Affinity-Based Protein Profiling Reveals IDH2 as a Mitochondrial Target of Cannabinol in Receptor-Independent Neuroprotection.

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Tác giả: Michael Decker, Stephanie Lamer, Pamela Maher, Eva Schaller, Andreas Schlosser, Christian Stigloher

Ngôn ngữ: eng

Ký hiệu phân loại: 577 Ecology

Thông tin xuất bản: Germany : Chemistry (Weinheim an der Bergstrasse, Germany) , 2025

Mô tả vật lý:

Bộ sưu tập: NCBI

ID: 747832

Phytocannabinoids are attracting growing attention because of their potential for treatment of neurodegenerative diseases. Among them, the "minor" cannabinoid, cannabinol (CBN), has emerged as a promising neuroprotective agent, acting independently of classical cannabinoid receptors through as-yet unidentified mitochondrial targets. To uncover the molecular basis of its neuroprotective effects, we designed and synthesized a chemical probe based on CBN, incorporating a minimalist diazirine linker. Functional assays confirmed that the probe retains CBN's mitochondrial activity and exhibits strong mitochondrial enrichment, as demonstrated by fluorescence microscopy and click-correlative light and electron microscopy (click-CLEM). By affinity-based protein profiling (AfBPP), we identified isocitrate dehydrogenase 2 (IDH2) as a key mitochondrial target of CBN. This finding was further substantiated by siRNA knockdown studies, which revealed that the absence of IDH2 partially phenocopies CBN's effects, validating its role as a critical mediator of CBN's neuroprotective activity.
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