ArticlePharmaceuticals (Basel, Switzerland)2022
Identifying Human PTP1B Enzyme Inhibitors from Marine Natural Products: Perspectives for Developing of Novel Insulin-Mimetic Drugs.
Article in Pharmaceuticals (Basel, Switzerland), 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed, 15 citations in OpenAlex.
- Computational identification of a marine derived dual inhibitor for type 2 diabetes mellitus using integrated in silico approaches.Scientific reports · 2026Article
- Discovery of Novel PTP1B Inhibitors by High-throughput Virtual Screening.Current computer-aided drug design · 2026Article
- Guardians of the sea: molecular and biochemical adaptations in sharks and whales for atherosclerosis resistance and their potential in human cardioprotection.Diabetology & metabolic syndrome · 2025Review
- Unlocking potent anti-tuberculosis natural products through structure-activity relationship analysis.Natural products and bioprospecting · 2025Review
- The Mediterranean Sea on the Bench: Unveiling the Marine InvertebrateMarine drugs · 2025Article
- Identification of Antioxidant Methyl Derivatives ofInternational journal of molecular sciences · 2024Article
- Discovery of Cell-Permeable Allosteric Inhibitors of Liver Pyruvate Kinase: Design and Synthesis of Sulfone-Based Urolithins.International journal of molecular sciences · 2024Article
- Marine-Derived Phosphoeleganin and Its Semisynthetic Derivative Decrease IL6 Levels and Improve Insulin Signaling in Human Hepatocellular Carcinoma Cells.International journal of molecular sciences · 2024Article
- Article
- Natural Bioactive Compounds from Marine Invertebrates That Modulate Key Targets Implicated in the Onset of Type 2 Diabetes Mellitus (T2DM) and Its Complications.Pharmaceutics · 2023Review
- Article
- Active Biomolecules from Vegetable Extracts with Antitumoral Activity against Pancreas Cancer: A Systematic Review (2011-2021).Life (Basel, Switzerland) · 2022Review
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Authors and funding
10 authors at 3 institutions in 1 country.
Funding
Abstract
Diabetes mellitus (DM) represents a complex and multifactorial disease that causes metabolic disorders with acute and long-term serious complications. The onset of DM, with over 90% of cases of diabetes classified as type 2, implies several metabolic dysfunctions leading to consider DM a worldwide health problem. In this frame, protein tyrosine phosphatase 1B (PTP1B) and aldose reductase (AR) are two emerging targets involved in the development of type 2 diabetes mellitus (T2DM) and its chronic complications. Herein, we employed a marine-derived dual type inhibitor of these enzymes, phosphoeleganin, as chemical starting point to perform a fragment-based process in search for new inhibitors. Phosphoeleganin was both disassembled by its oxidative cleavage and used as model structure for the synthesis of a small library of functionalized derivatives as rationally designed analogues. Pharmacological screening supported by in silico docking analysis outlined the mechanism of action against PTP1B exerted by a phosphorylated fragment and a synthetic simplified analogue, which represent the most potent inhibitors in the library.
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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.