Targeting the NLRP3: From Novel Inhibitor Design to Clinic Trials and Therapeutic Applications
A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Biopharmaceuticals".
Deadline for manuscript submissions: 31 May 2026 | Viewed by 213
Special Issue Editors
Interests: inflammatory; anticancer; drug discovery; PET tracer; medicinal chemistry; photoaffinity labeling; inflammasome; GSDMD
Interests: design and synthesis of chemical probes for epigenetic modification enzymes; development of chemical tools to study DNA modifications; targeting NAD metabolism for drug discovery
Special Issues, Collections and Topics in MDPI journals
Special Issue Information
Dear Colleagues,
The NLRP3 inflammasome is a multiprotein complex that plays a critical role in mediating immune responses and maintaining homeostasis in the presence of pathogenic threats and danger signals. Dysregulated activation of NLRP3 has been implicated in a wide range of pathophysiological conditions, including metabolic disorders (diabetes, obesity, gout), cardiovascular diseases (atherosclerosis), neurological disorders (Alzheimer’s disease, Parkinson’s disease, multiple sclerosis), and autoinflammatory syndromes (CAPS), as well as various cancers and chronic inflammatory diseases. These associations underscore its importance as a promising therapeutic target.
The activation of the NLRP3 inflammasome occurs through two sequential steps: priming and activation. Interference with this process can involve multiple molecular targets and events, including transcriptional regulation (e.g., via Toll-like receptor signaling), post-translational modifications (PTMs), and intracellular mechanisms such as K⁺ efflux, mitochondrial dysfunction, reactive oxygen species (ROS) production, and lysosomal disruption. In addition, targeting the disruption of inflammasome complex assembly, caspase-1 activation, and gasdermin D (GSDMD) cleavage represents an effective strategy for inhibiting NLRP3 inflammasome activation. In comparison, the direct inhibition of NLRP3 offers more precise control over the inflammatory cascade, potentially minimizing the off-target effects associated with less specific strategies. Consequently, the development of highly selective, direct NLRP3 inhibitors has emerged as a major focus in drug discovery.
This Special Issue will showcase papers highlighting the latest advances in the development of direct NLRP3 inhibitors, particularly those that have entered clinical trials, as well as their emerging therapeutic applications.
Dr. Yiming Xu
Dr. Yana Cen
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 250 words) can be sent to the Editorial Office for assessment.
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. Pharmaceuticals 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 2900 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
- NLRP3 inflammasome
- selective and direct NLRP3 inhibitors
- drug discovery
- clinical trial
- therapeutic applications
Benefits of Publishing in a Special Issue
- Ease of navigation: Grouping papers by topic helps scholars navigate broad scope journals more efficiently.
- Greater discoverability: Special Issues support the reach and impact of scientific research. Articles in Special Issues are more discoverable and cited more frequently.
- Expansion of research network: Special Issues facilitate connections among authors, fostering scientific collaborations.
- External promotion: Articles in Special Issues are often promoted through the journal's social media, increasing their visibility.
- Reprint: MDPI Books provides the opportunity to republish successful Special Issues in book format, both online and in print.
Further information on MDPI's Special Issue policies can be found here.
