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Special Issue "Theranostic Targeting of Cyclooxygenase-2: The Why, How and When?"

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

Deadline for manuscript submissions: 28 February 2021.

Special Issue Editors

Prof. Dr. Jens Pietzsch
Website1 Website2
Guest Editor
Helmholtz-Zentrum Dresden-Rossendorf (HZDR), Institute of Radiopharmaceutical Cancer Research, Department of Radiopharmaceutical and Chemical Biology & Technische Universität Dresden (TUD), School of Science, Faculty of Chemistry and Food Chemistry; Germany
Interests: cancer; inflammation; theranostics; radiotracer; endoradiotherapy; radiosensitizer; therapy resistance; tumor microenvironment; extracellular matrix; preclinical molecular imaging; multimodal imaging; imaging probes; positron emission tomography (PET); single-photon emission computed tomography (SPECT); optical imaging
Dr. Markus Laube

Guest Editor
Helmholtz-Zentrum Dresden-Rossendorf (HZDR), Institute of Radiopharmaceutical Cancer Research, Department of Radiopharmaceutical and Chemical Biology; Germany
Interests: imaging probes, radiotracer development, radiochemistry, radiosensitizer, radioprotectants

Special Issue Information

Dear Colleagues,

COX-2, the inducible isoform of cyclooxygenases or prostaglandin-endoperoxide synthases (EC, is a key player in inflammatory, regenerative, and tumor-associated processes. The fact that this enzyme is only basally expressed and synthesized in a few organs and tissues in the healthy state, but is induced and highly activated in a tissue inflammatory response, makes it a highly attractive target for diagnostic and therapeutic approaches.

From the diagnostic side, non-invasive imaging and quantification of the functional expression of this enzyme as an indicator of an acute or chronic inflammatory response is highly desirable. However, COX-2 is a very challenging molecular target due to its localization within the cell and its lipophilic substrate and inhibitor-binding pocket. After all, a tracer, whether radionuclide- or dye-labeled, must penetrate two membranes in suitable quantities and with a suitable time window in order to reach the enzyme. This requires both sufficient lipophilicity as well as selectivity regarding the concomitant inhibition of COX-1 in addition to the maintenance of specificity. Despite extensive efforts, no suitable tracer approach has yet found its way into the clinic.

This Special Issue therefore invites all groups committed to the development of COX-2-targeting tracer and imaging approaches in order to present novel research involved in visualizing this enzyme, either in vitro or in vivo, as well as pharmacokinetic studies providing leads for radionuclide-based imaging rather than classical therapeutic interventions. In addition, we hope to stimulate an open, critical, and sound debate about the chances but also woes and sorrows, or even the pros and cons, of COX-2 as an imaging target.

There is no doubt that knowledge of the functional expression of this enzyme during the course of a disease, during therapy, and in the healing process will allow important differential diagnostic and therapeutic conclusions to be drawn. Experience in recent years with anti-inflammatory treatment selectively directed against COX-2 by selective COX-2 inhibitors, also named coxibs, has shown that mere inhibition of the enzyme is not always indicated. It is often important to modulate the activity of COX-2 to the right extent and in the right time window. The short-term use of selective COX-2 inhibitors can certainly be considered a success story with respect to less gastric irritation and decreased risk of peptic ulceration compared to non-selective inhibitors. Increasingly, combined/adjuvant approaches are also discussed, for example, to support tissue regeneration, radiosensitize tumors, or in the radioprotection of normal tissue. Long-term treatment, on the other hand, can disturb the balance in prostanoid metabolism and, thus, is often accompanied by serious side effects, particularly, affecting the vascular system.

This Special Issue therefore also aims to provide a forum for contributions that present or critically examine current developments and possibilities for application of selective COX-2 inhibitors, and then enter into an inspiring discussion on new therapeutic approaches, such as novel lead structures, dual inhibitors, adjuvant and combined therapeutic approaches, drug release aspects, and more.

This Special Issue is roughly divided into four chapters. The content of the individual submitted papers is assigned on the basis of the selected keywords, which can be found in the following list. 

Prof. Dr. Jens Pietzsch
Dr. Markus Laube
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at 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.


  • cyclooxygenases
  • adverse effects
  • inflammatory diseases
  • cancer
  • dual inhibitors
  • non-steroidal anti-inflammatory drugs
  • selective cyclooxygenase-2 inhibitors
  • pharmacokinetics
  • imaging
  • radiosynthesis
  • radiotracers
  • fluorescent probes
  • positron emission tomography (PET)
  • single-photon emission computed tomography (SPECT)
  • radiopharmacology
  • metabolic stability
  • multimodal imaging approaches
  • radiotherapeutics
  • radiomodulators
  • radiosensitizer
  • radioprotection
  • organic synthesis
  • NO donors
  • prodrugs
  • drug delivery

Published Papers

This special issue is now open for submission.
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