Nature Communications (Mar 2023)
Structural basis of selective cannabinoid CB2 receptor activation
- Xiaoting Li,
- Hao Chang,
- Jara Bouma,
- Laura V. de Paus,
- Partha Mukhopadhyay,
- Janos Paloczi,
- Mohammed Mustafa,
- Cas van der Horst,
- Sanjay Sunil Kumar,
- Lijie Wu,
- Yanan Yu,
- Richard J. B. H. N. van den Berg,
- Antonius P. A. Janssen,
- Aron Lichtman,
- Zhi-Jie Liu,
- Pal Pacher,
- Mario van der Stelt,
- Laura H. Heitman,
- Tian Hua
Affiliations
- Xiaoting Li
- iHuman Institute, ShanghaiTech University
- Hao Chang
- iHuman Institute, ShanghaiTech University
- Jara Bouma
- Division of Drug Discovery and Safety, Leiden Academic Center for Drug Research, Leiden University, Oncode Institute
- Laura V. de Paus
- Department of Molecular Physiology, Leiden Institute of Chemistry, Leiden University, Oncode Institute
- Partha Mukhopadhyay
- Laboratory of Cardiovascular Physiology and Tissue Injury, National Institute of Health/National Institute on Alcohol Abuse and Alcoholism
- Janos Paloczi
- Laboratory of Cardiovascular Physiology and Tissue Injury, National Institute of Health/National Institute on Alcohol Abuse and Alcoholism
- Mohammed Mustafa
- Department of Pharmacology and Toxicology, Virginia Commonwealth University
- Cas van der Horst
- Division of Drug Discovery and Safety, Leiden Academic Center for Drug Research, Leiden University, Oncode Institute
- Sanjay Sunil Kumar
- Division of Drug Discovery and Safety, Leiden Academic Center for Drug Research, Leiden University, Oncode Institute
- Lijie Wu
- iHuman Institute, ShanghaiTech University
- Yanan Yu
- iHuman Institute, ShanghaiTech University
- Richard J. B. H. N. van den Berg
- Department of Molecular Physiology, Leiden Institute of Chemistry, Leiden University, Oncode Institute
- Antonius P. A. Janssen
- Department of Molecular Physiology, Leiden Institute of Chemistry, Leiden University, Oncode Institute
- Aron Lichtman
- Department of Pharmacology and Toxicology, Virginia Commonwealth University
- Zhi-Jie Liu
- iHuman Institute, ShanghaiTech University
- Pal Pacher
- Laboratory of Cardiovascular Physiology and Tissue Injury, National Institute of Health/National Institute on Alcohol Abuse and Alcoholism
- Mario van der Stelt
- Department of Molecular Physiology, Leiden Institute of Chemistry, Leiden University, Oncode Institute
- Laura H. Heitman
- Division of Drug Discovery and Safety, Leiden Academic Center for Drug Research, Leiden University, Oncode Institute
- Tian Hua
- iHuman Institute, ShanghaiTech University
- DOI
- https://doi.org/10.1038/s41467-023-37112-9
- Journal volume & issue
-
Vol. 14,
no. 1
pp. 1 – 16
Abstract
Cannabinoid CB2 receptor (CB2R) agonists are investigated as therapeutic agents in the clinic. Here, authors report the discovery of LEI-102, a CB2R agonist, used in conjunction with three other CBR ligands (APD371, HU308, and CP55,940) to investigate selective CB2R activation.
