This technology is a CNS-focused P2X7 receptor antagonist platform based on urea and carbamate chemotypes that enables functional modulation of neuroinflammatory signaling.
By targeting the allosteric portal of the central pocket (PCP), the compounds suppress P2X7-mediated calcium signaling and IL-1β secretion without nonspecific cytotoxicity.
The approach overcomes limitations of rigid P2X7 antagonists developed for peripheral inflammation.
It provides a differentiated strategy for disease-modifying therapies in neuroinflammation-associated CNS disorders.
Chronic CNS neuroinflammation is increasingly recognized as an upstream driver of disorders such as depression, Parkinson’s disease, and Alzheimer’s disease, where conventional symptom-focused therapies show limited efficacy. P2X7 receptor–mediated activation of the NLRP3 inflammasome plays a central role in IL-1β release, microglial activation, and downstream neurotoxic signaling.
This platform introduces urea- and carbamate-based allosteric antagonists that bind to the portal of the central pocket (PCP) of P2X7, a site distinct from the ATP-binding domain. The flexible chemotypes are designed to accommodate structural heterogeneity across PCP sub-pockets, enabling stable modulation of channel gating and preferential stabilization of non-conductive P2X7 states.
Lead compounds demonstrate dose-dependent inhibition of Bz-ATP–induced P2X7 activation, suppressing calcium-dependent signaling and IL-1β secretion while preserving intracellular IL-1β production and ERK signaling, indicating functional selectivity rather than nonspecific inhibition. This mechanism supports CNS-relevant efficacy with an improved safety profile.
The platform supports chemotype expansion, P2X7-specific functional validation, and CNS-relevant translational frameworks linked to neuroinflammatory subtypes and biomarkers. Commercialization opportunities include staged IP licensing and collaborative preclinical R&D with pharmaceutical and biotech partners developing disease-modifying therapies for CNS neuroinflammation.
IBU Inc. is a technology commercialization and consulting firm supporting licensing, co-development, and venture creation based on deep-tech and research-originated technologies.
The company operates as a technology transfer partner, startup studio, and accelerator, working with universities, research institutes, and industry players.
IBU Inc. connects technology owners with corporate partners and investors by structuring collaboration models, commercialization strategies, and market-oriented pathways.
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