The sphingosine 1-phosphate receptor 2/4 antagonist JTE-013 elicits off-target effects on sphingolipid metabolism.

ABSTRACT: Sphingosine 1-phosphate (S1P) is a signaling lipid that has broad roles, working either intracellularly through various protein targets, or extracellularly via a family of five G-protein coupled receptors_. Agents that selectively and specifically target each of the S1P receptors have been sought as both biological tools and potential therapeutics. JTE-013, a small molecule antagonist of S1P receptors 2 and 4 (S1P₂ and S1P₄) has been widely used in defining the roles of these receptors in various biological processes. Indeed, our previous studies showed that JTE-013 had anti-acute myeloid leukaemia (AML) activity, supporting a role for S1P₂ in the biology and therapeutic targeting of AML. Here we examined this further and describe lipidomic analys

SUBMITTER: Pitman MR 

PROVIDER: S-EPMC8748775 | biostudies-literature | 2022 Jan

REPOSITORIES: biostudies-literature