Skip to main page content
Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
Review
. 2012 May 9;112(5):2593-603.
doi: 10.1021/cr2003213. Epub 2012 Feb 15.

Chemical Evolution of Autotaxin Inhibitors

Affiliations
Free PMC article
Review

Chemical Evolution of Autotaxin Inhibitors

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

Figures

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.

Similar articles

See all similar articles

Cited by 18 articles

See all "Cited by" articles

References

    1. Stracke M. L.; Krutzsch H. C.; Unsworth E. J.; Arestad A.; Cioce V.; Schiffmann E.; Liotta L. A. J. Biol. Chem. 1992, 267, 2524. - PubMed
    1. Stefan C.; Jansen S.; Bollen M. Purinergic Signalling 2006, 2, 361. - PMC - PubMed
    1. Tokumura A.; Majima E.; Kariya Y.; Tominaga K.; Kogure K.; Yasuda K.; Fukuzawa K. J. Biol. Chem. 2002, 277, 39436. - PubMed
    1. Umezu-Goto M.; Kishi Y.; Taira A.; Hama K.; Dohmae N.; Takio K.; Yamori T.; Mills G. B.; Inoue K.; Aoki J.; Arai H. J. Cell Biol. 2002, 158, 227. - PMC - PubMed
    1. Noguchi K.; Herr D.; Mutoh T.; Chun J. Curr. Opin. Pharmacol. 2009, 9, 15. - PubMed

Publication types

MeSH terms

Substances

LinkOut - more resources

Feedback