Literature DB >> 11133079

Optimization of a somatostatin mimetic via constrained amino acid and backbone incorporation.

A J Souers1, A Rosenquist, E M Jarvie, M Ladlow, W Feniuk, J A Ellman.   

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.

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Year:  2000        PMID: 11133079     DOI: 10.1016/s0960-894x(00)00552-7

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  1 in total

Review 1.  Drug design at peptide receptors: somatostatin receptor ligands.

Authors:  Jason P Hannon; Caroline Nunn; Barbara Stolz; Christians Bruns; Gisbert Weckbecker; Ian Lewis; Thomas Troxler; Konstanze Hurth; Daniel Hoyer
Journal:  J Mol Neurosci       Date:  2002 Feb-Apr       Impact factor: 3.444

  1 in total

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