Discovery and synthetic optimization of a novel scaffold for hydrophobic tunnel-targeted autotaxin inhibition

Autotaxin (ATX) is a ubiquitous ectoenzyme that hydrolyzes lysophosphatidylcholine (LPC) to form the bioactive lipid mediator lysophosphatidic acid (LPA). LPA activates specific G-protein coupled receptors to elicit downstream effects leading to cellular motility, survival, and invasion. Through the...

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Pubblicato in:Bioorg Med Chem
Autori principali: Ragle, Lauren E., Palanisamy, Dilip J., Joe, Margaux J., Stein, Rachel S., Norman, Derek D., Tigyi, Gabor, Baker, Daniel L., Parrill, Abby L.
Natura: Artigo
Lingua:Inglês
Pubblicazione: 2016
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Article
Accesso online:https://ncbi.nlm.nih.gov/pmc/articles/PMC5023007/
https://ncbi.nlm.nih.gov/pubmed/27544588
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmc.2016.08.004
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