Fig. 2.

Antagonist properties of pharmacoperones, In3, Q89, TAK-013, and A17777, assessed by inhibition of buserelin-stimulated IP production. Cos-7 cells were transfected with 10 ng of DNA for (A) hWT or (B) hWT-desK¹⁹¹ GnRHR as described in Materials and Methods. IP production was measured in response to 10⁻⁹ m Buserelin (a metabolically stable GnRH agonist) and in the presence of the indicated level of four different pharmacoperones as indicated. At least three independent experiments were performed in replicates of four to six. The optimal doses of pharmacoperones were selected from earlier studies (4).