E-Mail Alert

Add your e-mail address to receive forthcoming issues of this journal:

Journal Browser

Journal Browser

Special Issue "Progress on Marine Natural Products as Lead Compounds"

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

Deadline for manuscript submissions: 31 July 2018

Special Issue Editors

Guest Editor
Prof. Dr. Ana Lourenço

LAQV, REQUIMTE, Departamento de Química, Faculdade de Ciências e Tecnologia, Universidade NOVA de Lisboa, 2829-516 Caparica, Portugal
Website | E-Mail
Interests: phytochemistry; marine metabolites; bioactive metabolites; organic chemistry
Guest Editor
Dr. Patrícia Máximo

LAQV, REQUIMTE, Departamento de Química, Faculdade de Ciências e Tecnologia, Universidade NOVA de Lisboa, 2829-516 Caparica, Portugal
Website | E-Mail
Interests: phytochemistry; marine metabolites; structure identification; organic chemistry

Special Issue Information

Dear Colleagues,

The development of therapeutic lead molecules encompasses many steps in different scientific areas. All converge to make headway to more efficient and available compounds. This Special Issue intends to cover progresses in molecular structures of different scaffolds that include the discovery of new compounds, the production by marine microorganisms cultures of compounds traditionally known from other sources, the knowledge of chemical diversity and bioactivity, together with synthetic approaches to produce active compounds from inactive ones, the study of the beneficial effects of compounds present in crude-drugs focused in preclinical and clinical studies, and the exploration of marine natural products by computational methodologies.

Prof. Dr. Ana Lourenço
Dr. Patrícia Máximo
Guest Editors

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 1800 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

  • natural products
  • natural products analogs
  • biological activity
  • microbial production
  • marine Crude-drugs
  • preclinical and clinical studies
  • computer aided drug-discovery

Published Papers (1 paper)

View options order results:
result details:
Displaying articles 1-1
Export citation of selected articles as:

Research

Open AccessArticle Marine-Derived 2-Aminoimidazolone Alkaloids. Leucettamine B-Related Polyandrocarpamines Inhibit Mammalian and Protozoan DYRK & CLK Kinases
Mar. Drugs 2017, 15(10), 316; doi:10.3390/md15100316
Received: 30 August 2017 / Revised: 28 September 2017 / Accepted: 12 October 2017 / Published: 17 October 2017
PDF Full-text (1869 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
A large diversity of 2-aminoimidazolone alkaloids is produced by various marine invertebrates, especially by the marine Calcareous sponges Leucetta and Clathrina. The phylogeny of these sponges and the wide scope of 2-aminoimidazolone alkaloids they produce are reviewed in this article. The origin
[...] Read more.
A large diversity of 2-aminoimidazolone alkaloids is produced by various marine invertebrates, especially by the marine Calcareous sponges Leucetta and Clathrina. The phylogeny of these sponges and the wide scope of 2-aminoimidazolone alkaloids they produce are reviewed in this article. The origin (invertebrate cells, associated microorganisms, or filtered plankton), physiological functions, and natural molecular targets of these alkaloids are largely unknown. Following the identification of leucettamine B as an inhibitor of selected protein kinases, we synthesized a family of analogues, collectively named leucettines, as potent inhibitors of DYRKs (dual-specificity, tyrosine phosphorylation regulated kinases) and CLKs (cdc2-like kinases) and potential pharmacological leads for the treatment of several diseases, including Alzheimer’s disease and Down syndrome. We assembled a small library of marine sponge- and ascidian-derived 2-aminoimidazolone alkaloids, along with several synthetic analogues, and tested them on a panel of mammalian and protozoan kinases. Polyandrocarpamines A and B were found to be potent and selective inhibitors of DYRKs and CLKs. They inhibited cyclin D1 phosphorylation on a DYRK1A phosphosite in cultured cells. 2-Aminoimidazolones thus represent a promising chemical scaffold for the design of potential therapeutic drug candidates acting as specific inhibitors of disease-relevant kinases, and possibly other disease-relevant targets. Full article
(This article belongs to the Special Issue Progress on Marine Natural Products as Lead Compounds)
Figures

Journal Contact

MDPI AG
Marine Drugs Editorial Office
St. Alban-Anlage 66, 4052 Basel, Switzerland
E-Mail: 
Tel. +41 61 683 77 34
Fax: +41 61 302 89 18
Editorial Board
Contact Details Submit to Special Issue Edit a special issue Review for Marine Drugs
logo
loading...
Back to Top