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Special Issue "Protease and Carbonic Anhydrase Inhibitors and Their Roles in Pathological Processes"

A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Molecular Pathology, Diagnostics, and Therapeutics".

Deadline for manuscript submissions: 31 May 2018

Special Issue Editor

Guest Editor
Prof. Dr. Claudiu T. Supuran

Neurofarba Department, Sezione di Scienze Farmaceutiche e Nutraceutiche, Università degli Studi di Firenze, Sesto Fiorentino (Florence) 50019, Italy
Website | E-Mail
Phone: +39-055-4573729/3005
Fax: +39-055-4573385
Interests: drug design; metalloenzymes; carbonic anhydrases; anticancer agents; antiinfectives; sulfonamides; coumarins

Special Issue Information

Dear Colleagues,

Proteases and carbonic anhydrases are among the most widespread enzymes in organisms all over the phylogenetic tree, in which they play crucial physiological roles. Dysregulation of their activity is connected with many diseases, such as tumors, viral infections, blood coagulation disorders, digestive diseases, etc. Protease inhibitors targeting all classes of such known enzymes are widely used as antivirals (against HIV and hepatitis C infections), antithromodotics (targeting serine proteases involved in the blood coagulation cascade), whereas inhibitors of other proteases, such as matrix metalloproteinases, have found fewer applications due to their toxicity problems. Carbonic anhydrase inhibitors, on the other hand, are used as antiglaucoma, antiepileptic, antiobesity, and as diuretic drugs, whereas newer applications target metastatic tumors, both for treatment and imaging, with one small molecule and one antibody in advanced clinical trials. Antiinfectives, based on inhibition of carbonic anhydrases from pathogenic bacteria, fungi, and protozoa, have also begun to be investigated. The present Special Issue of the International Journal of Molecular Sciences welcomes contributions dealing with all aspects connected to the chemistry, biochemistry, pharmacology and toxicology of this important class of enzyme inhibitors.

Prof. Dr. Claudiu T. Supuran
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. International Journal of Molecular Sciences 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

  • carbonic anhydrase
  • protease
  • inhibitor
  • antiviral drug
  • antitumor drug
  • drug design
  • serine protease
  • metalloprotease
  • aspartic protease

Published Papers (1 paper)

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Research

Open AccessArticle Low Levels of IgG Recognizing the α-1-Antitrypsin Peptide and Its Association with Taiwanese Women with Primary Sjögren’s Syndrome
Int. J. Mol. Sci. 2017, 18(12), 2750; doi:10.3390/ijms18122750
Received: 28 October 2017 / Revised: 11 December 2017 / Accepted: 12 December 2017 / Published: 18 December 2017
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Abstract
The aim of this study was to examine oxidative stress and low level of α-1-antitrypsin (A1AT) in primary Sjögren’s syndrome (pSS), and evaluate the associated autoreactivity against unmodified and their 4-hydroxy-2-nonenal (HNE)-modified peptides with pSS. Two differentially expressed proteins, α-1-acid glycoprotein 1 (A1AG1)
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The aim of this study was to examine oxidative stress and low level of α-1-antitrypsin (A1AT) in primary Sjögren’s syndrome (pSS), and evaluate the associated autoreactivity against unmodified and their 4-hydroxy-2-nonenal (HNE)-modified peptides with pSS. Two differentially expressed proteins, α-1-acid glycoprotein 1 (A1AG1) and A1AT, exhibited 2-fold differences, and their HNE modifications were identified by depleted-albumin and immunoglobulin G (IgG) serum protein, in-solution digestion, in-gel digestion, and nano-liquid chromatography–tandem mass spectrometry (nano-LC-MS/MS) from pSS patients and age-matched healthy controls (HCs). Furthermore, levels of proteins, confirmation of HNE modifications, HNE-protein adducts and autoreactivity against unmodified and their HNE-modified peptides were further validated. Levels of the HNE-protein adduct and A1AG1 were significantly higher in pSS patients than HCs, but levels of A1AT were significantly lower in pSS patients compared to HCs. Only the HNE modification of A1AT was confirmed. Our study suggests that elevated HNE-protein adduct, oxidative stress, level (odds ratio (OR) 4.877, p = 0.003), lowered A1AT level (OR 3.910, p = 0.010) and a decreased level of anti-A1AT50–63 IgG (OR 3.360, p = 0.010) showed an increased risk in pSS patients compared to HCs, respectively. Full article
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