ArticleJournal of medicinal chemistry2021
Scaffold-Hopping Strategy on a Series of Proteasome Inhibitors Led to a Preclinical Candidate for the Treatment of Visceral Leishmaniasis.
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Article in Journal of medicinal chemistry, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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18citing papers in PubMed
6.3field-weighted citation impact, top 3% of its field
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Who cites it
18 citing papers in PubMed, 38 citations in OpenAlex.
- Safety and pharmacokinetics of GSK3494245, a highly selective Leishmaniasis kinetoplastid proteasome inhibitor for the treatment of visceral leishmaniasis: A Phase 1, randomized, single ascending dose escalation study in healthy participants.PLoS neglected tropical diseases · 2026Trial
- Optimization of Species-Selective Reversible Proteasome Inhibitors for the Treatment of Malaria.Journal of medicinal chemistry · 2025Article
- Applications of Bridgehead Heterocycles in Drug Design and Medicinal Chemistry.Topics in current chemistry (Cham) · 2025Review
- Uncovering the Mechanism of Action of Antiprotozoal Agents: A Survey on Photoaffinity Labeling Strategy.Pharmaceuticals (Basel, Switzerland) · 2024Review
- Discovery of a Series of Macrocycles as Potent Inhibitors ofJournal of medicinal chemistry · 2024Article
- Identification of Novel Flavonoids and Ansa-Macrolides with Activities againstPathogens (Basel, Switzerland) · 2024Article
- 4-Aminoquinoline as a privileged scaffold for the design of leishmanicidal agents: structure-property relationships and key biological targets.Frontiers in chemistry · 2024Review
- Structures revealing mechanisms of resistance and collateral sensitivity of Plasmodium falciparum to proteasome inhibitors.Nature communications · 2023Article
- Structure-Guided Design and Synthesis of a Pyridazinone Series ofJournal of medicinal chemistry · 2023Article
- Article
- Compound 275# Induces Mitochondria-Mediated Apoptosis and Autophagy Initiation in Colorectal Cancer Cells through an Accumulation of Intracellular ROS.Molecules (Basel, Switzerland) · 2023Article
- Design of Cytochrome P450 1B1 InhibitorsJournal of medicinal chemistry · 2023Article
- Current leishmaniasis drug discovery.RSC medicinal chemistry · 2022Review
- Design, Synthesis, and Optimization of Macrocyclic Peptides as Species-Selective Antimalaria Proteasome Inhibitors.Journal of medicinal chemistry · 2022Article
- Transcriptome-Wide Identification of Coding and Noncoding RNA-Binding Proteins Defines the Comprehensive RNA Interactome of Leishmania mexicana.Microbiology spectrum · 2022Article
- Identification of a Proteasome-Targeting Arylsulfonamide with Potential for the Treatment of Chagas' Disease.Antimicrobial agents and chemotherapy · 2022Article
- Microbial proteasomes as drug targets.PLoS pathogens · 2021Review
- In Silico Survey and Characterization ofPathogens (Basel, Switzerland) · 2021Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
24 authors at 2 institutions in 2 countries.
Michael ThomasDrug Discovery Unit, Wellcome Centre for Anti-Infectives Research, Division of Biological Chemistry, University of Dundee, Dundee DD1 5EH, U.K.ORCID 0000-0003-0377-0281
Stephen BrandDrug Discovery Unit, Wellcome Centre for Anti-Infectives Research, Division of Biological Chemistry, University of Dundee, Dundee DD1 5EH, U.K.
Manu De RyckerDrug Discovery Unit, Wellcome Centre for Anti-Infectives Research, Division of Biological Chemistry, University of Dundee, Dundee DD1 5EH, U.K.ORCID 0000-0002-3171-3519
Fabio ZuccottoDrug Discovery Unit, Wellcome Centre for Anti-Infectives Research, Division of Biological Chemistry, University of Dundee, Dundee DD1 5EH, U.K.ORCID 0000-0002-3888-7423
Iva LukacDrug Discovery Unit, Wellcome Centre for Anti-Infectives Research, Division of Biological Chemistry, University of Dundee, Dundee DD1 5EH, U.K.
Peter G DoddDrug Discovery Unit, Wellcome Centre for Anti-Infectives Research, Division of Biological Chemistry, University of Dundee, Dundee DD1 5EH, U.K.
Eun-Jung KoDrug Discovery Unit, Wellcome Centre for Anti-Infectives Research, Division of Biological Chemistry, University of Dundee, Dundee DD1 5EH, U.K.ORCID 0000-0003-1222-1938
Sujatha ManthriDrug Discovery Unit, Wellcome Centre for Anti-Infectives Research, Division of Biological Chemistry, University of Dundee, Dundee DD1 5EH, U.K.
Kate McGonagleDrug Discovery Unit, Wellcome Centre for Anti-Infectives Research, Division of Biological Chemistry, University of Dundee, Dundee DD1 5EH, U.K.ORCID 0000-0001-8485-7180
Maria Osuna-CabelloDrug Discovery Unit, Wellcome Centre for Anti-Infectives Research, Division of Biological Chemistry, University of Dundee, Dundee DD1 5EH, U.K.
Jennifer RileyDrug Discovery Unit, Wellcome Centre for Anti-Infectives Research, Division of Biological Chemistry, University of Dundee, Dundee DD1 5EH, U.K.
Caterina PontDrug Discovery Unit, Wellcome Centre for Anti-Infectives Research, Division of Biological Chemistry, University of Dundee, Dundee DD1 5EH, U.K.
Frederick SimeonsDrug Discovery Unit, Wellcome Centre for Anti-Infectives Research, Division of Biological Chemistry, University of Dundee, Dundee DD1 5EH, U.K.
Laste StojanovskiDrug Discovery Unit, Wellcome Centre for Anti-Infectives Research, Division of Biological Chemistry, University of Dundee, Dundee DD1 5EH, U.K.
John ThomasDrug Discovery Unit, Wellcome Centre for Anti-Infectives Research, Division of Biological Chemistry, University of Dundee, Dundee DD1 5EH, U.K.
Stephen ThompsonDrug Discovery Unit, Wellcome Centre for Anti-Infectives Research, Division of Biological Chemistry, University of Dundee, Dundee DD1 5EH, U.K.
Elisabet ViaynaDrug Discovery Unit, Wellcome Centre for Anti-Infectives Research, Division of Biological Chemistry, University of Dundee, Dundee DD1 5EH, U.K.
Jose M FiandorGlobal Health R&D, GlaxoSmithKline, Tres Cantos 28760, Spain.
Julio MartinGlobal Health R&D, GlaxoSmithKline, Tres Cantos 28760, Spain.ORCID 0000-0003-1887-0859
Paul G WyattDrug Discovery Unit, Wellcome Centre for Anti-Infectives Research, Division of Biological Chemistry, University of Dundee, Dundee DD1 5EH, U.K.ORCID 0000-0002-0397-245X
Timothy J MilesGlobal Health R&D, GlaxoSmithKline, Tres Cantos 28760, Spain.ORCID 0000-0001-7407-7404
Kevin D ReadDrug Discovery Unit, Wellcome Centre for Anti-Infectives Research, Division of Biological Chemistry, University of Dundee, Dundee DD1 5EH, U.K.ORCID 0000-0002-8536-0130
Maria MarcoGlobal Health R&D, GlaxoSmithKline, Tres Cantos 28760, Spain.ORCID 0000-0002-2442-0021
Ian H GilbertDrug Discovery Unit, Wellcome Centre for Anti-Infectives Research, Division of Biological Chemistry, University of Dundee, Dundee DD1 5EH, U.K.ORCID 0000-0002-5238-1314
University of Dundee · GBGlaxoSmithKline (Spain) · ES
Funding
Wellcome Trust 092340Wellcome Trust 100476Wellcome Trust 105021Wellcome Trust 203134Wellcome Trust 203134/Z/16/ZWellcome Trust 204672/Z/16/Z
Abstract
There is an urgent need for new treatments for visceral leishmaniasis (VL), a parasitic infection which impacts heavily large areas of East Africa, Asia, and South America. We previously reported on the discovery of GSK3494245/DDD01305143 (
Indexed as
Drug DesignAnimalsAntiprotozoal AgentsBinding SitesCell LineDrug Evaluation, PreclinicalHalf-LifeHumansLeishmania donovaniLeishmaniasis, VisceralMiceMolecular Dynamics SimulationProteasome Endopeptidase ComplexProteasome InhibitorsProtein SubunitsProtozoan ProteinsAntiprotozoal Agentsimidazo(1,2-a)pyridineProteasome Endopeptidase ComplexProteasome InhibitorsProtein SubunitsProtozoan ProteinsPyridines
Identifiers
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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.