Therapeutic Marine Enzyme Inhibitors as Leads for the Discovery of New Bioactive Drugs

A special issue of Marine Drugs (ISSN 1660-3397).

Deadline for manuscript submissions: closed (15 October 2020) | Viewed by 5069

Special Issue Editor


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Guest Editor
Department of Biological, Chemical, and Pharmaceutical Sciences and Technologies (STEBICEF), University of Palermo, via Archirafi 32, 90123 Palermo, Italy
Interests: synthesis; reactivity studies of policondensed nitrogen heterocycles; synthesis of marine-derived analogs
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Special Issue Information

Dear Colleagues,                

Enzyme inhibitors, which are bioactive molecules that are able to bind enzymes decreasing their bioactivity, are applied in different therapeutic areas since they are enzymes involved in the control of complex biochemical networks. Many marine natural products are enzyme inhibitors used as chemical defences in their natural environment. Considering their significant biological activity and their structural variety, they represent important lead compounds for the discovery of new molecules with therapeutic applications.

This Special Issue "Therapeutic Marine Enzyme Inhibitors as Leads for the Discovery of New Bioactive Drugs" focuses on recent advances in the isolation, synthesis, biosynthesis, and characterization of marine-derived compounds or analogs designed through an in silico or classical medicinal chemistry approach, with enzyme inhibitory activity that could be useful for the treatment of various diseases.

Dr. Barbara Parrino
Guest Editor

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Keywords

  • Drug discovery
  • Marine-derived molecule
  • Marine-derived analogs
  • Synthesis
  • Enzyme inhibitors
  • Biological activity
  • Computational studies
  • Therapeutic drugs

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Published Papers (1 paper)

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Research

13 pages, 2455 KiB  
Article
CYC31, A Natural Bromophenol PTP1B Inhibitor, Activates Insulin Signaling and Improves Long Chain-Fatty Acid Oxidation in C2C12 Myotubes
by Jiao Luo, Yufei Hou, Mengyue Xie, Wanli Ma, Dayong Shi and Bo Jiang
Mar. Drugs 2020, 18(5), 267; https://doi.org/10.3390/md18050267 - 19 May 2020
Cited by 14 | Viewed by 4328
Abstract
3-bromo-4,5-Bis(2,3-dibromo-4,5-dihydroxybenzyl)-1,2-benzenediol (CYC31) is a bromophenol protein tyrosine phosphatase 1B (PTP1B) inhibitor isolated from the red alga Rhodomela confervoides. Here, the effect of CYC31 on the insulin signaling and fatty-acid-induced disorders in C2C12 myotubes was investigated. Molecular docking assay showed that CYC31 was [...] Read more.
3-bromo-4,5-Bis(2,3-dibromo-4,5-dihydroxybenzyl)-1,2-benzenediol (CYC31) is a bromophenol protein tyrosine phosphatase 1B (PTP1B) inhibitor isolated from the red alga Rhodomela confervoides. Here, the effect of CYC31 on the insulin signaling and fatty-acid-induced disorders in C2C12 myotubes was investigated. Molecular docking assay showed that CYC31 was embedded into the catalytic pocket of PTP1B. A cellular study found that CYC31 increased the activity of insulin signaling and promoted 2-NBDG uptake through GLUT4 translocation in C2C12 myotubes. Further studies showed that CYC31 ameliorated palmitate-induced insulin resistance in C2C12 myotubes. Moreover, CYC31 treatment significantly increased the mRNA expression of carnitine palmitoyltransferase 1B (CPT-1B) and fatty acid binding protein 3 (FABP3), which was tightly linked with fatty acid oxidation. These findings suggested that CYC31 could prevent palmitate-induce insulin resistance and could improve fatty acid oxidation through PTP1B inhibition. Full article
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