Upon binding of LH to the external part of the membrane spanning receptor, a transduction of the signal takes place. This process results in the activation of a heterotrimeric G protein. Binding of LH to the receptor shifts its conformation. The activated receptor promotes the binding of GTP to the G protein and its subsequent activation. After binding GTP, the G protein heterotrimer detaches from the receptor and disassembles. The alpha-subunit Gs binds adenylate cyclase and activates the cAMP system.
It is believed that a receptor molecule exists in a conformational equilibrium between active and inactive states. The binding of LH (or CG) to the receptor shifts the equilibrium towards the active form of the receptor. For a cell to respond to LH only a small percentage (≈1%) of receptor sites need to be activated.