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Special Issue "Recent Trends on Enzymes Inhibitors and Activators in Drug Research"

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

Deadline for manuscript submissions: 30 April 2018

Special Issue Editor

Guest Editor
Dr. Athina Geronikaki

Department of Medicinal Chemistry, School of Pharmacy, Aristotle University of Thessaloniki, Thessaloniki, Greece
Website | E-Mail
Phone: +302310997616
Interests: COX; LOX; PTP1B; HIV; antimicrobial; antiinflammatory

Special Issue Information

Dear Colleagues,

It is known that enzymes are involved in many pathological conditions, such as inflammation, diabetes, microbial infections, HIV, and neoplastic diseases among others. Enzyme inhibition is universally accepted as a strategy to treat the above mentioned conditions or to alternate the mechanism involved. Thus, the aim of the current Special Issue is to collect and present recent advances in the research fields connected to inhibition of different types of enzymes, such as Cyclooxygenase-1/Cyclooxygenase-2 (COX-1/COX-2.), Lipoxygenase (LOX), Protein tyrosine phosphatase 1B (PTP-1B), Peroxisome Proliferator-Activated Receptor Gamma (PPAR-γ), reverse transcriptase, integrase, gyrase, MurB, aldose reductase, carbonic anhydrise, etc.

Dr. Athina Geronikaki
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 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

  • COX/LOX
  • Reverse transcriptase
  • Integrase
  • gyrase
  • aldose reductase
  • carbonic anhydrise
  • PTP-1B

Published Papers (3 papers)

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Research

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Open AccessArticle 4-Thiazolidinone Derivatives as MMP Inhibitors in Tissue Damage: Synthesis, Biological Evaluation and Docking Studies
Molecules 2018, 23(2), 415; doi:10.3390/molecules23020415
Received: 30 October 2017 / Revised: 1 February 2018 / Accepted: 3 February 2018 / Published: 14 February 2018
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Abstract
Nine 2-(1,2-benzothiazol-3-yl)-N-(4-oxo-2-phenyl-1,3-thiazolidin-3-yl)propanamides combining a benzisothiazole and 4-thiazolidinone in one framework were designed and synthesized. The aim of the study was to verify their effectiveness to affect the inflammatory/oxidative process in which free oxygen and nitrite (ROS and RNS) radicals, inflammatory mediators,
[...] Read more.
Nine 2-(1,2-benzothiazol-3-yl)-N-(4-oxo-2-phenyl-1,3-thiazolidin-3-yl)propanamides combining a benzisothiazole and 4-thiazolidinone in one framework were designed and synthesized. The aim of the study was to verify their effectiveness to affect the inflammatory/oxidative process in which free oxygen and nitrite (ROS and RNS) radicals, inflammatory mediators, such as nuclear factor κB (NF-κB), and matrix metalloproteinases (MMPs) are involved. Docking studies of all the compounds were performed in order to explore their binding mode at the MMP-9 protein. An appreciable anti-inflammatory/potential wound healing effects of the tested compounds was highlighted. Derivative 23, bearing a 4-carboxyphenyl substituent at C2 of the 4-thiazolidinone ring, exhibited the highest activity, being able to inhibit MMP-9 at nanomolar level(IC50 = 40 nM). Full article
(This article belongs to the Special Issue Recent Trends on Enzymes Inhibitors and Activators in Drug Research)
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Review

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Open AccessReview HIV Resistance Prediction to Reverse Transcriptase Inhibitors: Focus on Open Data
Molecules 2018, 23(4), 956; doi:10.3390/molecules23040956
Received: 21 March 2018 / Revised: 16 April 2018 / Accepted: 17 April 2018 / Published: 19 April 2018
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Abstract
Research and development of new antiretroviral agents are in great demand due to issues with safety and efficacy of the antiretroviral drugs. HIV reverse transcriptase (RT) is an important target for HIV treatment. RT inhibitors targeting early stages of the virus-host interaction are
[...] Read more.
Research and development of new antiretroviral agents are in great demand due to issues with safety and efficacy of the antiretroviral drugs. HIV reverse transcriptase (RT) is an important target for HIV treatment. RT inhibitors targeting early stages of the virus-host interaction are of great interest for researchers. There are a lot of clinical and biochemical data on relationships between the occurring of the single point mutations and their combinations in the pol gene of HIV and resistance of the particular variants of HIV to nucleoside and non-nucleoside reverse transcriptase inhibitors. The experimental data stored in the databases of HIV sequences can be used for development of methods that are able to predict HIV resistance based on amino acid or nucleotide sequences. The data on HIV sequences resistance can be further used for (1) development of new antiretroviral agents with high potential for HIV inhibition and elimination and (2) optimization of antiretroviral therapy. In our communication, we focus on the data on the RT sequences and HIV resistance, which are available on the Internet. The experimental methods, which are applied to produce the data on HIV-1 resistance, the known data on their concordance, are also discussed. Full article
(This article belongs to the Special Issue Recent Trends on Enzymes Inhibitors and Activators in Drug Research)
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Open AccessReview Thiazoles and Thiazolidinones as COX/LOX Inhibitors
Molecules 2018, 23(3), 685; doi:10.3390/molecules23030685
Received: 28 February 2018 / Revised: 14 March 2018 / Accepted: 16 March 2018 / Published: 18 March 2018
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Abstract
Inflammation is a natural process that is connected to various conditions and disorders such as arthritis, psoriasis, cancer, infections, asthma, etc. Based on the fact that cyclooxygenase isoenzymes (COX-1, COX-2) are responsible for the production of prostaglandins that play an important role in
[...] Read more.
Inflammation is a natural process that is connected to various conditions and disorders such as arthritis, psoriasis, cancer, infections, asthma, etc. Based on the fact that cyclooxygenase isoenzymes (COX-1, COX-2) are responsible for the production of prostaglandins that play an important role in inflammation, traditional treatment approaches include administration of non-steroidal anti-inflammatory drugs (NSAIDs), which act as selective or non-selective COX inhibitors. Almost all of them present a number of unwanted, often serious, side effects as a consequence of interference with the arachidonic acid cascade. In search for new drugs to avoid side effects, while maintaining high potency over inflammation, scientists turned their interest to the synthesis of dual COX/LOX inhibitors, which could provide numerous therapeutic advantages in terms of anti-inflammatory activity, improved gastric protection and safer cardiovascular profile compared to conventional NSAIDs. Τhiazole and thiazolidinone moieties can be found in numerous biologically active compounds of natural origin, as well as synthetic molecules that possess a wide range of pharmacological activities. This review focuses on the biological activity of several thiazole and thiazolidinone derivatives as COX-1/COX-2 and LOX inhibitors. Full article
(This article belongs to the Special Issue Recent Trends on Enzymes Inhibitors and Activators in Drug Research)
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