Journal article

Drug design at peptide receptors - Somatostatin receptor ligands

JP Hannon, C Nunn, B Stolz, C Bruns, G Weckbecker, I Lewis, T Troxler, K Hurth, D Hoyer

Journal of Molecular Neuroscience | HUMANA PRESS INC | Published : 2002


Somatostatin (SRIF, somatotropin release inhibiting factor), discovered for its inhibitory action on growth hormone (GH) secretion from pituitary, is an abundant neuropeptide. Two forms, SRIF14 and SRIF28 exist. Recently, a second family of peptides with very similar sequences and features was described; the cortistatins (CST), CST17 and CST29 which are brain selective. The five cloned SRIF receptors (sst1-5) belong to the G-protein coupled/ heptathelical receptor family. Structural and operational features distinguish two classes of receptors; SRIF1 - sst2/sst3/sst5 (high affinity for octreotide or seglitide) and SRIF2 = sst1/sst4(very low affinitty for the aforementioned ligands). The affi..

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