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TitleLigand and G-protein selectivity in the κ-opioid receptor.
Journal, issue, pagesNature, Vol. 617, Issue 7960, Page 417-425, Year 2023
Publish dateMay 3, 2023
AuthorsJianming Han / Jingying Zhang / Antonina L Nazarova / Sarah M Bernhard / Brian E Krumm / Lei Zhao / Jordy Homing Lam / Vipin A Rangari / Susruta Majumdar / David E Nichols / Vsevolod Katritch / Peng Yuan / Jonathan F Fay / Tao Che /
PubMed AbstractThe κ-opioid receptor (KOR) represents a highly desirable therapeutic target for treating not only pain but also addiction and affective disorders. However, the development of KOR analgesics has ...The κ-opioid receptor (KOR) represents a highly desirable therapeutic target for treating not only pain but also addiction and affective disorders. However, the development of KOR analgesics has been hindered by the associated hallucinogenic side effects. The initiation of KOR signalling requires the G-family proteins including the conventional (G, G, G, G and G) and nonconventional (G and G) subtypes. How hallucinogens exert their actions through KOR and how KOR determines G-protein subtype selectivity are not well understood. Here we determined the active-state structures of KOR in a complex with multiple G-protein heterotrimers-G, G, G and G-using cryo-electron microscopy. The KOR-G-protein complexes are bound to hallucinogenic salvinorins or highly selective KOR agonists. Comparisons of these structures reveal molecular determinants critical for KOR-G-protein interactions as well as key elements governing G-family subtype selectivity and KOR ligand selectivity. Furthermore, the four G-protein subtypes display an intrinsically different binding affinity and allosteric activity on agonist binding at KOR. These results provide insights into the actions of opioids and G-protein-coupling specificity at KOR and establish a foundation to examine the therapeutic potential of pathway-selective agonists of KOR.
External linksNature / PubMed:37138078 / PubMed Central
MethodsEM (single particle)
Resolution2.61 - 2.82 Å
Structure data

27804

8dzp

EMDB-27804, PDB-8dzp:
momSalB bound Kappa Opioid Receptor in complex with Gi1
Method: EM (single particle) / Resolution: 2.71 Å

27805

8dzq

EMDB-27805, PDB-8dzq:
momSalB bound Kappa Opioid Receptor in complex with GoA
Method: EM (single particle) / Resolution: 2.82 Å

27806

8dzr

EMDB-27806, PDB-8dzr:
GR89,696 bound Kappa Opioid Receptor in complex with gustducin
Method: EM (single particle) / Resolution: 2.61 Å

27807

8dzs

EMDB-27807, PDB-8dzs:
GR89,696 bound Kappa Opioid Receptor in complex with Gz
Method: EM (single particle) / Resolution: 2.65 Å

EMDB-41876: momSalB bound Kappa Opioid Receptor in complex with GoA
Method: EM (single particle) / Resolution: 2.8 Å

EMDB-43732: momSalB bound Kappa Opioid Receptor in complex Gi1
Method: EM (single particle) / Resolution: 2.71 Å

EMDB-43733: GR89,696 bound Kappa Opioid Receptor in complex with Gz
Method: EM (single particle) / Resolution: 2.73 Å

EMDB-43734: GR89,696 bound Kappa Opioid Receptor in complex with gustducin
Method: EM (single particle) / Resolution: 2.72 Å

Chemicals

ChemComp-U99:
methyl (2S,4aR,6aR,7R,9S,10aS,10bR)-2-(furan-3-yl)-9-(methoxymethoxy)-6a,10b-dimethyl-4,10-dioxododecahydro-2H-naphtho[2,1-c]pyran-7-carboxylate

ChemComp-U9I:
methyl (3R)-4-[(3,4-dichlorophenyl)acetyl]-3-[(pyrrolidin-1-yl)methyl]piperazine-1-carboxylate

Source
  • homo sapiens (human)
  • mus musculus (house mouse)
KeywordsMEMBRANE PROTEIN / GPCR / KAPPA OPIOID Receptor / SALVINORIN / Receptor / Kappa / KOR / Opioid / G protein

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