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Structure paper

TitleCSN5i-3 is an orthosteric molecular glue inhibitor of COP9 signalosome
Journal, issue, pagesNature, Year 2026
Publish dateOct 24, 2024 (structure data deposition date)
AuthorsShi H / Wang X / Yu C / Mao H / Jiao F / Braitbard M / Shor B / Zhang Z / Hinds TR / Cao S ...Shi H / Wang X / Yu C / Mao H / Jiao F / Braitbard M / Shor B / Zhang Z / Hinds TR / Cao S / Fan E / Schneidman-Duhovny D / Huang L / Zheng N
External linksNature / Search PubMed
MethodsEM (single particle)
Resolution2.96 - 4.6 Å
Structure data

EMDB-47500: Cryo-EM structure of COP9 signalosome precatalytic state with neddylated cullin-1
Method: EM (single particle) / Resolution: 3.2 Å

EMDB-47502: Focused map of COP9 signalosome precatalytic state with neddylated cullin-1
Method: EM (single particle) / Resolution: 3.2 Å

EMDB-47532, PDB-9e5z:
Cryo-EM structure of COP9 signalosome
Method: EM (single particle) / Resolution: 3.4 Å

EMDB-47660, PDB-9e77:
Cryo-EM structure of CSN-N8 in complex with CSN5i-3
Method: EM (single particle) / Resolution: 3.3 Å

EMDB-47663: Cryo-EM structure of COP9 signalosome deneddylation state with cullin-5
Method: EM (single particle) / Resolution: 3.5 Å

EMDB-47665: Focused map of COP9 signalosome deneddylation state with cullin-5
Method: EM (single particle) / Resolution: 3.7 Å

EMDB-47698, PDB-9e81:
Cryo-EM structure of COP9 signalosome in complex with CSN5i-3
Method: EM (single particle) / Resolution: 3.3 Å

EMDB-47699: Focused map of COP9 signalosome deneddylation state with cullin-4A
Method: EM (single particle) / Resolution: 3.5 Å

EMDB-47701: Cryo-EM structure of COP9 signalosome deneddylation complex with cullin-2
Method: EM (single particle) / Resolution: 3.0 Å

EMDB-47702: Focused map of COP9 signalosome deneddylation complex with cullin-2
Method: EM (single particle) / Resolution: 3.0 Å

EMDB-47729: Cryo-EM structure of CSN-N8CUL1 complex with CSN5i-3
Method: EM (single particle) / Resolution: 3.0 Å

EMDB-47767: Focused map of CSN-N8CUL1 in complex with CSN5i-3
Method: EM (single particle) / Resolution: 3.34 Å

EMDB-47776: Cryo-EM structure of COP9 signalosome deneddylation complex with cullin-3
Method: EM (single particle) / Resolution: 3.93 Å

EMDB-47976, PDB-9efm:
Cryo-EM structure of COP9 signalosome precatalytic state with neddylated cullin-1
Method: EM (single particle) / Resolution: 3.16 Å

EMDB-47977, PDB-9efq:
Cryo-EM structure of COP9 signalosome precatalytic state with neddylated cullin-2
Method: EM (single particle) / Resolution: 2.96 Å

EMDB-47981, PDB-9efv:
Cryo-EM structure of CSN-N8CUL1 in complex with CSN5i-3
Method: EM (single particle) / Resolution: 3.03 Å

EMDB-47983, PDB-9eg1:
COP9 signalosome deneddylation complex with cullin-5
Method: EM (single particle) / Resolution: 3.52 Å

EMDB-47985: Focused map of COP9 signalosome deneddylation complex with neddylated cullin-3
Method: EM (single particle) / Resolution: 4.6 Å

EMDB-47986, PDB-9eg8:
Cryo-EM structure of COP9 signalosome precatalytic state with neddylated cullin-4A
Method: EM (single particle) / Resolution: 3.39 Å

EMDB-47990, PDB-9egl:
Cryo-EM structure of COP9 signalosome precatalytic state with neddylated cullin-3
Method: EM (single particle) / Resolution: 3.93 Å

EMDB-71639, PDB-9ph4:
Cryo-EM structure of COP9 signalosome in complex with CSN5i-1a
Method: EM (single particle) / Resolution: 3.0 Å

Chemicals

ChemComp-ZN:
Unknown entry

ChemComp-6LT:
3-(difluoromethyl)-N-{6-[(5S,6S)-6-hydroxy-6,7,8,9-tetrahydro-5H-imidazo[1,5-a]azepin-5-yl][1,1'-biphenyl]-3-yl}-1-(propan-2-yl)-1H-pyrazole-5-carboxamide

PDB-1ch3:
RECOMBINANT SPERM WHALE MYOGLOBIN L89W MUTANT (MET)

Source
  • homo sapiens (human)
KeywordsMETAL BINDING PROTEIN / COP9 / COP9 signalosome / signalosome / deneddylation / CSN5 / metalloprotease / SIGNALING PROTEIN / NEDD8 / CSN5i-3 / N8CUL1 / CSN / cullin-2 / CSN-N8CUL2 / CUL2 / othosteric molecular glue / N8CUL5 / CUL5 / N8CUL4A / CUL4A / deneddylation complex / CSN5i-1a

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