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- Tetrahydrocannabinol_Protein_Interaction_Landscape_in_Neuroblastoma_Cells
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Development of a Cannabinoid-Based Photoaffinity Probe to Determine the D8/9- Tetrahydrocannabinol Protein Interaction Landscape in Neuroblastoma Cells
Introduction: Δ9-Tetrahydrocannabinol (THC), the principle psychoactive ingredient in Cannabis, is widely used for its therapeutic effects in a large variety of diseases, but it also has numerous neurological side effects. The cannabinoid receptors (CBRs) are responsible to a large extent for these, but not all biological responses are mediated via the CBRs.
Objectives: The identification of additional target proteins of THC to enable a better understanding of the (adverse) physiological effects of THC.
Methods: In this study, a chemical proteomics approach using a two-step photoaffinity probe is applied to identify potential proteins that may interact with THC.
Results: Photoaffinity probe 1, containing a diazirine as a photocrosslinker, and a terminal alkyne as a ligation handle, was synthesized in 14 steps. It demonstrated high affinity for both CBRs. Subsequently, two-step photoaffinity labeling in...
Show moreIntroduction: Δ9-Tetrahydrocannabinol (THC), the principle psychoactive ingredient in Cannabis, is widely used for its therapeutic effects in a large variety of diseases, but it also has numerous neurological side effects. The cannabinoid receptors (CBRs) are responsible to a large extent for these, but not all biological responses are mediated via the CBRs.
Objectives: The identification of additional target proteins of THC to enable a better understanding of the (adverse) physiological effects of THC.
Methods: In this study, a chemical proteomics approach using a two-step photoaffinity probe is applied to identify potential proteins that may interact with THC.
Results: Photoaffinity probe 1, containing a diazirine as a photocrosslinker, and a terminal alkyne as a ligation handle, was synthesized in 14 steps. It demonstrated high affinity for both CBRs. Subsequently, two-step photoaffinity labeling in neuroblastoma cells led to identification of four potential novel protein targets of THC. The identification of these putative protein hits is a first step towards a better understanding of the protein interaction profile of THC, which could ultimately lead to the development of novel therapeutics based on THC.
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- Soethoudt, M.; Alachouzos, G.; Rooden, E.J. van; Moya Garzón, M.D.; Berg, R.J.B.H.N. van den; Heitman, L.H.; Stelt, M. van der
- Date
- 2018-12-31
- Volume
- 3
- Issue
- 1
- Pages
- 136 - 151