Figure 2.
Activation of FSHR. Based on the recent crystal structure (77), FSHR exists as trimer in the basal state (A). FSH binding leads to dissociation and activation of the receptor (B). Due to the bulky glycan, only one FSH can bind to the trimeric FSHR. Small molecule modulators by binding to the allosteric site in the transmembrane domain opens up the receptor and enables three FSH binding (C). On the other hand, three deglycosylated FSH can bind to the trimeric receptor without dissociation and activation of the receptor (D).