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TRP Channels for Pain, Itch and Inflammation Relief: 2nd Edition
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TRP Channels for Pain, Itch and Inflammation Relief: 2nd Edition

A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Molecular Immunology".

Deadline for manuscript submissions: 20 September 2025 | Viewed by 4068

Special Issue Editors

Dr. Arpad Szallasi

E-Mail Website
Guest Editor
Department of Pathology and Experimental Cancer Research, Faculty of Medicine, Semmelweis University, Budapest, Hungary
Interests: the capsaicin (vanilloid) receptor TRPV1; "thermoTRP" expression in cancer; TRP channels as oncotargets; TRP channels as tumor suppressors; sensory nerve-tumor interactions; oncothermia
Special Issues, Collections and Topics in MDPI journals
Dr. Ari-Pekka Koivisto

E-Mail Website
Guest Editor
Research and Development, Orion Corporation Orion Pharma, 20360 Turku, Finland
Interests: TRPA1; TRP ion channels; drug discovery; cardiac electrophysiology; chronic pain; neuropathic and osteoarthritis pain
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

This is a continued series of the hot topic of TRP Channels for Pain, Itch and Inflammation Relief. We already have done a successful special issue that received interesting contributions and discussions (https://www.mdpi.com/journal/ijms/special_issues/TRP_Pain_Itch_Inflammation).

Transient Receptor Potential (TRP) channels are multifunctional signaling molecules with important roles in sensory perception and cellular physiology. More than two decades of intensive preclinical and clinical research supports the involvement of TRP channels in pain, itch, and neurogenic inflammation. In fact, a number of potent small molecule TRPA1 and TRPV1 antagonists have already been advanced into clinical trials for the treatment of inflammatory and neuropathic pain. Other TRP channels (e.g., TRPV2, TRPV3, TRPM2, TRPM3, TRPM8 and TRPC4/C5) are also of significant interest.

This Special Issue will review the preclinical promise and therapeutic value of TRP channel modulators aimed both established and emerging targets, along with the challenges that these compounds may face in clinical practice. Experimental and clinical studies with pain, itch and inflammation will be discussed, along with the emerging roles of TRP gene polymorphism and epigenetic regulation in disease risk and altered sensory perception. Critical review articles of old concepts and new thoughts are also welcome for consideration.

Dr. Arpad Szallasi
Dr. Ari-Pekka Koivisto
Guest Editors

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 submissions that pass pre-check are 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 semimonthly journal published by MDPI.

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Keywords

  • TRP channels
  • “thermoTRP” channels
  • neuropathic pain
  • inflammatory pain
  • cancer pain
  • pruritic skin iseases
  • itch
  • neurogenic inflammation
  • migraine

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Published Papers (2 papers)

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12 pages, 1754 KiB  
Article
Three-Dimensional Quantitative Structure–Activity Relationship Study of Transient Receptor Potential Vanilloid 1 Channel Antagonists Reveals Potential for Drug Design Purposes
by Beatrice Gianibbi, Anna Visibelli, Giacomo Spinsanti and Ottavia Spiga
Int. J. Mol. Sci. 2024, 25(14), 7951; https://doi.org/10.3390/ijms25147951 - 21 Jul 2024
Viewed by 1110
Abstract
Transient receptor potential vanilloid 1 (TRPV1) was reported to be a putative target for recovery from chronic pain, producing analgesic effects after its inhibition. A series of drug candidates were previously developed, without the ability to ameliorate the therapeutic outcome. Starting from previously [...] Read more.
Transient receptor potential vanilloid 1 (TRPV1) was reported to be a putative target for recovery from chronic pain, producing analgesic effects after its inhibition. A series of drug candidates were previously developed, without the ability to ameliorate the therapeutic outcome. Starting from previously designed compounds, derived from the hybridization of antagonist SB-705498 and partial agonist MDR-652, we performed a virtual screening on a pharmacophore model built by exploiting the Cryo-EM 3D structure of a nanomolar antagonist in complex with the human TRPV1 channel. The pharmacophore model was described by three pharmacophoric features, taking advantage of both the bioactive pose of the antagonist and the receptor exclusion spheres. The results of the screening were implemented inside a 3D-QSAR model, correlating with the negative decadic logarithm of the inhibition rate of the ligands. After the validation of the obtained 3D-QSAR model, we designed a new series of compounds by introducing key modifications on the original scaffold. Again, we determined the compounds’ binding poses after alignment to the pharmacophoric model, and we predicted their inhibition rates with the validated 3D-QSAR model. The obtained values resulted in being even more promising than parent compounds, demonstrating that ongoing research still leaves much room for improvement. Full article
(This article belongs to the Special Issue TRP Channels for Pain, Itch and Inflammation Relief: 2nd Edition)
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Review

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28 pages, 2059 KiB  
Review
The Role of TRP Channels in Sepsis and Colitis
by Kristina A. Dvornikova, Olga N. Platonova and Elena Y. Bystrova
Int. J. Mol. Sci. 2024, 25(9), 4784; https://doi.org/10.3390/ijms25094784 - 27 Apr 2024
Cited by 2 | Viewed by 2007
Abstract
To date, several members of the transient receptor potential (TRP) channels which provide a wide array of roles have been found in the gastrointestinal tract (GI). The goal of earlier research was to comprehend the intricate signaling cascades that contribute to TRP channel [...] Read more.
To date, several members of the transient receptor potential (TRP) channels which provide a wide array of roles have been found in the gastrointestinal tract (GI). The goal of earlier research was to comprehend the intricate signaling cascades that contribute to TRP channel activation as well as how these receptors’ activity affects other systems. Moreover, there is a large volume of published studies describing the role of TRP channels in a number of pathological disorders, including inflammatory bowel disease (IBD) and sepsis. Nevertheless, the generalizability of these results is subject to certain limitations. For instance, the study of IBD relies on various animal models and experimental methods, which are unable to precisely imitate the multifactorial chronic disease. The diverse pathophysiological mechanisms and unique susceptibility of animals may account for the inconsistency of the experimental data collected. The main purpose of this study was to conduct a comprehensive review and analysis of existing studies on transient receptor potential (TRP) channels implicating specific models of colitis and sepsis, with particular emphasis on their involvement in pathological disorders such as IBD and sepsis. Furthermore, the text endeavors to evaluate the generalizability of experimental findings, taking into consideration the limitations posed by animal models and experimental methodologies. Finally, we also provide an updated schematic of the most important and possible molecular signaling pathways associated with TRP channels in IBD and sepsis. Full article
(This article belongs to the Special Issue TRP Channels for Pain, Itch and Inflammation Relief: 2nd Edition)
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