ArticleJournal of medicinal chemistry2013
Potent elastase inhibitors from cyanobacteria: structural basis and mechanisms mediating cytoprotective and anti-inflammatory effects in bronchial epithelial cells.
Article in Journal of medicinal chemistry, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 38 papers.
What it found
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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.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
38 citing papers in PubMed, 73 citations in OpenAlex.
- Investigating the Gut Microbiota-Inflammatory Cytokine-Skin Axis in Inflammatory Skin Diseases: Evidence from Mendelian Randomization.Clinical, cosmetic and investigational dermatology · 2026Article
- The ornithine-arginine cycle supported a toxic, metalimnic Planktothrix rubescens bloom.Harmful algae · 2026Article
- Alteration in Amino Acid Composition and Configuration in Cyanobacterial Peptides Affects Biological Activity.Journal of natural products · 2025Article
- Chemical diversity of cyanobacterial natural products.Natural product reports · 2025Review
- Structural Diversity and Biological Activity of Cyanopeptolins Produced byMarine drugs · 2023Article
- Marine Organisms as a Prolific Source of Bioactive Depsipeptides.Marine drugs · 2023Review
- Computational Approaches to Enzyme Inhibition by Marine Natural Products in the Search for New Drugs.Marine drugs · 2023Review
- Native metabolomics identifies the rivulariapeptolide family of protease inhibitors.Nature communications · 2022Article
- Bioactive Peptides and Proteins from Centipede Venoms.Molecules (Basel, Switzerland) · 2022Review
- Peptide Human Neutrophil Elastase Inhibitors from Natural Sources: An Overview.International journal of molecular sciences · 2022Review
- Cyanobacteria and microalgae bioactive compounds in skin-ageing: potential to restore extracellular matrix filling and overcome hyperpigmentation.Journal of enzyme inhibition and medicinal chemistry · 2021Review
- New Micropeptins with Anti-Neuroinflammatory Activity Isolated from a Cyanobacterial Bloom.ACS omega · 2021Article
- Bioinformatics and Network Pharmacology Identify the Therapeutic Role and Potential Mechanism of Melatonin in AD and Rosacea.Frontiers in immunology · 2021Article
- Ahp-Cyclodepsipeptides as tunable inhibitors of human neutrophil elastase and kallikrein 7: Total synthesis of tutuilamide A, serine protease selectivity profile and comparison with lyngbyastatin 7.Bioorganic & medicinal chemistry · 2020Article
- Anti-inflammatory Activity of Bioactive Compounds from Microalgae and Cyanobacteria by Focusing on the Mechanisms of Action.Molecular biology reports · 2020Review
- Targeting eukaryotic proteases for natural products-based drug development.Natural product reports · 2020Review
- Marine Cyanobacteria: A Source of Lead Compounds and their Clinically-Relevant Molecular Targets.Molecules (Basel, Switzerland) · 2020Review
- Ahp-Cyclodepsipeptide Inhibitors of Elastase: Lyngbyastatin 7 Stability, Scalable Synthesis, and Focused Library Analysis.ACS medicinal chemistry letters · 2020Article
- Palstimolide A: A Complex Polyhydroxy Macrolide with Antiparasitic Activity.Molecules (Basel, Switzerland) · 2020Article
- Tutuilamides A-C: Vinyl-Chloride-Containing Cyclodepsipeptides from Marine Cyanobacteria with Potent Elastase Inhibitory Properties.ACS chemical biology · 2020Article
Corrections and comments
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Authors and funding
7 authors at 4 institutions in 2 countries.
Funding
Abstract
We discovered new structural diversity to a prevalent, yet medicinally underappreciated, cyanobacterial protease inhibitor scaffold and undertook comprehensive protease profiling to reveal potent and selective elastase inhibition. Structure-activity relationship (SAR) studies and X-ray cocrystal structure analysis allowed a detailed assessment of critical and tunable structural elements. To realize the therapeutic potential of these cyclodepsipeptides, we probed the cellular effects of a novel and representative family member, symplostatin 5 (1), which attenuated the downstream cellular effects of elastase in an epithelial lung airway model system, alleviating clinical hallmarks of chronic pulmonary diseases such as cell death, cell detachment, and inflammation. This compound attenuated the effects of elastase on receptor activation, proteolytic processing of the adhesion protein ICAM-1, NF-κB activation, and transcriptomic changes, including the expression of pro-inflammatory cytokines IL1A, IL1B, and IL8. Compound 1 exhibited activity comparable to the clinically approved elastase inhibitor sivelestat in short-term assays and demonstrated superior sustained activity in longer-term assays.
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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.