Signal transduction by HDL: agonists, receptors, and signaling cascades.
Münster, Germany. In Handb Exp Pharmacol, 2014
Several HDL-associated receptor ligands such as apolipoprotein A-I (apoA-I) or sphingosine-1-phosphate (S1P) have been identified in addition to HDL holoparticles, which interact with surface receptors such as ATP-binding cassette transporter A1 (ABCA1); S1P receptor types 1, 2, and 3 (S1P1, S1P2, and S1P3); or scavenger receptor type I (SR-BI) and activate intracellular signaling cascades encompassing kinases, phospholipases, trimeric and small G-proteins, and cytoskeletal proteins such as actin or junctional protein such as connexin43.
Identification of a Novel Agonist of the Sphingosine 1-phosphate Receptor 4 (S1P4)
Bethesda, United States. In Unknown Journal, 0001
ML248 activates S1P4 receptor with a half maximal effective concentration (EC50) of 37.7 nM–79.1 nM, and is inactive as an agonist against other members of the receptor family, with EC50s > 25 μM against S1P1, S1P2, and S1P3 receptors, and an EC50 of 2.1 μM against the S1P5 receptor.