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TitleRational design of G-biased CB1 agonist with reduced side effects.
Journal, issue, pagesCell, Year 2026
Publish dateApr 13, 2026
AuthorsYu-Ying Liao / Jinxin Che / Yun-Tao Gao / Jianheng Xue / Linjie Li / Lin-Lin Wu / Jia-Xue Hu / Meng-Ting Hu / Linghua Xie / Huibing Zhang / Dan-Dan Shen / Yingjun Dong / Shaokun Zang / Na Zhang / Hao Wang / Yan Zhang / Xiaowu Dong / Xiao-Ming Li /
PubMed AbstractThe cannabinoid receptor 1 (CB1) has emerged as a promising candidate for next-generation non-opioid therapies. However, the development of therapeutics targeting CB1 has been consistently hindered ...The cannabinoid receptor 1 (CB1) has emerged as a promising candidate for next-generation non-opioid therapies. However, the development of therapeutics targeting CB1 has been consistently hindered by significant adverse effects. Here, through structure-activity relationship analyses focused on biased signaling, we rationally design two G-biased CB1 agonists, LZD503 and LZD505. Our design strategy employed structural spatial tuning of the agonist scaffold to disrupt specific molecular interactions and minimize steric conflicts with critical tip residues within the ligand-binding pocket, thereby promoting preferential G-pathway signaling. Cryo-electron microscopy structures of the CB1-G-protein complexes bound to these designed agonists confirmed that their anticipated conformational poses favored G-biased signaling. Both designed compounds demonstrated promising results by alleviating pain and mitigating unwanted responses in mice. The elucidated CB1 complex structures and the resulting insights establish a comprehensive framework for the structure-guided development of innovative CB1-targeted analgesics with reduced adverse effect profiles.
External linksCell / PubMed:41980782
MethodsEM (single particle)
Resolution2.42 Å
Structure data

69005

23iv

EMDB-69005, PDB-23iv:
Cannabinoid Receptor 1-Gi Complex
Method: EM (single particle) / Resolution: 2.42 Å

69006

23iw

EMDB-69006, PDB-23iw:
Cannabinoid Receptor 1-Gi Complex
Method: EM (single particle) / Resolution: 2.42 Å

Chemicals

PDB-1e5s:
Proline 3-hydroxylase (type II) - Iron form

PDB-1e5t:
PROLYL OLIGOPEPTIDASE FROM PORCINE BRAIN, MUTANT

Source
  • homo sapiens (human)
  • mus musculus (house mouse)
KeywordsMEMBRANE PROTEIN/IMMUNE SYSTEM / Cannabinoid Receptor 1 / GPCR / membrane protein / active / MEMBRANE PROTEIN-IMMUNE SYSTEM complex

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