ArticleACS chemical biology2015
N-myristoyltransferase is a cell wall target in Aspergillus fumigatus.
Article in ACS chemical biology, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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Who cites it
16 citing papers in PubMed, 44 citations in OpenAlex.
- Structure guided modification of 2-chloro-5-(ethyl-phenyl-sulfamoyl)-N-[2-(2-oxo-pyrrolidin-1-yl)-phenyl]-benzamide to afford selective inhibitors of Cryptosporidium parvum N-myristoyltransferase.Bioorganic & medicinal chemistry letters · 2025Article
- Romanian Bee Product Analysis: Chemical Composition, Antimicrobial Activity, and Molecular Docking Insights.Foods (Basel, Switzerland) · 2024Article
- Discovery of Novel Myristic Acid Derivatives as N-Myristoyltransferase Inhibitors: Design, Synthesis, Analysis, Computational Studies and Antifungal Activity.Antibiotics (Basel, Switzerland) · 2023Article
- Article
- Post-translational modifications drive secondary metabolite biosynthesis in Aspergillus: a review.Environmental microbiology · 2022Review
- Molecular targets for antifungals in amino acid and protein biosynthetic pathways.Amino acids · 2021Review
- A Not-So-Ancient Grease History: Click Chemistry and Protein Lipid Modifications.Chemical reviews · 2021Review
- Novel Thienopyrimidine Inhibitors ofJournal of medicinal chemistry · 2020Article
- N-Myristoyltransferase as a Glycine and Lysine Myristoyltransferase in Cancer, Immunity, and Infections.ACS chemical biology · 2020Review
- Wheat pathogenRSC chemical biology · 2020Article
- Inhibition of N-myristoyltransferase1 affects dengue virus replication.MicrobiologyOpen · 2019Article
- Structure-Guided Identification of Resistance Breaking Antimalarial N‑Myristoyltransferase Inhibitors.Cell chemical biology · 2019Article
- Design and Synthesis of Brain Penetrant Trypanocidal N-Myristoyltransferase Inhibitors.Journal of medicinal chemistry · 2017Article
- N-Myristoyltransferase Inhibition Induces ER-Stress, Cell Cycle Arrest, and Apoptosis in Cancer Cells.ACS chemical biology · 2016Article
- Structure and Functional Diversity of GCN5-Related N-Acetyltransferases (GNAT).International journal of molecular sciences · 2016Review
- All about that fat: Lipid modification of proteins in Cryptococcus neoformans.Journal of microbiology (Seoul, Korea) · 2016Review
Corrections and comments
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Authors and funding
11 authors at 2 institutions in 1 country.
Funding
Abstract
Treatment of filamentous fungal infections relies on a limited repertoire of antifungal agents. Compounds possessing novel modes of action are urgently required. N-myristoylation is a ubiquitous modification of eukaryotic proteins. The enzyme N-myristoyltransferase (NMT) has been considered a potential therapeutic target in protozoa and yeasts. Here, we show that the filamentous fungal pathogen Aspergillus fumigatus possesses an active NMT enzyme that is essential for survival. Surprisingly, partial repression of the gene revealed downstream effects of N-myristoylation on cell wall morphology. Screening a library of inhibitors led to the discovery of a pyrazole sulphonamide compound that inhibits the enzyme and is fungicidal under partially repressive nmt conditions. Together with a crystallographic complex showing the inhibitor binding in the peptide substrate pocket, we provide evidence of NMT being a potential drug target in A. fumigatus.
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Registered trials
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.