Structural Characterization of Macromolecular Assemblies
Structure & pharmacological properties of SST and CST analogs
Somatostatin (SST) is a 14-amino acid natural peptide that is currently used as a gastric anti-secretory drug to treat human growth hormone secretion disorders and endocrine tumors. Several years ago, Cortistatin (CST), a neuro-peptide hormone similar in sequence to SST was found to play immunomodulatory roles and that its external administration protected mice models of Crohn disease from colitis development. Together with the groups of Dr. A. Riera (IRB Barcelona) and Dr. M. Delgado (Institute López Neyra, CSIC) and with the company BCN peptides, we have studied several analogs of these hormones, designed to improve their stability and specificity. By enhancing specific aromatic–aromatic interactions in these analogues, we have obtained several peptides with high receptor selectivity and stability (Scientific reports 2016) and with anti- inflammatory activity in models of Ulcerative colitis and Crohn’s disease, (Rol Á. et al, in revision).
- Martín-Gago P., Rol Á., Todorovski T., Aragón E., Martin-Malpartida P., Verdaguer X., Vallès Miret M., Fernández- Carneado J., Ponsati B., Macias M.J.*, Riera A. Peptide aromatic interactions modulated by fluorinated residues: Synthesis, structure and biological activity of Somatostatin analogs containing 3-(3',5'-difluorophenyl)-alanine., Scientific Reports, 6, 27285, 2016
- Rol Á., Todorovski T., Martin-Malpartida P., Escolà A., Gonzáles-Rey E., Aragón E., Verdaguer X., Vallès-Miret M., Farrera-Sinfreu J., Puig E., Fernández-Carneado J., Ponsati B., Delgado M., Riera A., Macias M.J.* Structure- based design of a Cortistatin analog with improved immunoregulatory activity against inflammatory bowel disease (@bioRxiv, doi.org/10.1101/839787, manuscript under revision).