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2012 Feb 1;40(1):31–6. Role of autotaxin in cancer stem cells. Autotaxin has lysophospholipase D activity leading to tumor cell growth and motility by lysophosphatidic acid production. The Journal of CellBiology. Structure–Activity Relationships of SmallMolecule Autotaxin Inhibitors with a Discrete Binding Mode.
Traditionally, drug discovery has focused on small-molecule therapeutics, typically with a molecular weight of less than 500 Daltons. 2 Typically, small-molecule drugs target active sites buried inside proteins. What are macrocycles and why are they interesting for drug discovery?
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