ArticleScience translational medicine2022
The anticancer human mTOR inhibitor sapanisertib potently inhibits multiple
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Article in Science translational medicine, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers.
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25citing papers in PubMed
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25 citing papers in PubMed, 42 citations in OpenAlex.
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- Using Unbiased Chemical Proteomics Approaches to Explore the Target Landscape of the Resistance Refractory 7-Azaindole MMV022224 inACS infectious diseases · 2026Article
- Repurposing Drugs for Malaria through a Human Dose Prediction: A Case Study with Berzosertib.Clinical pharmacology and therapeutics · 2026Article
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- Repositioning a Human Kinase Platelet-Derived Growth Factor Receptor Alpha Type II Inhibitor for Malaria and Inhibition of Hemozoin Formation.ACS medicinal chemistry letters · 2026Article
- PI3K/AKT signaling in parasites and parasite diseases: Role and therapeutic potential.Virulence · 2025Review
- Optimization of 2,8-Diaryl-1,5-naphthyridines asJournal of medicinal chemistry · 2025Article
- Novel Inhibitors ofJournal of medicinal chemistry · 2025Article
- The ATM Kinase Inhibitor AZD0156 Is a Potent Inhibitor of Plasmodium Phosphatidylinositol 4-Kinase (PI4Kβ) and Is an Attractive Candidate for Medicinal Chemistry Optimization Against Malaria.Angewandte Chemie (International ed. in English) · 2025Article
- Medicinal Chemistry Progression of Sapanisertib, the Anticancer and DualJournal of medicinal chemistry · 2025Article
- PI3-kinase has multiple functions in asexual blood stages of Plasmodium falciparum.Scientific reports · 2025Article
- Towards next-generation treatment options to combat Plasmodium falciparum malaria.Nature reviews. Microbiology · 2025Review
- Establishment and application of a zebrafish model of Werner syndrome identifies sapanisertib as a potential antiaging drug.Proceedings of the National Academy of Sciences of the United States of America · 2025Article
- The Tuberculosis Drug Candidate SQ109 and Its Analogs Have Multistage Activity againstACS infectious diseases · 2024Article
- Heme oxygenase 1-mediated ferroptosis in Kupffer cells initiates liver injury during heat stroke.Acta pharmaceutica Sinica. B · 2024Article
- Transmission-Blocking Strategies for Malaria Eradication: Recent Advances in Small-Molecule Drug Development.Pharmaceuticals (Basel, Switzerland) · 2024Review
- 2,8-Disubstituted-1,5-naphthyridines as Dual Inhibitors ofJournal of medicinal chemistry · 2024Article
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Authors and funding
30 authors at 10 institutions in 5 countries.
Lauren B ArendseDrug Discovery and Development Centre (H3D), University of Cape Town, Rondebosch, Cape Town 7701, South Africa.ORCID 0000-0003-4699-0428
James M MurithiDepartment of Microbiology and Immunology, Columbia University Irving Medical Center, New York, NY 10032, USA.ORCID 0000-0003-0741-8461
Tarrick QahashDepartment of Biochemistry and Molecular Biology, Pennsylvania State University, University Park, PA 16802, USA.ORCID 0000-0003-2891-3090
Charisse Flerida A PasajeDepartment of Biological Engineering, Massachusetts Institute of Technology, Cambridge, MA 02139, USA.ORCID 0000-0002-9780-3680
Luiz C GodoyDepartment of Biological Engineering, Massachusetts Institute of Technology, Cambridge, MA 02139, USA.
Sumanta DeyDepartment of Biological Engineering, Massachusetts Institute of Technology, Cambridge, MA 02139, USA.ORCID 0000-0002-5945-976X
Liezl GibhardDrug Discovery and Development Centre (H3D), University of Cape Town, Rondebosch, Cape Town 7701, South Africa.
Sonja Ghidelli-DisseCellzome GmbH, a GSK Company, Heidelberg 69117, Germany.ORCID 0000-0002-7735-9746
Gerard DrewesCellzome GmbH, a GSK Company, Heidelberg 69117, Germany.ORCID 0000-0003-0575-6766
Marcus BantscheffCellzome GmbH, a GSK Company, Heidelberg 69117, Germany.ORCID 0000-0002-8343-8977
Maria J Lafuente-MonasterioTres Cantos Medicines Development Campus-Diseases of the Developing World, GlaxoSmithKline, Tres Cantos, Madrid 28760, Spain.ORCID 0000-0002-4583-9649
Stephen FienbergDrug Discovery and Development Centre (H3D), University of Cape Town, Rondebosch, Cape Town 7701, South Africa.ORCID 0000-0002-6228-6783
Lynn WambuaInstitute of Infectious Disease and Molecular Medicine, University of Cape Town, Observatory, Cape Town 7925, South Africa.ORCID 0000-0002-6218-199X
Samuel GachuhiDepartment of Chemistry, University of Cape Town, Rondebosch, Cape Town 7701, South Africa.ORCID 0000-0002-3907-5179
Dina CoertzenDepartment of Biochemistry, Genetics and Microbiology, Institute for Sustainable Malaria Control, University of Pretoria, Hatfield 0028, South Africa.ORCID 0000-0002-8408-244X
Mariëtte van der WattDepartment of Biochemistry, Genetics and Microbiology, Institute for Sustainable Malaria Control, University of Pretoria, Hatfield 0028, South Africa.ORCID 0000-0002-9933-8647
Janette ReaderDepartment of Biochemistry, Genetics and Microbiology, Institute for Sustainable Malaria Control, University of Pretoria, Hatfield 0028, South Africa.ORCID 0000-0001-9026-0583
Ayesha S AswatWits Research Institute for Malaria, School of Pathology, Faculty of Health Sciences, University of the Witwatersrand, Johannesburg 2193, South Africa.ORCID 0000-0002-5326-6764
Erica ErlankWits Research Institute for Malaria, School of Pathology, Faculty of Health Sciences, University of the Witwatersrand, Johannesburg 2193, South Africa.ORCID 0000-0002-9687-6095
Nelius VenterWits Research Institute for Malaria, School of Pathology, Faculty of Health Sciences, University of the Witwatersrand, Johannesburg 2193, South Africa.
Nimisha MittalSchool of Medicine, University of California, San Diego, La Jolla, CA 92093, USA.ORCID 0000-0002-4810-9334
Madeline R LuthSchool of Medicine, University of California, San Diego, La Jolla, CA 92093, USA.ORCID 0000-0001-9059-1200
Sabine OttilieSchool of Medicine, University of California, San Diego, La Jolla, CA 92093, USA.ORCID 0000-0001-9797-2612
Elizabeth A WinzelerSchool of Medicine, University of California, San Diego, La Jolla, CA 92093, USA.
Lizette L KoekemoerWits Research Institute for Malaria, School of Pathology, Faculty of Health Sciences, University of the Witwatersrand, Johannesburg 2193, South Africa.ORCID 0000-0003-4236-6345
Lyn-Marie BirkholtzDepartment of Biochemistry, Genetics and Microbiology, Institute for Sustainable Malaria Control, University of Pretoria, Hatfield 0028, South Africa.ORCID 0000-0001-5888-2905
Jacquin C NilesDepartment of Biological Engineering, Massachusetts Institute of Technology, Cambridge, MA 02139, USA.ORCID 0000-0002-6250-8796
Manuel LlinásDepartment of Biochemistry and Molecular Biology, Pennsylvania State University, University Park, PA 16802, USA.ORCID 0000-0002-6173-5882
David A FidockDepartment of Microbiology and Immunology, Columbia University Irving Medical Center, New York, NY 10032, USA.ORCID 0000-0001-6753-8938
Kelly ChibaleDrug Discovery and Development Centre (H3D), University of Cape Town, Rondebosch, Cape Town 7701, South Africa.ORCID 0000-0002-4541-646X
Massachusetts Institute of Technology · USNational Health Laboratory Service · ZAUniversity of California San Diego · USUniversity of Cape Town · ZAUniversity of Pretoria · ZAHeidelberg Engineering (Germany) · DEColumbia University Irving Medical Center · USPennsylvania State University · USSouth African Medical Research Council · ZAGlaxoSmithKline (France) · FR
Funding
Training Program in Basic Clinical GeneticsT32GM008666 · NIGMS · UNIVERSITY OF CALIFORNIA, SAN DIEGO · PI HAMILTON, BRUCE A · 1998 to 2021
$8.6MNIGMS NIH HHS T32 GM008666
Abstract
Compounds acting on multiple targets are critical to combating antimalarial drug resistance. Here, we report that the human "mammalian target of rapamycin" (mTOR) inhibitor sapanisertib has potent prophylactic liver stage activity, in vitro and in vivo asexual blood stage (ABS) activity, and transmission-blocking activity against the protozoan parasite
Indexed as
AntimalarialsPlasmodium1-Phosphatidylinositol 4-KinaseAdenineAnimalsBenzoxazolesGuanosine MonophosphateHumansLife Cycle StagesMammalsMTOR InhibitorsPlasmodium falciparumSirolimusTOR Serine-Threonine Kinases1-Phosphatidylinositol 4-KinaseAdenineAntimalarialsBenzoxazolesGuanosine MonophosphateMTOR InhibitorsMTOR protein, humansapanisertibSirolimusTOR Serine-Threonine Kinases
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.