ArticleJournal of medicinal chemistry2009
Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation.
Article in Journal of medicinal chemistry, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 50 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
50 citing papers in PubMed, 104 citations in OpenAlex.
- Pobacilamides A and B, two linear depsipeptides from a marine-derived Bacillus sp. ROA-056.The Journal of antibiotics · 2026Article
- Abastatins A-C: Cathepsin D-Inhibitory Depsipeptides From a Marine Okeania sp. Cyanobacterium.Chemistry (Weinheim an der Bergstrasse, Germany) · 2026Article
- Antioxidant, Anti-Inflammatory and Anticancer Peptides from Extreme Marine Environments.Antioxidants (Basel, Switzerland) · 2026Review
- Computational theranostics strategy for pancreatic ductal adenocarcinoma.Molecular diversity · 2026Article
- A two-sample Mendelian randomization study and mediation analysis exploring the link between cathepsins and epilepsy.Epilepsia open · 2026Article
- Tandem ketone reduction in pepstatin biosynthesis reveals an FNature communications · 2025Article
- Article
- Natural Products That Contain Higher Homologated Amino Acids.Chembiochem : a European journal of chemical biology · 2024Review
- A Review of the Antimicrobial Properties of Cyanobacterial Natural Products.Molecules (Basel, Switzerland) · 2023Review
- Structural Congeners of Izenamides Responsible for Cathepsin D Inhibition: Insights from Synthesis-Derived Elucidation.Marine drugs · 2023Article
- Marine Organisms as a Prolific Source of Bioactive Depsipeptides.Marine drugs · 2023Review
- Lead/Drug Discovery from Natural Resources.Molecules (Basel, Switzerland) · 2022Review
- Therapeutic Potential of Marine Peptides in Prostate Cancer: Mechanistic Insights.Marine drugs · 2022Review
- Microglial cathepsin E plays a role in neuroinflammation and amyloid β production in Alzheimer's disease.Aging cell · 2022Article
- Therapeutic potential of marine peptides in cervical and ovarian cancers.Molecular and cellular biochemistry · 2022Review
- Oncogenic KRAS promotes growth of lung cancer cells expressing SLC3A2-NRG1 fusion via ADAM17-mediated shedding of NRG1.Oncogene · 2022Article
- Marine-Derived Compounds for the Potential Treatment of Glucocorticoid Resistance in Severe Asthma.Marine drugs · 2021Review
- Phormidepistatin from the Cyanobacterium UIC 10484: Assessing the Phylogenetic Distribution of the Statine Pharmacophore.Journal of natural products · 2021Article
- Genome Reduction and Secondary Metabolism of the Marine Sponge-Associated CyanobacteriumMarine drugs · 2021Article
- Characterization of Macroscopic Colony-Forming Filamentous Cyanobacteria from Okinawan Coasts as Potential Sources of Bioactive Compounds.Marine biotechnology (New York, N.Y.) · 2020Article
Corrections and comments
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Authors and funding
5 authors at 2 institutions in 1 country.
Funding
Abstract
In our efforts to explore marine cyanobacteria as a source of novel bioactive compounds, we discovered a statine unit-containing linear decadepsipeptide, grassystatin A (1), which we screened against a diverse set of 59 proteases. We describe the structure determination of 1 and two natural analogues, grassystatins B (2) and C (3), using NMR, MS, and chiral HPLC techniques. Compound 1 selectively inhibited cathepsins D and E with IC(50)s of 26.5 nM and 886 pM, respectively. Compound 2 showed similar potency and selectivity against cathepsins D and E (IC(50)s of 7.27 nM and 354 pM, respectively), whereas the truncated peptide analogue grassystatin C (3), which consists of two fewer residues than 1 and 2, was less potent against both but still selective for cathepsin E. The selectivity of compounds 1-3 for cathepsin E over D (20-38-fold) suggests that these natural products may be useful tools to probe cathepsin E function. We investigated the structural basis of this selectivity using molecular docking. We also show that 1 can reduce antigen presentation by dendritic cells, a process thought to rely on cathepsin E.
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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.