Evaluation of the European Foundation Initiative into African Research in Neglected Tropical Diseases by the African Fellows

O’Neill, Hester G.; Mzilahowa, Themba; Deus, Nilsa de; Njenga, Sammy M.; Mmbaga, Elia John; Kariuki, Thomas

doi:10.1371/journal.pntd.0002019

Cited by 2 publications

(2 citation statements)

References 21 publications

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“…EFINTD has strengthened research capacity in NTDs by empowering young African researchers who are based in their home countries to perform research on various NTDs [131] and has created the African Network for NTDs (ARNTD).…”

Section: Main Textmentioning

confidence: 99%

The cross-cutting contribution of the end of neglected tropical diseases to the sustainable development goals

et al. 2017

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The Sustainable Development Goals (SDGs) call for an integrated response, the kind that has defined Neglected Tropical Diseases (NTDs) efforts in the past decade.NTD interventions have the greatest relevance for SDG3, the health goal, where the focus on equity, and its commitment to reaching people in need of health services, wherever they may live and whatever their circumstances, is fundamentally aligned with the target of Universal Health Coverage. NTD interventions, however, also affect and are affected by many of the other development areas covered under the 2030 Agenda. Strategies such as mass drug administration or the programmatic integration of NTD and WASH activities (SDG6) are driven by effective global partnerships (SDG17). Intervention against the NTDs can also have an impact on poverty (SDG1) and hunger (SDG2), can improve education (SDG4), work and economic growth (SDG8), thereby reducing inequalities (SDG10). The community-led distribution of donated medicines to more than 1 billion people reinforces women’s empowerment (SDG5), logistics infrastructure (SDG9) and non-discrimination against disability (SDG16). Interventions to curb mosquito-borne NTDs contribute to the goals of urban sustainability (SDG11) and resilience to climate change (SDG13), while the safe use of insecticides supports the goal of sustainable ecosystems (SDG15). Although indirectly, interventions to control water- and animal-related NTDs can facilitate the goals of small-scale fishing (SDG14) and sustainable hydroelectricity and biofuels (SDG7).NTDs proliferate in less developed areas in countries across the income spectrum, areas where large numbers of people have little or no access to adequate health care, clean water, sanitation, housing, education, transport and information. This scoping review assesses how in this context, ending the epidemic of the NTDs can impact and improve our prospects of attaining the SDGs.Electronic supplementary materialThe online version of this article (doi:10.1186/s40249-017-0288-0) contains supplementary material, which is available to authorized users.

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Section: Main Textmentioning

confidence: 99%

The cross-cutting contribution of the end of neglected tropical diseases to the sustainable development goals

et al. 2017

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“…Proteases have been identified as eligible and interesting targets and gathered global funding to address HIV/ AIDS, opening the gate to the same family enzymes for malaria and tuberculosis [4]. Further, comparative studies initiative has been carried out to get insight into S2' pocket fitting at Pf and HIV aspartic proteases' active sites for inhibition with compounds such as KNI -10006 containing a norstatine core [5].…”

Section: Introductionmentioning

confidence: 99%

Insight into binding mode of nitrile inhibitors of Plasmodium falciparum Falcipain-3, QSAR and Pharmacophore models, virtual design of new analogues with favorable pharmacokinetic profiles

Esmel¹,

Keita²,

Megnassan³

et al. 2017

SDRP-JCCMM

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We have carried out computational optimization of antiparasitic azadipeptide nitrile inhibitors (AZN) of falcipain-3 (FP3) of Plasmodium falciparum (Pf), a cysteine protease of the papain superfamily, using structurebased drug design and computer-assisted combinatorial chemistry. Three-dimensional (3D) models of complexes of inhibitor -FP3 for a training sets of published AZN analogs with experimentally determined inhibitory potencies were prepared by in situ modification of the crystal structure of PfFP3 inhibited by K11017 (Protein Data Bank entry 3BWK). We have used molecular mechanics, conformational searching and implicit solvation model to compute Gibbs free energies of inhibitor -FP3 receptor complex formation and built quantitative structure-activity relationships (QSAR) model by correlating the experimental inhibitory potencies with the computed binding affinities. The model was able to explain 97% of the FP3 inhibition data variation and was further validated with help of 3D-QSAR pharmacophore model generation (PH4). Structural information obtained from the 3D models of the AZN -FP3 complexes and the PH4 guided us in designing virtual combinatorial libraries of novel AZN analogs. Comparative analysis of the active site interactions directed us in the selection of building blocks used in the libraries. The initial virtual library was focused by means of computationally predicted oral bioavailability and subsequently in silico screened with the PH4 pharmacophore models to identify new AZN inhibitor candidates. Their inhibitory activities predicted by the QSAR model fall into the low nanomolar concentration range.

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Evaluation of the European Foundation Initiative into African Research in Neglected Tropical Diseases by the African Fellows

Cited by 2 publications

References 21 publications

The cross-cutting contribution of the end of neglected tropical diseases to the sustainable development goals

The cross-cutting contribution of the end of neglected tropical diseases to the sustainable development goals

Insight into binding mode of nitrile inhibitors of Plasmodium falciparum Falcipain-3, QSAR and Pharmacophore models, virtual design of new analogues with favorable pharmacokinetic profiles

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