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Predictive modeling of anti-malarial molecules inhibiting apicoplast formation
2013
BMC Bioinformatics
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Results: In the present study, we have used high-throughput screen datasets for the discovery of apicoplast inhibitors of the malarial pathogen as assayed from the delayed death response. ...
We employed machine learning approach and developed computational predictive models to predict the biological activity of new antimalarial compounds. ...
This work was funded by the Council of Scientific and Industrial Research (CSIR), India for funding through the Open Source Drug Discovery Project (HCP001). ...
doi:10.1186/1471-2105-14-55
pmid:23419172
pmcid:PMC3599641
fatcat:xvehkyac75a65ehyzauqf6mdmu
Recent advances in the biology and drug targeting of malaria parasite aminoacyl-tRNA synthetases
2016
Malaria Journal
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Escalating drug resistance in malaria parasites and lack of vaccine entails the discovery of novel drug targets and inhibitor molecules. ...
Malaria parasites contain three translational compartments: the cytoplasm, apicoplast and mitochondrion, of which the latter two are of the prokaryotic type. ...
Reported anti-malarials that target aaRSs are listed in Table 2 and key targets and their inhibition are discussed below. ...
doi:10.1186/s12936-016-1247-0
pmid:27068331
pmcid:PMC4828885
fatcat:iqtoj6idvjaa3lqash6ar7v2gu
Discovery of small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase
[article]
2022
bioRxiv
pre-print
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The apicoplast genome is replicated by a single DNA polymerase (apPOL), which is an attractive target for anti-malarial drugs. ...
We screened small-molecule libraries (206,504 compounds) using a fluorescence-based high-throughput DNA polymerase assay. ...
J Chem Inf Model. 2015 Feb 23;55(2):460-73. mechanisms of DNA polymerase inhibition or as lead compounds for further optimization into anti-malaria drugs. ...
doi:10.1101/2022.03.04.482688
fatcat:w3kpc2rf5zexxe6ebv46bheqgm
QSAR based predictive modeling for anti-malarial molecules
2017
Bioinformation
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Keywords: Malaria, apicoplast, predictive model building, R statistical package Background: Malaria is endemic in many tropical and subtropical regions causing high mortality and morbidity. ...
In the present work, we describe a standard protocol to develop molecular descriptor based predictive models (QSAR models), which can be further utilized for the screening of large chemical libraries. ...
The workflow is applied in the predictive model building of biologically active inhibitor molecules against apicoplast formation. ...
doi:10.6026/97320630013154
pmid:28690382
pmcid:PMC5498782
fatcat:5a5mq6bxu5gwfbs6aahhhht22y
The apicoplast as an antimalarial drug target
2001
Drug resistance updates
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The apicoplast contains a range of metabolic pathways and housekeeping processes that differ radically to those of the host thereby presenting ideal strategies for drug therapy. ...
The recent identification of a relict chloroplast (apicoplast) in malaria and related parasites offers numerous new targets for drug therapy using well-characterized compounds. ...
Various derivatives of quinolones and fluoroquinolones have been tested for their ability to inhibit apicoplast DNA replication and models for their mode of action proposed. 6 These findings validate ...
doi:10.1054/drup.2001.0205
pmid:11768328
fatcat:6uudlwirazgzthonmrv435mao4
Targeting apicoplasts in malaria parasites
2012
Expert opinion on therapeutic targets
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the study of anti-malarials targeting the apicoplast. ...
anti-malarials. ...
doi:10.1517/14728222.2013.739158
pmid:23231425
fatcat:y6jgr2thubc2voeq5h5rujglxi
A supervised classifier based chemoinformatics model to predict inhibitors essential for sexual reproduction and transmission of the P. falciparum parasite into mosquitoes
2019
International Journal of Advanced and Applied Sciences
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The availability of Highthroughput Screening (HTS) anti-malarial bioassay dataset has provided an opportunity to build ML-based chemoinformatics, predictive models, using features extracted from different ...
The J48 classifier based predictive model was found to accurately predict active anti-PfCDPK4 molecule based on better Accuracy, Recall, Precision, and Area under the Curve (AUC) values. ...
Compliance with ethical standards
Conflict of interest The authors declare that they have no conflict of interest. ...
doi:10.21833/ijaas.2019.10.011
fatcat:umv6qbsntfdmlefh2wjsllguc4
Plasmodial sugar transporters as anti-malarial drug targets and comparisons with other protozoa
2011
Malaria Journal
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Inhibition of cellular glucose uptake (the first step in its utilization) has, therefore, received attention as a potential therapeutic strategy to treat various unrelated diseases including malaria and ...
Plasmodium falciparum is the most dangerous human malarial parasite and its hexose transporter has been identified as being the major glucose transporter. ...
Thus, inhibition of hexose transport may present an attractive approach in the development of other new anti-parasitic drugs, in addition to the discovery of novel anti-malarials. ...
doi:10.1186/1475-2875-10-165
pmid:21676209
pmcid:PMC3135577
fatcat:scdlvwexsfbzvcrk4nelwmu3wu
A Systematic In Silico Search for Target Similarity Identifies Several Approved Drugs with Potential Activity against the Plasmodium falciparum Apicoplast
2013
PLoS ONE
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Here, we focus on the apicoplast, a malarial plastid-like organelle of algal source which evolved through secondary endosymbiosis. ...
We were able to identify several drugs that are expected to interact with forty-seven (47) peptides predicted to be involved in the biology of the P. falciparum apicoplast. ...
Acknowledgments The authors wish to thank Professor José Clecildo Barreto Bezerra for his encouragements throughout the course of this work.
Author Contributions ...
doi:10.1371/journal.pone.0059288
pmid:23555651
pmcid:PMC3608639
fatcat:6z3fdtgqrbgnjo5xb2hbfuclie
DNA organization by the apicoplast-targeted bacterial histone-like protein of Plasmodium falciparum
2008
Nucleic Acids Research
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In contrast to bacterial HUs that bend DNA, PfHU promotes concatenation of linear DNA and inhibits DNA circularization. ...
Atomic Force Microscopic study of PfHU-DNA complexes shows protein concentration-dependent DNA stiffening, intermolecular bundling and formation of DNA bridges followed by assembly of condensed DNA networks ...
E.V.S.R.R. and R.N. are recipients of research fellowships from the Council of Scientific and Industrial Research and Department of Biotechnology, respectively. This is CDRI communication no. 7456. ...
doi:10.1093/nar/gkn483
pmid:18663012
pmcid:PMC2528193
fatcat:ppq3fscaknf47guypum4xdttui
Plasmodium falciparum: multifaceted resistance to artemisinins
2016
Malaria Journal
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Plasmodium falciparum resistance to artemisinins, the most potent and fastest acting anti-malarials, threatens malaria elimination strategies. ...
response, the PI3K/PI3P/AKT pathway, the PfPK4/eIF2α cascade and yet unidentified transcription factor(s), with minimal energetic requirements and fatty acid metabolism maintained in the mitochondrion and apicoplast ...
supported in part by the French Agence Nationale de la Recherche (Grant ANR-13-BSV3-0018-01) and by the French Government programme Investissement d' Avenir, Laboratoire d'Excellence "Integrative Biology of ...
doi:10.1186/s12936-016-1206-9
pmid:26955948
pmcid:PMC4784301
fatcat:jlnqc2eqx5fpdpotftlhbegmmu
The Clp Chaperones and Proteases of the Human Malaria Parasite Plasmodium falciparum
2010
Journal of Molecular Biology
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Our data suggest the presence of a ClpCRP complex in the apicoplast of P. falciparum. ...
The proteins were localized to the apicoplast, a non-photosynthetic organelle that accommodates several important metabolic pathways in P. falciparum, with the exception of PfClpB2 (also known as Hsp101 ...
Hence, targeting the activity of this complex might be a promising approach for the development of anti-malarial drugs as was recently suggested. 3 3 Dysregulation 3 4 or selective inhibition 35 of ...
doi:10.1016/j.jmb.2010.09.051
pmid:20887733
fatcat:p2yxxunzgvctpkxujey4dqg5i4
Selected Derivatives of Erythromycin B-In Silico and Anti-Malarial Studies
2021
Materials
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segment from the exit tunnel from the apicoplast of P. falciparum is the reason for their weak in vitro anti-malarial activities. ...
These compounds were investigated for their anti-malarial activities, by their in silico molecular docking into segments of the exit tunnel of the apicoplast ribosome from Plasmodium falciparum. ...
Molecular docking can also be a good tool for the prediction of anti-malarial activity of derivatives with previously undetermined anti-malarial activity. ...
doi:10.3390/ma14226980
pmid:34832380
pmcid:PMC8618316
fatcat:j4qbeahuqbhv3manejfhmyf5pi
The primase domain of PfPrex is a proteolytically matured, essential enzyme of the apicoplast
2011
Molecular and biochemical parasitology (Print)
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Taken together, these observations strongly suggest an essential role of PfPrex primase in the production of RNA primers for lagging strand DNA synthesis of the apicoplast genome. ...
Finally, overexpression in P. falciparum of PfPrex's trafficking and primase sequences yielded specific and dynamic localization to foci within the apicoplast. ...
McFadden for providing the anti-PfACP antibody, and J. Berger for purified recombinant EcDnaG. We also thank the Keck and Kappe labs for critical discussion of this work. ...
doi:10.1016/j.molbiopara.2011.08.002
pmid:21856338
pmcid:PMC3196721
fatcat:xpy35kcjmjeshhmey22ctumc7e
Homology Modeling And Docking Study Of Shewanella Like Protein Phosphatase Involved In Development Of Ookinetes In Plasmodium
[article]
2018
bioRxiv
pre-print
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SHLP deletion results in a reduction in microneme formation, ookinetes (zygote) development and complete ablation of oocyst formation, thereby blocking transmission of parasite. ...
Structure Modeling of SHLP protein can be helpful in understanding the active site and binding site information and hence can be used for drug designing for therapeutics against malaria. ...
An antioxidant is a molecule that inhibits the oxidation of other molecules [19] . ...
doi:10.1101/297770
fatcat:srw2gdyivjgqnbiryxyj3wmqwa
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