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Progress in Drug Development for Inflammatory Diseases

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

Deadline for manuscript submissions: 31 December 2024 | Viewed by 1272

Special Issue Editors


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Guest Editor
Department of Drug Chemistry and Technologies, Sapienza University of Rome, P.le A. Moro 5, 00185 Rome, Italy
Interests: drug design; enzyme inhibition; antitumoral drugs; carbonic anhydrase; MAO; neurodegenerative diseases; CORMs; MOF; ADC

E-Mail Website
Guest Editor
Department of Drug Chemistry and Technologies, Sapienza University of Rome, P.le A. Moro 5, 00185 Rome, Italy
Interests: drug design; enzyme inhibition; antitumoral drugs; carbonic anhydrase; MAO; neurodegenerative diseases; CORMs; MOF; ADC

E-Mail Website
Guest Editor
IC2MP UMR 7285, Université de Poitiers-CNRS, 4 rue Michel Brunet TSA, CEDEX 9, 86073 Poitiers, France
Interests: drug design; enzyme inhibition; CORMs; carbonic anhydrase; MAO; fluorine chemistry; superacid chemistry; inflammatory diseases

Special Issue Information

Dear Colleagues,

Inflammatory-based disorders are a large group of diseases which affect a high percentage of the global community, representing a significant social and economic burden. Among them, rheumatic-based diseases, which affect the joints of the patients and impair their everyday lives with disabling ache-associated symptoms, are still far from being effectively treated. The dangerous side effects of the disease-modifying anti-rheumatic drugs (DMARDs), currently used as first line treatment, represent a limitation with their chronic use and there is an urgent need for new therapeutic tools.

Increasing evidence suggests that inflammation also plays a critical role in neurodegenerative diseases (NNDs), which are multifactorial, progressive, and debilitating disorders whose aetiology are still not completely unravelled. The partially unknown pathological mechanisms make their therapy extremely difficult and the currently available therapeutics are focused on relief of symptoms, the drugs being unable to counteract their progression. In these regards, novel drugs and therapies targeting, among others, inflammatory pathways, can be very useful as neuroprotective strategies.

In this Special Issue, we aim to collect the latest advances in the study and development of new molecules, as potential agents for the treatment of an array of diseases involving inflammation and/or neurodegeneration.

Both original articles and reviews are welcome.

We look forward to receiving your contributions, and hope that the resulting collection will provide a realistic overview of the current medicinal chemistry approaches for the treatment of inflammatory diseases.

Dr. Guglielmi Paolo
Prof. Dr. Daniela Secci
Dr. Emanuela Berrino
Guest Editors

Manuscript Submission Information

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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 2700 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

  • inflammation
  • rheumatic diseases
  • neurodegeneration
  • monoamine oxidases (MAOs)
  • cholinesterases (ChEs)
  • antioxidants
  • structure-activity relationship
  • drug design

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Published Papers (1 paper)

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Review

28 pages, 2441 KiB  
Review
TSPO Radioligands for Neuroinflammation: An Overview
by Silvia Salerno, Monica Viviano, Emma Baglini, Valeria Poggetti, Doralice Giorgini, Jacopo Castagnoli, Elisabetta Barresi, Sabrina Castellano, Federico Da Settimo and Sabrina Taliani
Molecules 2024, 29(17), 4212; https://doi.org/10.3390/molecules29174212 - 5 Sep 2024
Viewed by 736
Abstract
The translocator protein (TSPO) is predominately localized on the outer mitochondrial membrane in steroidogenic cells. In the brain, TSPO expression, low under normal conditions, results upregulated in response to glial cell activation, that occurs in neuroinflammation. As a consequence, TSPO has been extensively [...] Read more.
The translocator protein (TSPO) is predominately localized on the outer mitochondrial membrane in steroidogenic cells. In the brain, TSPO expression, low under normal conditions, results upregulated in response to glial cell activation, that occurs in neuroinflammation. As a consequence, TSPO has been extensively studied as a biomarker of such conditions by means of TSPO-targeted radiotracers. Although [11C]-PK11195, the prototypical TSPO radioligand, is still widely used for in vivo studies, it is endowed with severe limitations, mainly low sensitivity and poor amenability to quantification. Consequently, several efforts have been focused on the design of new radiotracers for the in vivo imaging of TSPO. The present review will provide an outlook on the latest advances in TSPO radioligands for neuroinflammation imaging. The final goal is to pave the way for (radio)chemists in the future design and development of novel effective and sensitive radiopharmaceuticals targeting TSPO. Full article
(This article belongs to the Special Issue Progress in Drug Development for Inflammatory Diseases)
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