N-Adamantyl-1-Pentyl-4-Oxo-1,4-Dihydroquinoline-3-Carboxamide and N-(Adamantan-1-Yl)-2-(Alkyloxy)benzamide Derivatives as Fluorescent Probes for Selective CB2R Targeting

Gabriella Rosanna Musillo, Giovanni Graziano, Mariachiara Mammone, Francesco Mastropasqua, Maria Majellaro, Claudia Gioè-Gallo +12 more

Background/Objectives: The cannabinoid receptor subtype 2 (CB2R) is an increasingly important therapeutic and diagnostic target because of its involvement in inflammation-associated disorders, including cancer and neurodegenerative diseases. CB2R biology has traditionally been investigated using radioligands, whose broader application is limited by safety, regulatory, operational, and environmental constraints. Fl…

CC48 a new CB2R agonist/FAAH inhibitor dual drug blocks gastric cancer progression and overcomes paclitaxel resistance.

Annalisa Schirizzi, Natasha Renna, Giampiero De Leonardis, Rosangela Montanaro, Francesco Mastropasqua, Giovanni Graziano +13 more

Gastric cancer (GC) has poor survival in advanced stages, with limited treatment options. Paclitaxel (PTX) is commonly used, but resistance often arises, highlighting the need for targeted therapies. Cannabinoid receptor type 2 (CB2R) is overexpressed in several cancers and its activation has been associated with reduced tumor growth and metastasis. This study evaluated the antitumor activity of selected CB2R agon…

Identification of a Cannabinoid Receptor 2 Allosteric Site Using Computational Modeling and Pharmacological Analysis.

Zara Farooq, Pietro Delre, Stylianos Iliadis, Giuseppe Felice Mangiatordi, Marialessandra Contino, Lesley A. Howell +1 more

Emerging evidence has demonstrated that cannabinoid receptor 2 (CB2) is involved in a number of diseases, such as neurodegenerative disorders and various types of cancer, making it an attractive pharmacological target. Classically, a protein active site or an orthosteric binding site, where the endogenous ligand binds to, is used as a target for the design of most small-molecule drugs. This can present challenges…

Role of Cannabidiol for Improvement of the Quality of Life in Cancer Patients: Potential and Challenges.

Ryan Green, Roukiah Khalil, Shyam S Mohapatra, Subhra Mohapatra, Marialessandra Contino

There is currently a growing interest in the use of cannabidiol (CBD) to alleviate the symptoms caused by cancer, including pain, sleep disruption, and anxiety. CBD is often self-administered as an over-the-counter supplement, and patients have reported benefits from its use. However, despite the progress made, the mechanisms underlying CBD's anti-cancer activity remain divergent and unclear. Herein, we provide a…

Editorial: The Canonical and Non-Canonical Endocannabinoid System as a Target in Cancer and Acute and Chronic Pain.

Marialessandra Contino, Peter J. McCormick

Editorial: The CB2 Cannabinoid System: A New Strategy in Neurodegenerative Disorder and Neuroinflammation.

Marialessandra Contino, Elena Capparelli, Nicola A Colabufo, Ashley I Bush