon L Croft; Edward A Anderson
Journal:  Nat Prod Rep       Date:  2021-12-15       Impact factor: 13.423

4.  Past and future of trypanosomatids high-throughput phenotypic screening.

Authors:  Rafael Ferreira Dantas; Eduardo Caio Torres-Santos; Floriano Paes Silva
Journal:  Mem Inst Oswaldo Cruz       Date:  2022-03-11       Impact factor: 2.743

5.  Heterologous vaccine therapy associated with half course of Miltefosine promote activation of the proinflammatory response with control of splenic parasitism in a hamster model of visceral leishmaniasis.

Authors:  Lívia Mendes Carvalho; Francielle Carvalho Ferreira; Miriã Rodrigues Gusmão; Ana Flávia Pereira Costa; Rory Cristiane Fortes de Brito; Rodrigo Dian de Oliveira Aguiar-Soares; Alexandre Barbosa Reis; Jamille Mirelle de Oliveira Cardoso; Cláudia Martins Carneiro; Bruno Mendes Roatt
Journal:  Curr Res Immunol       Date:  2021-11-05

6.  Collaborative virtual screening to elaborate an imidazo[1,2-a]pyridine hit series for visceral leishmaniasis.

Authors:  Yuichiro Akao; Stacie Canan; Yafeng Cao; Kevin Condroski; Ola Engkvist; Sachiko Itono; Rina Kaki; Chiaki Kimura; Thierry Kogej; Kazuya Nagaoka; Akira Naito; Hiromi Nakai; Garry Pairaudeau; Constantin Radu; Ieuan Roberts; Mitsuyuki Shimada; David Shum; Nao-Aki Watanabe; Huanxu Xie; Shuji Yonezawa; Osamu Yoshida; Ryu Yoshida; Charles Mowbray; Benjamin Perry
Journal:  RSC Med Chem       Date:  2021-01-21

7.  Influence of N-Methylation and Conformation on Almiramide Anti-Leishmanial Activity.

Authors:  Anh Minh Thao Nguyen; Skye Brettell; Noélie Douanne; Claudia Duquette; Audrey Corbeil; Emanuella F Fajardo; Martin Olivier; Christopher Fernandez-Prada; William D Lubell
Journal:  Molecules       Date:  2021-06-12       Impact factor: 4.411

Review 8.  Screening Marine Natural Products for New Drug Leads against Trypanosomatids and Malaria.

Authors:  María Álvarez-Bardón; Yolanda Pérez-Pertejo; César Ordóñez; Daniel Sepúlveda-Crespo; Nestor M Carballeira; Babu L Tekwani; Sankaranarayanan Murugesan; Maria Martinez-Valladares; Carlos García-Estrada; Rosa M Reguera; Rafael Balaña-Fouce
Journal:  Mar Drugs       Date:  2020-03-31       Impact factor: 5.118

9.  Antileishmanial activity of terpenylquinones on Leishmania infantum and their effects on Leishmania topoisomerase IB.

Authors:  Yolanda Pérez-Pertejo; José M Escudero-Martínez; Rosa M Reguera; Rafael Balaña-Fouce; Pablo A García; Pablo G Jambrina; Arturo San Feliciano; María-Ángeles Castro
Journal:  Int J Parasitol Drugs Drug Resist       Date:  2019-10-22       Impact factor: 4.077

  9 in total

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