ArticleAntimicrobial agents and chemotherapy2012
E1210, a new broad-spectrum antifungal, suppresses Candida albicans hyphal growth through inhibition of glycosylphosphatidylinositol biosynthesis.
Article in Antimicrobial agents and chemotherapy, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 104 papers.
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104 citing papers in PubMed, 164 citations in OpenAlex.
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- Clinical safety and efficacy of novel antifungal, fosmanogepix, for the treatment of candidaemia: results from a Phase 2 trial.The Journal of antimicrobial chemotherapy · 2023Trial
- Clinical Efficacy and Safety of a Novel Antifungal, Fosmanogepix, in Patients with Candidemia Caused by Candida aurisAntimicrobial agents and chemotherapy · 2023Trial
- Safety and Pharmacokinetics of Intravenous and Oral Fosmanogepix, a First-in-Class Antifungal Agent, in Healthy Volunteers.Antimicrobial agents and chemotherapy · 2023Trial
- Fosmanogepix: A comprehensive review of its origin, mechanism, antifungal efficacy, and resistance (Review).Biomedical reports · 2026Review
- New Perspectives on Antimicrobial Agents: Fosmanogepix.Antimicrobial agents and chemotherapy · 2026Review
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- Addressing the dual-use of antifungals and fungal antimicrobial resistance (fAMR) through a One Health approach.npj antimicrobials and resistance · 2026Review
- Drug Discovery and Repurposing forJournal of fungi (Basel, Switzerland) · 2025Review
- Eumycetoma: pathogenesis, current treatments, and the search for new drugs.Applied microbiology and biotechnology · 2025Review
- Next-generation antifungal drugs: Mechanisms, efficacy, and clinical prospects.Acta pharmaceutica Sinica. B · 2025Review
- Antibiofilm activity of manogepix, ibrexafungerp, amphotericin B, rezafungin, and caspofungin againstAntimicrobial agents and chemotherapy · 2025Article
- Fungal biofilms in human health and disease.Nature reviews. Microbiology · 2025Review
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- Induction Treatment for HIV-Associated Cryptococcal Meningitis: Where Have We Been and Where Are We Going?Microorganisms · 2025Review
- Recent developments inMicrobiology and molecular biology reviews : MMBR · 2025Review
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- Baicalein as a potent antifungal agent againstFrontiers in microbiology · 2025Article
- Exploring the Arsenal of Novel Antifungal Drug Targets for Combating Fungal Infections.Current pharmaceutical biotechnology · 2025Review
- The evolution of antifungal therapy: Traditional agents, current challenges and future perspectives.Current research in microbial sciences · 2025Review
44 more citing papers are in PubMed but not listed here.
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Authors and funding
6 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Continued research toward the development of new antifungals that act via inhibition of glycosylphosphatidylinositol (GPI) biosynthesis led to the design of E1210. In this study, we assessed the selectivity of the inhibitory activity of E1210 against Candida albicans GWT1 (Orf19.6884) protein, Aspergillus fumigatus GWT1 (AFUA_1G14870) protein, and human PIG-W protein, which can catalyze the inositol acylation of GPI early in the GPI biosynthesis pathway, and then we assessed the effects of E1210 on key C. albicans virulence factors. E1210 inhibited the inositol acylation activity of C. albicans Gwt1p and A. fumigatus Gwt1p with 50% inhibitory concentrations (IC(50)s) of 0.3 to 0.6 μM but had no inhibitory activity against human Pig-Wp even at concentrations as high as 100 μM. To confirm the inhibition of fungal GPI biosynthesis, expression of ALS1 protein, a GPI-anchored protein, on the surfaces of C. albicans cells treated with E1210 was studied and shown to be significantly lower than that on untreated cells. However, the ALS1 protein levels in the crude extract and the RHO1 protein levels on the cell surface were found to be almost the same. Furthermore, E1210 inhibited germ tube formation, adherence to polystyrene surfaces, and biofilm formation of C. albicans at concentrations above its MIC. These results suggested that E1210 selectively inhibited inositol acylation of fungus-specific GPI which would be catalyzed by Gwt1p, leading to the inhibition of GPI-anchored protein maturation, and also that E1210 suppressed the expression of some important virulence factors of C. albicans, through its GPI biosynthesis inhibition.
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