Title of article
Optimization of a somatostatin mimetic via constrained amino acid and backbone incorporation
Author/Authors
Andrew J. Souers، نويسنده , , Asa Rosenquist، نويسنده , , Emma M. Jarvie، نويسنده , , Mark Ladlow، نويسنده , , Wasyl Feniuk، نويسنده , , Jonathan A. Ellman، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2000
Pages
3
From page
2731
To page
2733
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.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2000
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
791192
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