Literature & Media

Designing Small Molecule Inhibitors for Autotaxin

Case Study

PharmAkea, a startup biotechnology company located in San Diego, California, contacted Cayman Chemical to help determine the mode of binding for their small molecule autotaxin (ATX) inhibitors.
  • Cayman Chemical’s structural biologists provided a drug discovery platform for the generation of small molecule autotaxin (ATX) inhibitors using their gene-to-structure pipeline.
  • Crystal structures of mutant human ATX in complex with four structurally distinct ATX inhibitors are presented.
  • Crystal structures confirm the unique mechanisms of inhibition displayed by ATX.
  • A crystal structure with arachidonic acid (AA) represents the first ATX structure containing a substrate-bound secondary lysophosphatidic acid (LPA) binding site.
  • This work enhanced our client’s drug discovery efforts, leading to a clinical candidate.
To cite this case study: Stein, A.J., Bain, G., Prodanovich, P., et al. Designing small molecule inhibitors for autotaxin. Case Study: Structural Biology Services, Cayman Chemical (2018).
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Designing Small Molecule Inhibitors for Autotaxin<br>
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