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Special Issue "Phospholipases and Lipases: Targets for Drug Development"

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: closed (28 February 2018).

Special Issue Editor

Prof. Dr. Dimitra Hadjipavlou-Litina
E-Mail Website
Guest Editor
Department of Pharmaceutical Chemistry, School of Pharmacy, Aristotle University of Thessaloniki, Thessaloniki 54124, Greece
Interests: synthesis and biological studies on anti-inflammatory and antioxidant agents, on inhibitors of enzymes implicated in the inflammation and in the coagulation process in general; correlation of inflammation with cancer; neurodegeneration; antioxidant activity; theoretical and experimental calculation of physicochemical parameters implicated in biological response; use of computational chemistry in drug design as well as bioactive compounds of natural origin, e.g., essential oils
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Special Issue Information

Dear Colleagues,

Lipases and phospholipases govern mammalian metabolism. They share many common features; however, they differ from other metabolic enzymes. Their potential as drug targets for the treatment of metabolic diseases, cancer, atheromatosis, neurogenerative diseases and inflammation is widely recognized, and the first lipase inhibitor drugs have been successfully introduced.

The potential for phospholipases as targets for treating atherogenesis has become more prominent over the past year with the publication of the results of Phase 2 clinical trials of two inhibitors of forms of phospholipase A2: darapladib (GSK), which inhibits lipoprotein-associated phospholipase A2 and varespladib (Anthera) an inhibitor of several secreted phospholipase A2s.

Phospholipase A2 is a known mediator of inflammation, atherosclerosis and cancer in mammals. Inhibition of PLA2 alters cancer. It, therefore, makes the enzyme a potential drug target. Furthermore, phospholipases can be used for liposome-based drug delivery and as diagnostic tools.

Prof. Dr. Dimitra Hadjipavlou-Litina
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. Molecules is an international peer-reviewed open access semimonthly 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

  • phospholipase inhibitors
  • lipase inhibitors
  • drug targets
  • cytosolic
  • secreted phospholipase
  • serine lipase
  • atheromatosis
  • neurogeneration
  • obesity
  • metabolism

Published Papers (2 papers)

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Research

Open AccessArticle
Small Peptides Able to Suppress Prostaglandin E2 Generation in Renal Mesangial Cells
Molecules 2018, 23(1), 158; https://doi.org/10.3390/molecules23010158 - 13 Jan 2018
Cited by 7 | Viewed by 1555
Abstract
Peptide drug discovery may play a key role in the identification of novel medicinal agents. Here, we present the development of novel small peptides able to suppress the production of PGE2 in mesangial cells. The new compounds were generated by structural alterations [...] Read more.
Peptide drug discovery may play a key role in the identification of novel medicinal agents. Here, we present the development of novel small peptides able to suppress the production of PGE2 in mesangial cells. The new compounds were generated by structural alterations applied on GK115, a novel inhibitor of secreted phospholipase A2, which has been previously shown to reduce PGE2 synthesis in rat renal mesangial cells. Among the synthesized compounds, the tripeptide derivative 11 exhibited a nice dose-dependent suppression of PGE2 production, similar to that observed for GK115. Full article
(This article belongs to the Special Issue Phospholipases and Lipases: Targets for Drug Development)
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Open AccessArticle
Evaluation of Rhamnetin as an Inhibitor of the Pharmacological Effect of Secretory Phospholipase A2
Molecules 2017, 22(9), 1441; https://doi.org/10.3390/molecules22091441 - 31 Aug 2017
Cited by 11 | Viewed by 2508
Abstract
Rhamnetin (Rhm), 3-O-methylquercetin (3MQ), and Rhamnazin (Rhz) are methylated derivatives of quercetin commonly found in fruits and vegetables that possess antioxidant and anti-inflammatory properties. Phospholipase A2 (PLA2) displays several important roles during acute inflammation; therefore, this study aimed at investigating new [...] Read more.
Rhamnetin (Rhm), 3-O-methylquercetin (3MQ), and Rhamnazin (Rhz) are methylated derivatives of quercetin commonly found in fruits and vegetables that possess antioxidant and anti-inflammatory properties. Phospholipase A2 (PLA2) displays several important roles during acute inflammation; therefore, this study aimed at investigating new compounds able to inhibit this enzyme, besides evaluating creatine kinase (CK) levels and citotoxicity. Methylated quercetins were compared with quercetin (Q) and were incubated with secretory PLA2 (sPLA2) from Bothrops jararacussu to determine their inhibitory activity. Cytotoxic studies were performed by using the J774 cell lineage incubated with quercertins. In vivo tests were performed with Swiss female mice to evaluate decreasing paw edema potential and compounds’ CK levels. Structural modifications on sPLA2 were made with circular dichroism (CD). Despite Q and Rhz showing greater enzymatic inhibitory potential, high CK was observed. Rhm exhibited sPLA2 inhibitory potential, no toxicity and, remarkably, it decreased CK levels. The presence of 3OH on the C-ring of Rhm may contribute to both its anti-inflammatory and enzymatic inhibition of sPLA2, and the methylation of ring A may provide the increase in cell viability and low CK level induced by sPLA2. These results showed that Rhm can be a candidate as a natural compound for the development of new anti-inflammatory drugs. Full article
(This article belongs to the Special Issue Phospholipases and Lipases: Targets for Drug Development)
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