3ZCW: EG5 - NEW Allosteric Binding Site

Citation:
Abstract
Human kinesin Eg5 is a target for drug development in cancer chemotherapy with compounds in phase II clinical trials. These agents bind to a well-characterized allosteric pocket involving the loop L5 region, a structural element in kinesin-5 family members thought to provide inhibitor specificity. Using X-ray crystallography, kinetic, and biophysical methods, we have identified and characterized a distinct allosteric pocket in Eg5 able to bind inhibitors with nanomolar K(d). This pocket is formed by key structural elements thought to be pivotal for force generation in kinesins and may represent a novel site for therapeutic intervention in this increasingly well-validated drug target.
PDB ID: 3ZCWDownload
MMDB ID: 106854
PDB Deposition Date: 2012/11/23
Updated in MMDB: 2013/02
Experimental Method:
x-ray diffraction
Resolution: 1.69  Å
Source Organism:
Similar Structures:
Biological Unit for 3ZCW: monomeric; determined by author and by software (PISA)
Molecular Components in 3ZCW
Label Count Molecule
Protein (1 molecule)
1
Kinesin-like Protein Kif11(Gene symbol: KIF11)
Molecule annotation
Chemicals (6 molecules)
1
1
2
1
3
2
4
1
5
1
* Click molecule labels to explore molecular sequence information.

Citing MMDB
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