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Highly Selective Drug-Derived Fluorescent Probes for the Cannabinoid Receptor Type 1 (CBR). | LitMetric

AI Article Synopsis

  • The cannabinoid receptor type 1 (CBR) plays a key role in various bodily functions, including appetite, pain, memory, and body temperature regulation, but our understanding of its cellular signaling and dynamics is limited.
  • Researchers developed new fluorescent probes for CBR by using a modular design approach that centers around a diethyl glycine-based building block, making synthesis easier and more efficient.
  • Validation of these probes through various assays supports their potential use in real-time imaging studies to explore CBR's localization, movement, and effects in different diseases.

Article Abstract

The cannabinoid receptor type 1 (CBR) is pivotal within the endocannabinoid system regulating various signaling cascades with effects in appetite regulation, pain perception, memory formation, and thermoregulation. Still, understanding of CBR's cellular signaling, distribution, and expression dynamics is very fragmentary. Real-time visualization of CBR is crucial for addressing these questions. Selective drug-like CBR ligands with a defined pharmacological profile were investigated for the construction of CBR fluorescent probes using a reverse design-approach. A modular design concept with a diethyl glycine-based building block as the centerpiece allowed for the straightforward synthesis of novel probe candidates. Validated by computational docking studies, radioligand binding, and cAMP assay, this systematic approach allowed for the identification of novel pyrrole-based CBR fluorescent probes. Application in fluorescence-based target-engagement studies and live cell imaging exemplify the great versatility of the tailored CBR probes for investigating CBR localization, trafficking, pharmacology, and its pathological implications.

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Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC11284800PMC
http://dx.doi.org/10.1021/acs.jmedchem.4c00465DOI Listing

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