ArticleEuropean journal of medicinal chemistry2012
Structural analysis of inhibition of Mycobacterium tuberculosis methionine aminopeptidase by bengamide derivatives.
Article in European journal of medicinal chemistry, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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Who cites it
11 citing papers in PubMed, 22 citations in OpenAlex.
- Ribosomal expansion segment contributes to translation fidelity via N-terminal processing of ribosomal proteins.Nucleic acids research · 2025Article
- The Development of the Bengamides as New Antibiotics against Drug-Resistant Bacteria.Marine drugs · 2022Review
- Identification of Antimycobacterial Natural Products from a Library of Marine Invertebrate Extracts.Medicines (Basel, Switzerland) · 2022Article
- Decoding the Function of Expansion Segments in Ribosomes.Molecular cell · 2018Article
- The Bengamides: A Mini-Review of Natural Sources, Analogues, Biological Properties, Biosynthetic Origins, and Future Prospects.Journal of natural products · 2017Review
- Marine Natural Products from New Caledonia--A Review.Marine drugs · 2016Review
- Advances in Bacterial Methionine Aminopeptidase Inhibition.Current topics in medicinal chemistry · 2016Review
- Crystal structure of XoLAP, a leucine aminopeptidase, from Xanthomonas oryzae pv. oryzae.Journal of microbiology (Seoul, Korea) · 2013Article
- Structural analysis of bengamide derivatives as inhibitors of methionine aminopeptidases.Journal of medicinal chemistry · 2012Article
- Myxobacteria versus sponge-derived alkaloids: the bengamide family identified as potent immune modulating agents by scrutiny of LC-MS/ELSD libraries.Bioorganic & medicinal chemistry · 2012Article
- Methionine aminopeptidases: Potential therapeutic target for microsporidia and other microbes.The Journal of eukaryotic microbiologyReview
Corrections and comments
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Authors and funding
3 authors at 1 institution in 2 countries.
Funding
Abstract
Natural product-derived bengamides possess potent antiproliferative activity and target human methionine aminopeptidases for their cellular effects. Using bengamides as a template, several derivatives were designed and synthesized as inhibitors of methionine aminopeptidases of Mycobacterium tuberculosis, and initial antitubercular activity were observed. Here, we present three new X-ray structures of the tubercular enzyme MtMetAP1c in complex with the inhibitors in the Mn(II) form and in the Ni(II) form. All amide moieties of the bengamide derivatives bind to the unique shallow cavity and interact with a flat surface created by His-212 of MtMetAP1c in the Mn(II) form. However, the active site metal has significant influence on the binding mode, because the amide takes a different conformation in the Ni(II) form. The interactions of these inhibitors at the active site provide the structural basis for further modification of these bengamide inhibitors for improved potency and selectivity.
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Registered trials
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