Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 60, Issue 5, Pages 2006-2017Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.6b01743
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Funding
- NINO [700.10.354]
- GlaxoSmithKline
- EPRSC [EP/L505080/1]
- Scottish Funding Council
- NIH [1R01HL120507]
- VA [BX001984-01]
- DOD [BC150305P1]
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Autotaxin produces the bioactive lipid lysophosphatidic acid (LPA) and is a drug target of considerable interest for numerous pathologies. We report the expedient, structure-guided evolution of weak physiological allosteric inhibitors (bile salts) into potent competitive Autotaxin inhibitors that do not interact with the catalytic site. Functional data confirms that our lead compound attenuates LPA mediated signaling in cells and reduces LPA synthesis in vivo, providing a promising natural product derived scaffold for drug discovery.
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