3ZLI: Crystal Structure Of Jmjc Domain Of Human Histone Demethylase Uty

Citation:
Abstract
The Jumonji C lysine demethylases (KDMs) are 2-oxoglutarate- and Fe(II)-dependent oxygenases. KDM6A (UTX) and KDM6B (JMJD3) are KDM6 subfamily members that catalyze demethylation of N()-methylated histone 3 lysine 27 (H3K27), a mark important for transcriptional repression. Despite reports stating that UTY(KDM6C) is inactive as a KDM, we demonstrate by biochemical studies, employing MS and NMR, that UTY(KDM6C) is an active KDM. Crystallographic analyses reveal that the UTY(KDM6C) active site is highly conserved with those of KDM6B and KDM6A. UTY(KDM6C) catalyzes demethylation of H3K27 peptides in vitro, analogously to KDM6B and KDM6A, but with reduced activity, due to point substitutions involved in substrate binding. The results expand the set of human KDMs and will be of use in developing selective KDM inhibitors.
PDB ID: 3ZLIDownload
MMDB ID: 107871
PDB Deposition Date: 2013/1/31
Updated in MMDB: 2015/05
Experimental Method:
x-ray diffraction
Resolution: 1.8  Å
Source Organism:
Similar Structures:
Biological Unit for 3ZLI: monomeric; determined by author and by software (PISA)
Molecular Components in 3ZLI
Label Count Molecule
Protein (1 molecule)
1
Histone Demethylase UTY(Gene symbol: UTY)
Molecule annotation
Chemicals (12 molecules)
1
9
2
1
3
1
4
1
* Click molecule labels to explore molecular sequence information.

Citing MMDB
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