Special Issue "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: 26 August 2020.

Special Issue Editor

Dr. Barbara Parrino
Website
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

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All papers will be peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Marine Drugs is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2000 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

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

Published Papers (1 paper)

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Research

Open AccessArticle
CYC31, A Natural Bromophenol PTP1B Inhibitor, Activates Insulin Signaling and Improves Long Chain-Fatty Acid Oxidation in C2C12 Myotubes
Mar. Drugs 2020, 18(5), 267; https://doi.org/10.3390/md18050267 - 19 May 2020
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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