ArticleProceedings of the National Academy of Sciences of the United States of America2021
Design of proteasome inhibitors with oral efficacy in vivo against
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Article in Proceedings of the National Academy of Sciences of the United States of America, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers.
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0cells of the map it votes in
24citing papers in PubMed
2.2field-weighted citation impact, top 11% of its field
What it found
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
24 citing papers in PubMed, 35 citations in OpenAlex.
- Structure-Activity Relationship Study of Antimalarial Asparagine-Derived Proteasome Inhibitors.ACS omega · 2026Article
- Trichomonas vaginalis Drug Targets and Their Role in Drug Discovery and Development.Pharmaceutical research · 2026Review
- Boosting ribosomal translationBioactive materials · 2026Article
- YAT2150 is irresistible in Plasmodium falciparum and active against Plasmodium vivax and Leishmania clinical isolates.Scientific reports · 2025Article
- Structural comparison of human and Plasmodium proteasome β5 subunits: informing selective inhibitor design for anti-malaria agents.Malaria journal · 2025Article
- Trends on Potential Boron-containing Drugs by Advancements in Ligand-protein Crystals Complexes.Current medicinal chemistry · 2025Review
- Identification of potent and reversible piperidine carboxamides that are species-selective orally active proteasome inhibitors to treat malaria.Cell chemical biology · 2024Article
- Peptidic Boronic AcidJournal of medicinal chemistry · 2024Article
- Transmission-Blocking Strategies for Malaria Eradication: Recent Advances in Small-Molecule Drug Development.Pharmaceuticals (Basel, Switzerland) · 2024Review
- Antiplasmodial potential of phytochemicals from Citrus aurantifolia peels: a comprehensive in vitro and in silico study.BMC chemistry · 2024Article
- Deaggregation of mutant Plasmodium yoelii de-ubiquitinase UBP1 alters MDR1 localization to confer multidrug resistance.Nature communications · 2024Article
- The proteasome as a drug target for treatment of parasitic diseases.Advances in parasitology · 2024Review
- Structures revealing mechanisms of resistance and collateral sensitivity of Plasmodium falciparum to proteasome inhibitors.Nature communications · 2023Article
- Covalent Macrocyclic Proteasome Inhibitors Mitigate Resistance inACS infectious diseases · 2023Article
- Covalent Inhibitors for Neglected Diseases: An Exploration of Novel Therapeutic Options.Pharmaceuticals (Basel, Switzerland) · 2023Review
- Mitigating the risk of antimalarial resistance via covalent dual-subunit inhibition of the Plasmodium proteasome.Cell chemical biology · 2023Article
- Dual-pharmacophore artezomibs hijack the Plasmodium ubiquitin-proteasome system to kill malaria parasites while overcoming drug resistance.Cell chemical biology · 2023Article
- Development of Potent and Highly Selective Epoxyketone-Based Plasmodium Proteasome Inhibitors.Chemistry (Weinheim an der Bergstrasse, Germany) · 2023Article
- Structure-Activity Relationship Studies of AntimalarialJournal of medicinal chemistry · 2023Article
- New targets for antimalarial drug discovery.Current opinion in microbiology · 2022Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
40 authors at 10 institutions in 5 countries.
Stanley C XieDepartment of Biochemistry and Pharmacology, Bio21 Molecular Science and Biotechnology Institute, The University of Melbourne, Melbourne, VIC 3010, Australia.ORCID 0000-0001-7003-4677
Riley D MetcalfeDepartment of Biochemistry and Pharmacology, Bio21 Molecular Science and Biotechnology Institute, The University of Melbourne, Melbourne, VIC 3010, Australia.ORCID 0000-0002-7154-780X
Hirotake MizutaniDiscovery Strategy and Operations, Takeda Pharmaceuticals International Co., Cambridge, MA 02139.ORCID 0000-0003-3320-9655
Tanya PuhalovichDepartment of Biochemistry and Pharmacology, Bio21 Molecular Science and Biotechnology Institute, The University of Melbourne, Melbourne, VIC 3010, Australia.
Eric HanssenDepartment of Biochemistry and Pharmacology, Bio21 Molecular Science and Biotechnology Institute, The University of Melbourne, Melbourne, VIC 3010, Australia.ORCID 0000-0002-4064-1844
Craig J MortonDepartment of Biochemistry and Pharmacology, Bio21 Molecular Science and Biotechnology Institute, The University of Melbourne, Melbourne, VIC 3010, Australia.ORCID 0000-0001-5452-5193
Yawei DuDepartment of Biochemistry and Pharmacology, Bio21 Molecular Science and Biotechnology Institute, The University of Melbourne, Melbourne, VIC 3010, Australia.ORCID 0000-0002-0829-1901
Con DogovskiDepartment of Biochemistry and Pharmacology, Bio21 Molecular Science and Biotechnology Institute, The University of Melbourne, Melbourne, VIC 3010, Australia.
Shih-Chung HuangDiscovery Strategy and Operations, Takeda Pharmaceuticals International Co., Cambridge, MA 02139.ORCID 0000-0001-8510-4850
Jeffrey CiavarriDiscovery Strategy and Operations, Takeda Pharmaceuticals International Co., Cambridge, MA 02139.ORCID 0000-0001-6837-8841
Paul HalesDiscovery Strategy and Operations, Takeda Pharmaceuticals International Co., Cambridge, MA 02139.ORCID 0000-0002-1010-5995
Robert J GriffinDiscovery Strategy and Operations, Takeda Pharmaceuticals International Co., Cambridge, MA 02139.ORCID 0000-0002-1907-2421
Lawrence H CohenDiscovery Strategy and Operations, Takeda Pharmaceuticals International Co., Cambridge, MA 02139.ORCID 0000-0002-9255-0119
Bei-Ching ChuangDiscovery Strategy and Operations, Takeda Pharmaceuticals International Co., Cambridge, MA 02139.
Sergio WittlinDepartment of Medical Parasitology and Infection Biology, Swiss Tropical and Public Health Institute, 4051 Basel, Switzerland.
Ioanna DeniDepartment of Microbiology & Immunology, Columbia University Irving Medical Center, New York, NY 10032.ORCID 0000-0002-5266-8243
Tomas YeoDepartment of Microbiology & Immunology, Columbia University Irving Medical Center, New York, NY 10032.ORCID 0000-0003-2923-6060
Kurt E WardDepartment of Microbiology & Immunology, Columbia University Irving Medical Center, New York, NY 10032.ORCID 0000-0002-3614-436X
Daniel C BarryDepartment of Biochemistry and Pharmacology, Bio21 Molecular Science and Biotechnology Institute, The University of Melbourne, Melbourne, VIC 3010, Australia.ORCID 0000-0001-5288-8863
Boyin LiuDepartment of Biochemistry and Pharmacology, Bio21 Molecular Science and Biotechnology Institute, The University of Melbourne, Melbourne, VIC 3010, Australia.
David L GillettDepartment of Biochemistry and Pharmacology, Bio21 Molecular Science and Biotechnology Institute, The University of Melbourne, Melbourne, VIC 3010, Australia.ORCID 0000-0002-1239-6888
Benigno F Crespo-FernandezGlobal Health Pharma Research Unit, GSK, 28760 Madrid, Spain.ORCID 0000-0002-5071-5819
Sabine OttilieDepartment of Pediatrics, School of Medicine, University of California San Diego, La Jolla, CA 92093.ORCID 0000-0001-9797-2612
Nimisha MittalDepartment of Pediatrics, School of Medicine, University of California San Diego, La Jolla, CA 92093.
Alisje ChurchyardDepartment of Life Sciences, Imperial College London, London SW7 2AZ, United Kingdom.
Daniel FergusonDepartment of Biology and South Texas Center for Emerging Infectious Diseases, University of Texas at San Antonio, San Antonio, TX 78249.ORCID 0000-0002-9124-7185
Anna Caroline C AguiarSão Carlos Institute of Physics, University of São Paulo, São Carlos 13563-120, Brazil.ORCID 0000-0003-0139-8279
Rafael V C GuidoSão Carlos Institute of Physics, University of São Paulo, São Carlos 13563-120, Brazil.ORCID 0000-0002-7187-0818
Jake BaumDepartment of Life Sciences, Imperial College London, London SW7 2AZ, United Kingdom.ORCID 0000-0002-0275-352X
Kirsten K HansonDepartment of Biology and South Texas Center for Emerging Infectious Diseases, University of Texas at San Antonio, San Antonio, TX 78249.ORCID 0000-0002-0154-0979
Elizabeth A WinzelerDepartment of Pediatrics, School of Medicine, University of California San Diego, La Jolla, CA 92093.ORCID 0000-0002-4049-2113
Francisco-Javier GamoGlobal Health Pharma Research Unit, GSK, 28760 Madrid, Spain.ORCID 0000-0002-1854-2882
David A FidockDepartment of Microbiology & Immunology, Columbia University Irving Medical Center, New York, NY 10032.ORCID 0000-0001-6753-8938
Delphine BaudDrug Discovery, Medicines for Malaria Venture, 1215 Geneva 15, Switzerland.
Michael W ParkerDepartment of Biochemistry and Pharmacology, Bio21 Molecular Science and Biotechnology Institute, The University of Melbourne, Melbourne, VIC 3010, Australia.ORCID 0000-0002-3101-1138
Stephen BrandDrug Discovery, Medicines for Malaria Venture, 1215 Geneva 15, Switzerland.ORCID 0000-0002-7010-5348
Lawrence R DickDepartment of Biochemistry and Pharmacology, Bio21 Molecular Science and Biotechnology Institute, The University of Melbourne, Melbourne, VIC 3010, Australia.ORCID 0000-0002-6880-0405
Michael D W GriffinDepartment of Biochemistry and Pharmacology, Bio21 Molecular Science and Biotechnology Institute, The University of Melbourne, Melbourne, VIC 3010, Australia.ORCID 0000-0001-9845-7735
Alexandra E GouldDiscovery Strategy and Operations, Takeda Pharmaceuticals International Co., Cambridge, MA 02139; ltilley@unimelb.edu.au sandy.gould@takeda.com.ORCID 0000-0002-1657-5891
Leann TilleyDepartment of Biochemistry and Pharmacology, Bio21 Molecular Science and Biotechnology Institute, The University of Melbourne, Melbourne, VIC 3010, Australia; ltilley@unimelb.edu.au sandy.gould@takeda.com.ORCID 0000-0001-9910-0199
The University of Melbourne · AUTakeda (United States) · USColumbia University Irving Medical Center · USUniversity of California San Diego · USImperial College London · GBMedicines for Malaria Venture · CHTexas Center for Infectious Disease · USUniversidade Federal de São Carlos · BRBiotechnology Institute · USSwiss Tropical and Public Health Institute · CH
Funding
Discovery of long-acting, chemoprotective antimalarial compoundsR01AI152533 · NIAID · UNIVERSITY OF CALIFORNIA, SAN DIEGO · PI WINZELER, ELIZABETH A · 2020 to 2024
$3.5MParasite-specific proteasome inhibitors to combat multi-drug resistant malariaR33AI127581 · NIAID · STANFORD UNIVERSITY · PI BOGYO, MATTHEW · 2019 to 2021
$1.4MNIAID NIH HHS R01 AI152533NIAID NIH HHS R33 AI127581Wellcome Trust
Abstract
The
Indexed as
Administration, OralAnimalsBoron CompoundsCatalytic DomainHumansMalaria, FalciparumMiceMice, Inbred NODMice, SCIDModels, MolecularPlasmodium falciparumProteasome Endopeptidase ComplexProteasome InhibitorsBoron CompoundsProteasome Endopeptidase ComplexProteasome Inhibitorsantimalarial drugcryo-EMpeptide boronatePlasmodiumproteasome
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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.