Syntheses and biological activities of potent bombesin receptor antagonists
| Autor: | M Llinares, Chantal Devin, Nicole Bernad, J Azay, José Luis Martínez, Jean-Alain Fehrentz, A. M. Noel-Artis, Olivier Chaloin |
|---|---|
| Rok vydání: | 1999 |
| Předmět: |
chemistry.chemical_classification
Bombesin digestive system complex mixtures Biochemistry 3T3 cells Bombesin receptor chemistry.chemical_compound Endocrinology Enzyme medicine.anatomical_structure chemistry Mechanism of action medicine Secretion medicine.symptom Receptor hormones hormone substitutes and hormone antagonists Gastrin |
| Zdroj: | The Journal of Peptide Research. 53:275-283 |
| ISSN: | 1397-002X |
| DOI: | 10.1034/j.1399-3011.1999.00028.x |
| Popis: | Bombesin receptor antagonists are potential therapeutic agents due to their ability to act as inhibitors of cellular proliferation. On the basis of our hypothesis concerning the mechanism of action of gastrin associating an activating enzyme to the receptor and on the results reported in the literature, we have synthesized bombesin analogs which have been modified in the C-terminal part. Potent bombesin receptor antagonists were obtained by replacement of Leu-13 with a statyl residue or with a residue bearing an hydroxyl group in place of the carbonyl function of Leu-13. Several inhibitors were able to recognize the bombesin receptor on rat pancreatic acini and antagonized bombesin stimulated amylase secretion in the nanomolar range. These compounds were also able to recognize the bombesin receptor and to inhibit [3H] thymidine incorporation in 3T3 cells with the same potency. |
| Databáze: | OpenAIRE |
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