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TropicalMed
Special Issues
Drug Discovery and Development for Tropical Diseases
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Drug Discovery and Development for Tropical Diseases

A special issue of Tropical Medicine and Infectious Disease (ISSN 2414-6366). This special issue belongs to the section "Neglected and Emerging Tropical Diseases".

Deadline for manuscript submissions: closed (1 March 2019) | Viewed by 26948

Special Issue Editor

Prof. Dr. Michael P. Pollastri

E-Mail Website
Guest Editor
Department of Chemistry & Chemical Biology, Northeastern University, Boston, MA, USA
Interests: medicinal chemistry; neglected diseases; drug discovery; global health

Special Issue Information

Dear Colleagues,

The tropical diseases highlighted by the World Health Organization represent an enormous disease burden, affecting billions worldwide. Importantly, those most affected by these diseases are those in the low-income populations of developing countries in Asia, South and Central America, and Africa.

The community of researchers focusing on drug discovery and development for tropical diseases has expanded over the last ten to fifteen years, spawned by significant investment by governmental, non-governmental, and charitable organizations. As a result, the literature has swelled with news of innovative approaches for discovery, new molecules for advancement to clinical trials, new drugs or drug combinations, and repurposed drugs for tropical disease therapeutics. Though the percentage of research dollars spent for tropical diseases remains significantly disproportionate to the disease burden presented by tropical diseases, there is reason for hope that progress will accelerate towards disease eradication or elimination over the coming decades.

This Special Issue in Tropical Medicine and Infectious Disease will be populated with new research reports, perspectives, and review articles focusing on the most cutting-edge research programs in tropical disease drug discovery and development.

We are seeking articles that span the broad range from early discovery (target identification and validation, compound screening), through medicinal chemistry optimization, preclinical research, and clinical trials. Beyond this, challenges of distribution of new therapeutics and disease monitoring are of interest. In a small community such as that focused on tropical disease drug discovery, it is essential that information is shared broadly across groups in order to reduce duplication of effort, to inform each other’s research, and to accelerate new discoveries.

Prof. Michael P. Pollastri
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Tropical Medicine and Infectious Disease is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2700 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • medicinal chemistry
  • neglected diseases
  • drug discovery
  • tropical diseases

Published Papers (5 papers)

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Research

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17 pages, 2249 KiB  
Article
Drug Discovery for Chagas Disease: Impact of Different Host Cell Lines on Assay Performance and Hit Compound Selection
by Caio Haddad Franco, Laura Maria Alcântara, Eric Chatelain, Lucio Freitas-Junior and Carolina Borsoi Moraes
Trop. Med. Infect. Dis. 2019, 4(2), 82; https://0-doi-org.brum.beds.ac.uk/10.3390/tropicalmed4020082 - 17 May 2019
Cited by 31 | Viewed by 5439
Abstract
Cell-based screening has become the major compound interrogation strategy in Chagas disease drug discovery. Several different cell lines have been deployed as host cells in screening assays. However, host cell characteristics and host-parasite interactions may play an important role when assessing anti-T. [...] Read more.
Cell-based screening has become the major compound interrogation strategy in Chagas disease drug discovery. Several different cell lines have been deployed as host cells in screening assays. However, host cell characteristics and host-parasite interactions may play an important role when assessing anti-T. cruzi compound activity, ultimately impacting on hit discovery. To verify this hypothesis, four distinct mammalian cell lines (U2OS, THP-1, Vero and L6) were used as T. cruzi host cells in High Content Screening assays. Rates of infection varied greatly between different host cells. Susceptibility to benznidazole also varied, depending on the host cell and parasite strain. A library of 1,280 compounds was screened against the four different cell lines infected with T. cruzi, resulting in the selection of a total of 82 distinct compounds as hits. From these, only two hits were common to all four cell lines assays (2.4%) and 51 were exclusively selected from a single assay (62.2%). Infected U2OS cells were the most sensitive assay, as 55 compounds in total were identified as hits; infected THP-1 yielded the lowest hit rates, with only 16 hit compounds. Of the selected hits, compound FPL64176 presented selective anti-T. cruzi activity and could serve as a starting point for the discovery of new anti-chagasic drugs. Full article
(This article belongs to the Special Issue Drug Discovery and Development for Tropical Diseases)
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Review

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26 pages, 3229 KiB  
Review
Advances in Antiwolbachial Drug Discovery for Treatment of Parasitic Filarial Worm Infections
by Malina A. Bakowski and Case W. McNamara
Trop. Med. Infect. Dis. 2019, 4(3), 108; https://0-doi-org.brum.beds.ac.uk/10.3390/tropicalmed4030108 - 18 Jul 2019
Cited by 20 | Viewed by 5325
Abstract
The intracellular bacteria now known as Wolbachia were first described in filarial worms in the 1970s, but the idea of Wolbachia being used as a macrofilaricidal target did not gain wide attention until the early 2000s, with research in filariae suggesting the requirement [...] Read more.
The intracellular bacteria now known as Wolbachia were first described in filarial worms in the 1970s, but the idea of Wolbachia being used as a macrofilaricidal target did not gain wide attention until the early 2000s, with research in filariae suggesting the requirement of worms for the endosymbiont. This new-found interest prompted the eventual organization of the Anti-Wolbachia Consortium (A-WOL) at the Liverpool School of Tropical Medicine, who, among others have been active in the field of antiwolbachial drug discovery to treat filarial infections. Clinical proof of concept studies using doxycycline demonstrated the utility of the antiwolbachial therapy, but efficacious treatments were of long duration and not safe for all infected. With the advance of robotics, automation, and high-speed computing, the search for superior antiwolbachials shifted away from smaller studies with a select number of antibiotics to high-throughput screening approaches, centered largely around cell-based phenotypic screens due to the rather limited knowledge about, and tools available to manipulate, this bacterium. A concomitant effort was put towards developing validation approaches and in vivo models supporting drug discovery efforts. In this review, we summarize the strategies behind and outcomes of recent large phenotypic screens published within the last 5 years, hit compound validation approaches and promising candidates with profiles superior to doxycycline, including ones positioned to advance into clinical trials for treatment of filarial worm infections. Full article
(This article belongs to the Special Issue Drug Discovery and Development for Tropical Diseases)
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18 pages, 1342 KiB  
Review
Artemisinin-Based Antimalarial Drug Therapy: Molecular Pharmacology and Evolving Resistance
by Laura E. Heller and Paul D. Roepe
Trop. Med. Infect. Dis. 2019, 4(2), 89; https://0-doi-org.brum.beds.ac.uk/10.3390/tropicalmed4020089 - 04 Jun 2019
Cited by 34 | Viewed by 6184
Abstract
The molecular pharmacology of artemisinin (ART)-based antimalarial drugs is incompletely understood. Clinically, these drugs are used in combination with longer lasting partner drugs in several different artemisinin combination therapies (ACTs). ACTs are currently the standard of care against Plasmodium falciparum malaria across much [...] Read more.
The molecular pharmacology of artemisinin (ART)-based antimalarial drugs is incompletely understood. Clinically, these drugs are used in combination with longer lasting partner drugs in several different artemisinin combination therapies (ACTs). ACTs are currently the standard of care against Plasmodium falciparum malaria across much of the world. A harbinger of emerging artemisinin resistance (ARTR), known as the delayed clearance phenotype (DCP), has been well documented in South East Asia (SEA) and is beginning to affect the efficacy of some ACTs. Though several genetic mutations have been associated with ARTR/DCP, a molecular mechanism remains elusive. This paper summarizes our current understanding of ART molecular pharmacology and hypotheses for ARTR/DCP. Full article
(This article belongs to the Special Issue Drug Discovery and Development for Tropical Diseases)
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Other

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9 pages, 402 KiB  
Perspective
Marine Microbiome as a Source of Antimalarials
by Peter J. McCarthy, Bracken F. Roberts, Abigail Carbonell, Jill Roberts, Amy E. Wright and Debopam Chakrabarti
Trop. Med. Infect. Dis. 2019, 4(3), 103; https://0-doi-org.brum.beds.ac.uk/10.3390/tropicalmed4030103 - 13 Jul 2019
Cited by 5 | Viewed by 3129
Abstract
It is important to discover novel antimalarial pharmacophores because of the widespread emergence of Plasmodium falciparum isolates resistant to the available drugs. Secondary metabolites derived from microbes associated with marine invertebrates are a valuable resource for the discovery of novel drug leads. However, [...] Read more.
It is important to discover novel antimalarial pharmacophores because of the widespread emergence of Plasmodium falciparum isolates resistant to the available drugs. Secondary metabolites derived from microbes associated with marine invertebrates are a valuable resource for the discovery of novel drug leads. However, the potential of marine microbes as a source of antimalarials has not been explored. We investigated the promise of marine microorganisms for the production of antimalarial activities by testing 2365 diverse microbial extracts using phenotypic screening of a multidrug resistant chloroquine resistant P. falciparum strain. We conducted counter screening against mammalian cells for the 317 active extracts that exhibited more than 70% inhibition at 1 µg/mL. The screen identified 17 potent bioactive leads from a broad range of taxa. Our results establish that the marine microbiome is a rich source of antiplasmodial compounds that warrants in depth exploration. Full article
(This article belongs to the Special Issue Drug Discovery and Development for Tropical Diseases)
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11 pages, 644 KiB  
Perspective
WIPO Re:Search: Catalyzing Public-Private Partnerships to Accelerate Tropical Disease Drug Discovery and Development
by Cathyryne K. Manner, Katy M. Graef and Jennifer Dent
Trop. Med. Infect. Dis. 2019, 4(1), 53; https://0-doi-org.brum.beds.ac.uk/10.3390/tropicalmed4010053 - 26 Mar 2019
Cited by 7 | Viewed by 5322
Abstract
Tropical diseases, including malaria and a group of infections termed neglected tropical diseases (NTDs), pose enormous threats to human health and wellbeing globally. In concert with efforts to broaden access to current treatments, it is also critical to expand research and development (R&D) [...] Read more.
Tropical diseases, including malaria and a group of infections termed neglected tropical diseases (NTDs), pose enormous threats to human health and wellbeing globally. In concert with efforts to broaden access to current treatments, it is also critical to expand research and development (R&D) of new drugs that address therapeutic gaps and concerns associated with existing medications, including emergence of resistance. Limited commercial incentives, particularly compared to products for diseases prevalent in high-income countries, have hindered many pharmaceutical companies from contributing their immense product development know-how and resources to tropical disease R&D. In this article we present WIPO Re:Search, an international initiative co-led by BIO Ventures for Global Health (BVGH) and the World Intellectual Property Organization (WIPO), as an innovative and impactful public-private partnership model that promotes cross-sector intellectual property sharing and R&D to accelerate tropical disease drug discovery and development. Importantly, WIPO Re:Search also drives progress toward the United Nations Sustainable Development Goals (SDGs). Through case studies, we illustrate how WIPO Re:Search empowers high-quality tropical disease drug discovery researchers from academic/non-profit organizations and small companies (including scientists in low- and middle-income countries) to leapfrog their R&D programs by accessing pharmaceutical industry resources that may not otherwise be available to them. Full article
(This article belongs to the Special Issue Drug Discovery and Development for Tropical Diseases)
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