Related Experiment Videos
Optimization of a somatostatin mimetic via constrained amino acid and backbone incorporation
A J Souers1, A Rosenquist, E M Jarvie
1Department of Chemistry, University of California, Berkeley 94720, USA.
Bioorganic & Medicinal Chemistry Letters
|January 2, 2001
Abstract:
Constrained analogues 5-7 of the potent and subtype selective somatostatin mimetic 1 were prepared by incorporating conformational constraints into the nine-membered heterocyclic scaffold. Each constrained peptidomimetic showed an altered activity profile relative to lead compound 1, with compound 7 exhibiting a 25-fold and 2-fold binding enhancement against somatostatin receptor subtypes sst4 and sst5, respectively.