Synthesis and conformational study of two cyclic analogues of somatostatin containing an AMPA-spacer unit
| Autor: | Dirk Tourwé, G. Van Binst, D. Gondol, C. Wynants, P. Vander Elst |
|---|---|
| Rok vydání: | 2009 |
| Předmět: |
chemistry.chemical_classification
Magnetic Resonance Spectroscopy Protein Conformation Stereochemistry Nuclear magnetic resonance spectroscopy AMPA receptor Phenylacetic acid Growth Hormone-Releasing Hormone Biochemistry Pentapeptide repeat Cyclic peptide Turn (biochemistry) chemistry.chemical_compound Somatostatin chemistry Growth Hormone Pituitary Gland Animals Indicators and Reagents Two-dimensional nuclear magnetic resonance spectroscopy Cells Cultured |
| Zdroj: | International Journal of Peptide and Protein Research. 29:331-346 |
| ISSN: | 0367-8377 |
| DOI: | 10.1111/j.1399-3011.1987.tb02260.x |
| Popis: | Two cyclic somatostatin analogues containing the active sequence Phe7-D-Trp8-Lys9-Thr10 and a meta- or para-(aminomethyl) phenylacetic acid (AMPA) spacer unit, have been synthesized. A conformational study using 2D n.m.r. techniques (COSY, NOESY) reveals that the conformation of the meta-AMPA analogue has some analogy with the bio-active conformation proposed earlier by Veber and colleagues, while in the para-AMPA analogue an equilibrium exists between a beta-II' turn and a gamma-turn structure. Both analogues show no GH-inhibition or LH-inhibition in in vitro assays. |
| Databáze: | OpenAIRE |
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