Conformationally restricted bicyclic analogs of somatostatin.

  title={Conformationally restricted bicyclic analogs of somatostatin.},
  author={Daniel F. Veber and Frederick W. Holly and William J. Paleveda and Ruth F. Nutt and S J Bergstrand and Mary Louise Torchiana and Monroe S. Glitzer and Richard Saperstein and Ralph F Hirschmann},
  journal={Proceedings of the National Academy of Sciences of the United States of America},
  volume={75 6},
A model for a biologically active conformation of somatostatin is proposed. This model is based primarily on the biological results obtained with novel bicyclic somatostatin analogs having a covalent bridge replacing the side chains of residues 5 and 10, 6 and 11, and 5 and 12, respectively, rather than on physical measurements on the hormone in solution. The high activity of an analog in which Phe6 and Phe11 are replaced by cystine provides evidence that these phenylalanines stabilize the… CONTINUE READING