Structural determinants of sphingosine‐1‐phosphate receptor selectivity
Friederike Wunsch,
Trung Ngoc Nguyen,
Gerhard Wolber
et al.
Abstract:Fingolimod, the prodrug of fingolimod‐1‐phosphate (F1P), was the first sphingosine‐1‐phosphate receptor (S1PR) modulator approved for multiple sclerosis. F1P unselectively targets all five S1PR subtypes. While agonism (functional antagonism via receptor internalization) at S1PR1 leads to the desired immune modulatory effects, agonism at S1PR3 is associated with cardiac adverse effects. This motivated the development of S1PR3‐sparing compounds and led to a second generation of S1PR1,5‐selective ligands like sip… Show more
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