329018-89-5Relevant academic research and scientific papers
Optimization of a somatostatin mimetic via constrained amino acid and backbone incorporation
Souers, Andrew J.,Rosenquist, Asa,Jarvie, Emma M.,Ladlow, Mark,Feniuk, Wasyl,Ellman, Jonathan A.
, p. 2731 - 2733 (2000)
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. (C) 2000 Elsevier Science Ltd.
