MAS1L Activators

Chemical activators of the MAS1L protein include a variety of compounds that engage different signaling pathways, leading to the functional activation of this G-protein-coupled receptor (GPCR). Angiotensin II, a potent vasoconstrictor peptide hormone, can activate MAS1L by binding to its receptors, which triggers the intracellular IP3/DAG pathway that culminates in the release of calcium from intracellular stores. Similarly, lysophosphatidic acid and endothelin-1 also operate through GPCR-mediated activation of phospholipase C, resulting in the production of IP3 and the subsequent increase of intracellular calcium levels, which can activate MAS1L. Sphingosine-1-phosphate, another lipid mediator, engages GPCRs that can activate the Rho/Rac pathway, which may lead to MAS1L activation through alterations in cytoskeletal dynamics.

Furthermore, thrombin, a serine protease, activates protease-activated receptors (PARs) that can lead to MAS1L activation through G-protein signaling pathways that involve the mobilization of calcium. Bradykinin, acting through its B2 receptors, and norepinephrine, through alpha-adrenergic receptors, both result in elevated intracellular calcium, which can activate MAS1L. Chemicals like aluminium fluoride stabilize G-proteins in their active form, potentially leading to MAS1L activation via changes in intracellular cAMP or calcium levels. The calcium ionophore A23187 directly increases intracellular calcium concentration, activating MAS1L. The peptide melittin stimulates phospholipase A2, leading to eicosanoid production, which can activate GPCRs and in turn MAS1L. U46619, a synthetic analog of thromboxane A2, activates thromboxane receptors and engages G-protein signaling pathways. Lastly, arginine vasopressin, by binding to vasopressin receptors, also causes an increase in intracellular calcium levels, which can lead to the activation of MAS1L.