3MTN: Usp21 In Complex With A Ubiquitin-based, Usp21-specific Inhibitor

Citation:
Abstract
The ubiquitin system regulates virtually all aspects of cellular function. We report a method to target the myriad enzymes that govern ubiquitination of protein substrates. We used massively diverse combinatorial libraries of ubiquitin variants to develop inhibitors of four deubiquitinases (DUBs) and analyzed the DUB-inhibitor complexes with crystallography. We extended the selection strategy to the ubiquitin conjugating (E2) and ubiquitin ligase (E3) enzymes and found that ubiquitin variants can also enhance enzyme activity. Last, we showed that ubiquitin variants can bind selectively to ubiquitin-binding domains. Ubiquitin variants exhibit selective function in cells and thus enable orthogonal modulation of specific enzymatic steps in the ubiquitin system.
PDB ID: 3MTNDownload
MMDB ID: 82660
PDB Deposition Date: 2010/4/30
Updated in MMDB: 2010/06
Experimental Method:
x-ray diffraction
Resolution: 2.7  Å
Source Organism:
Similar Structures:
Biological Unit for 3MTN: dimeric; determined by author and by software (PISA)
Molecular Components in 3MTN
Label Count Molecule
Proteins (2 molecules)
1
Ubiquitin Carboxyl-terminal Hydrolase 21(Gene symbol: USP21)
Molecule annotation
1
Ubiquitin Variant Ubv.21.4
Molecule annotation
Chemicals (5 molecules)
1
1
2
3
3
1
* Click molecule labels to explore molecular sequence information.

Citing MMDB
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