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Novel Potent Selective Orally Active S1P5 Receptor Antagonists.

ABSTRACT: S1P5 is one of the five sphingosine-1-phosphate (S1P) receptors which play important roles in immune and CNS cell homeostasis, growth, and differentiation. Little is known about the effect of modulation of S1P5 due to the lack of S1P5 specific modulators with suitable druglike properties. Here we describe the discovery and optimization of a novel series of potent selective S1P5 antagonists and the identification of an orally active brain-penetrant tool compound 15.

SUBMITTER: Ma B

PROVIDER: S-EPMC7957944 | biostudies-literature | 2021 Mar

REPOSITORIES: biostudies-literature

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Novel Potent Selective Orally Active S1P5 Receptor Antagonists.

Ma Bin B Guckian Kevin M KM Liu Xiao-Gao XG Yang Chunhua C Li Bing B Scannevin Robert R Mingueneau Michaël M Drouillard Annabelle A Walzer Thierry T

ACS medicinal chemistry letters 20210115 3

S1P5 is one of the five sphingosine-1-phosphate (S1P) receptors which play important roles in immune and CNS cell homeostasis, growth, and differentiation. Little is known about the effect of modulation of S1P5 due to the lack of S1P5 specific modulators with suitable druglike properties. Here we describe the discovery and optimization of a novel series of potent selective S1P5 antagonists and the identification of an orally active brain-penetrant tool compound <b>15</b>. ...[more]

PMID: 33738061

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