Additional info: |
The biological effects of prostaglandin E2 (PGE2) are mediated through interaction with four distinct membrane-bound G-protein coupled EP receptors: EP1, EP2, EP3, and EP4. Binding of PGE2 to the EP4 receptor causes an increase in intracellular cAMP and subsequent relaxation of smooth muscle. In addition to sequence differences, EP4 receptors are distinguished from EP2 receptors by their insensitivity to the EP2 receptor selective agonist butaprost. The EP4 receptor is expressed in multiple human tissues including kidney, small intestine, thymus, ileum, uterus, and lung, as well as in peripheral blood leukocytes. The receptor is also expressed in cultured human blood cell lines of monocytoid (U937 and THP-1) and lymphoid (MOLT-4, Jurkat, and Raji) origin. |