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. 2012 May 9;112(5):2593-603.
doi: 10.1021/cr2003213. Epub 2012 Feb 15.

Chemical Evolution of Autotaxin Inhibitors

Free PMC article

Chemical Evolution of Autotaxin Inhibitors

Harald M H G Albers et al. Chem Rev. .
Free PMC article


Scheme 1
Scheme 1. ATX Is Responsible for Hydrolyzing LPC into LPA in an Extracellular Environment
This reaction is catalyzed by a threonine residue and two zinc ions present in the ATX active site. LPA activates specific G-protein-coupled receptors stimulating migration, proliferation, and survival of cells. ATX is displayed as a cartoon representation of an ATX crystal structure (PDB ID 2XR9) with the SMB domains in purple, the PDE domain in green, and the nuclease-like domain in blue.
Figure 1
Figure 1
Identified natural substrates of ATX.
Scheme 2
Scheme 2. Labeling Mechanism of ATX with ATX-ABP
Only one of the potential labeled products resulting from the labeling is shown.
Figure 2
Figure 2
The inhibitor liganded ATX structure (PDB ID 2XRG). (A) Binding of HA155 with ATX. (B) Boronic acid in HA155 targeting the threonine (Thr) oxygen nucleophile and two zinc ions in the ATX active site.

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