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Identification via a Parallel Hit Progression Strategy of Improved Small Molecule Inhibitors of the Malaria Purine Uptake Transporter that Inhibit Plasmodium falciparum Parasite Proliferation

Autor: Widdowson Katherine L, Lorena A. Kallal, Yvett Sosa, Matthew S. Steiginga, Michael T. Ouellette, Myles H. Akabas, I. J. Frame, Andrew J. Pope, Roman Deniskin, Todd L. Graybill, Deepak Bandyopadhyay, Robert J. Young

Publikováno v: ACS Infectious Diseases. 5:1738-1753

Emerging resistance to current antimalarial medicines underscores the importance of identifying new drug targets and novel compounds. Malaria parasites are purine auxotrophic and import purines via the Plasmodium falciparum equilibrative nucleoside t

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::19f40902415475df50da84cc0ab7b2af
https://doi.org/10.1021/acsinfecdis.9b00168

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Identification via a Parallel Hit Progression Strategy of Improved Small Molecule Inhibitors of the Malaria Purine Uptake Transporter that Inhibit

Autor: Yvett, Sosa, Roman, Deniskin, I J, Frame, Matthew S, Steiginga, Deepak, Bandyopadhyay, Todd L, Graybill, Lorena A, Kallal, Michael T, Ouellette, Andrew J, Pope, Katherine L, Widdowson, Robert J, Young, Myles H, Akabas

Publikováno v: ACS Infect Dis

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::62c102406f489238db600f20b212aa91
https://pubmed.ncbi.nlm.nih.gov/31373203

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Targeting the Plasmodium vivax equilibrative nucleoside transporter 1 (PvENT1) for antimalarial drug development

Autor: I. J. Frame, Myles H. Akabas, Yvett Sosa, Roman Deniskin

Publikováno v: International Journal for Parasitology: Drugs and Drug Resistance, Vol 6, Iss 1, Pp 1-11 (2016)
International Journal for Parasitology: Drugs and Drug Resistance

Infection with Plasmodium falciparum and vivax cause most cases of malaria. Emerging resistance to current antimalarial medications makes new drug development imperative. Ideally a new antimalarial drug should treat both falciparum and vivax malaria.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7d369a70028fd3fb4d411b54bb547d0d
https://doi.org/10.1016/j.ijpddr.2015.11.003

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Yeast-Based High-Throughput Screen Identifies Plasmodium falciparum Equilibrative Nucleoside Transporter 1 Inhibitors That Kill Malaria Parasites

Autor: Ian M. Willis, Roman Deniskin, Olivia Coburn-Flynn, Myles H. Akabas, Robyn D. Moir, Alison Rinderspacher, David A. Fidock, I. J. Frame, Francine Katz, Sophie H. Adjalley, Donald W. Landry, Shi Xian Deng

Publikováno v: ACS Chemical Biology. 10:775-783

Equilibrative transporters are potential drug targets; however, most functional assays involve radioactive substrate uptake that is unsuitable for high-throughput screens (HTS). We developed a robust yeast-based growth assay that is potentially appli

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d1942696c19fce59752e93741c938eba
https://doi.org/10.1021/cb500981y

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UV-triggered Affinity Capture Identifies Interactions between the Plasmodium falciparum Multidrug Resistance Protein 1 (PfMDR1) and Antimalarial Agents in Live Parasitized Cells

Publikováno v: Journal of Biological Chemistry. 288:22576-22583

A representative of a new class of potent antimalarials with an unknown mode of action was recently described. To identify the molecular target of this class of antimalarials, we employed a photo-reactive affinity capture method to find parasite prot

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6ae6dab21838e58d1322f5002cde6596
https://doi.org/10.1074/jbc.m113.453159

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Malaria parasite type 4 equilibrative nucleoside transporters (ENT4) are purine transporters with distinct substrate specificity

Autor: Myles H. Akabas, I. J. Frame, Maria B. Cassera, Emilio F. Merino, Vern L. Schramm

Publikováno v: Biochemical Journal. 446:179-190

Malaria, caused by Plasmodia parasites, affects hundreds of millions of people. As purine auxotrophs, Plasmodia use transporters to import host purines for subsequent metabolism by the purine salvage pathway. Thus purine transporters are attractive d

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8d437031fef84a44699e2f6ff6f412ec
https://doi.org/10.1042/bj20112220

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Transmembrane Segment 11 Appears to Line the Purine Permeation Pathway of the Plasmodium falciparum Equilibrative Nucleoside Transporter 1 (PfENT1)

Autor: I. J. Frame, Paul M. Riegelhaupt, Myles H. Akabas

Publikováno v: Journal of Biological Chemistry. 285:17001-17010

Purine transport is essential for malaria parasites to grow because they lack the enzymes necessary for de novo purine biosynthesis. The Plasmodium falciparum Equilibrative Nucleoside Transporter 1 (PfENT1) is a member of the equilibrative nucleoside

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4b011582f1e810064f44e1ac496b25bd
https://doi.org/10.1074/jbc.m110.115758

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Purine import into malaria parasites as a target for antimalarial drug development

Autor: I J, Frame, Roman, Deniskin, Avish, Arora, Myles H, Akabas

Publikováno v: Annals of the New York Academy of Sciences. 1342

Infection with Plasmodium species parasites causes malaria. Plasmodium parasites are purine auxotrophs. In all life cycle stages, they require purines for RNA and DNA synthesis and other cellular metabolic processes. Purines are imported from the hos

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::9d65dab304ae0bb7e54aee42a2247595
https://pubmed.ncbi.nlm.nih.gov/25424653

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