› 5t35

X-ray diffraction
2.7Å resolution

The PROTAC MZ1 in complex with the second bromodomain of Brd4 and pVHL:ElonginC:ElonginB

Released:
DOI: 10.2210/pdb5t35/pdb
PDB entry 5t35 coloured by chain, front view.
PDB entry 5t35 coloured by chain, side view.
PDB entry 5t35 coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Structural basis of PROTAC cooperative recognition for selective protein degradation.
Gadd MS, Testa A, Lucas X, Chan KH, Chen W, Lamont DJ, Zengerle M, Ciulli A
Nat Chem Biol 13 514-521 (2017)
PMID: 28288108

Function and Biology Details

Biochemical function:
  • not assigned
Biological process:
Cellular component:
Sequence domains:

Structure analysis Details

Assembly composition:
hetero tetramer (preferred)
PDBe Complex ID:
PDB-CPX-130120 (preferred)
Entry contents:
4 distinct polypeptide molecules
Macromolecules (4 distinct):
Bromodomain-containing protein 4 Chains: A, E
Molecule details ›
Chains: A, E
Length: 130 amino acids
Theoretical weight: 15.06 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli BL21(DE3)
UniProt:
  • Canonical: O60885 (Residues: 333-460; Coverage: 9%)
Gene names: BRD4, HUNK1
Sequence domains: Bromodomain
Structure domains: Bromodomain-like
Elongin-B Chains: B, F
Molecule details ›
Chains: B, F
Length: 104 amino acids
Theoretical weight: 11.75 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli BL21(DE3)
UniProt:
  • Canonical: Q15370 (Residues: 1-104; Coverage: 88%)
Gene names: ELOB, TCEB2
Sequence domains: Ubiquitin family
Structure domains: Phosphatidylinositol 3-kinase Catalytic Subunit; Chain A, domain 1
Elongin-C Chains: C, G
Molecule details ›
Chains: C, G
Length: 97 amino acids
Theoretical weight: 10.97 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli BL21(DE3)
UniProt:
  • Canonical: Q15369 (Residues: 17-112; Coverage: 86%)
Gene names: ELOC, TCEB1
Sequence domains: Skp1 family, tetramerisation domain
Structure domains: Potassium Channel Kv1.1; Chain A
von Hippel-Lindau disease tumor suppressor Chains: D, H
Molecule details ›
Chains: D, H
Length: 162 amino acids
Theoretical weight: 18.7 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli BL21(DE3)
UniProt:
  • Canonical: P40337 (Residues: 54-213; Coverage: 75%)
Gene name: VHL
Sequence domains:
Structure domains:

Ligands and Environments

1 bound ligand:
Ligand 759 2 x 759
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: DIAMOND BEAMLINE I04-1
Spacegroup: P32
Unit cell:
a: 102.306Å b: 102.306Å c: 144.329Å
α: 90° β: 90° γ: 120°
R-values:
R R work R free
0.207 0.206 0.231
Expression system: Escherichia coli BL21(DE3)

Quick links

Citations

108 review citations

Kinase inhibitors: the road ahead.
Ferguson et al. (2018)
107 more

43 mentions without citation

PROTAC targeted protein degraders: the past is prologue.
Békés et al. (2022)
42 more