Allosteric and orthosteric binding modes of two nonpeptide human gonadotropin-releasing hormone receptor antagonists.

@article{Sullivan2006AllostericAO,
  title={Allosteric and orthosteric binding modes of two nonpeptide human gonadotropin-releasing hormone receptor antagonists.},
  author={Susan Kring Sullivan and Michael Scott Brown and Yinghong Gao and Colin J. Loweth and Francisco M. Lio and Paul D Crowe and Raymond Struthers and Stephen F. Betz},
  journal={Biochemistry},
  year={2006},
  volume={45 51},
  pages={15327-37}
}
Nonpeptide antagonists of the human gonadotropin-releasing hormone receptor (GnRH-R) have been the subject of considerable interest because of their potential as a new class of oral therapeutics for the treatment of sex hormone-dependent diseases and infertility. While many classes of competitive GnRH-R antagonists have been described, we present here the first characterization of an allosteric nonpeptide GnRH-R antagonist. Previously, 5-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydronaphthalen-2… CONTINUE READING