ArticleBioorganic & medicinal chemistry2016
Tasiamide F, a potent inhibitor of cathepsins D and E from a marine cyanobacterium.
Article in Bioorganic & medicinal chemistry, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers.
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Who cites it
23 citing papers in PubMed, 38 citations in OpenAlex.
- Abastatins A-C: Cathepsin D-Inhibitory Depsipeptides From a Marine Okeania sp. Cyanobacterium.Chemistry (Weinheim an der Bergstrasse, Germany) · 2026Article
- A two-sample Mendelian randomization study and mediation analysis exploring the link between cathepsins and epilepsy.Epilepsia open · 2026Article
- Chemical diversity of cyanobacterial natural products.Natural product reports · 2025Review
- Recent progression on phytochemicals and pharmacological properties of the filamentous cyanobacterium Lyngbya sp.Naunyn-Schmiedeberg's archives of pharmacology · 2023Review
- Stalling the Course of Neurodegenerative Diseases: Could Cyanobacteria Constitute a New Approach toward Therapy?Biomolecules · 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
- Natural Products from Plants and Algae for Treatment of Alzheimer's Disease: A Review.Biomolecules · 2022Review
- Marine-Derived Compounds with Anti-Alzheimer's Disease Activities.Marine drugs · 2021Review
- Bridging Cyanobacteria to Neurodegenerative Diseases: A New Potential Source of Bioactive Compounds against Alzheimer's Disease.Marine drugs · 2021Review
- Review
- 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
- Cathepsin E expression and activity: Role in the detection and treatment of pancreatic cancer.Pancreatology : official journal of the International Association of Pancreatology (IAP) ... [et al.] · 2019Review
- Total Syntheses of Cathepsin D Inhibitory Izenamides A, B, and C and Structural Confirmation of Izenamide B.Molecules (Basel, Switzerland) · 2019Article
- Natural Products from Cyanobacteria: Focus on Beneficial Activities.Marine drugs · 2019Review
- Discovery of Amantamide, a Selective CXCR7 Agonist from Marine Cyanobacteria.Organic letters · 2019Article
- Recent Advances in Exploration and Biotechnological Production of Bioactive Compounds in Three Cyanobacterial Genera:Frontiers in chemistry · 2019Review
- Discovery, Synthesis, Pharmacological Profiling, and Biological Characterization of Brintonamides A-E, Novel Dual Protease and GPCR Modulators from a Marine Cyanobacterium.Journal of medicinal chemistry · 2018Article
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Authors and funding
4 authors at 2 institutions in 1 country.
Funding
Abstract
In search of novel protease inhibitors with therapeutic potential, our efforts exploring the marine cyanobacterium Lyngbya sp. have led to the discovery of tasiamide F (1), which is an analogue of tasiamide B (2). The structure was elucidated using a combination of NMR spectroscopy and mass spectrometry. The key structural feature in 1 is the presence of the Phe-derived statine core, which contributes to its aspartic protease inhibitory activity. The antiproteolytic activity of 1 and 2 was evaluated in vitro against cathepsins D and E, and BACE1. Tasiamide F (1) displayed IC50 values of 57nM, 23nM, and 0.69μM, respectively, indicating greater selectivity for cathepsins over BACE1 compared with tasiamide B (2). Molecular docking experiments were carried out for compounds 1 and 2 against cathepsins D and E to rationalize their activity towards these proteases. The dysregulated activities of cathepsins D and E have been implicated in cancer and modulation of immune responses, respectively, and these proteases represent potential therapeutic targets.
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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.