Novel octreotide dicarba-analogues were synthesized and their affinity towards somatostatin receptors was tested. The correlation between conformation families and affinity data strongly indicates that the sst5 selectivity is favored by a helical conformation involving the C-terminus triad, while a pan-SRIF mimic activity is based mainly on a conformational equilibrium between extended and folded conformational states.
Novel octreotide dicarba-analogues with high affinity and different selectivity for somatostatin receptors / Di Cianni, A; Carotenuto, Alfonso; Brancaccio, Diego; Novellino, Ettore; Reubi, Jc; Beetschen, K; Papini, Am; Ginanneschi, M.. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 1520-4804. - 53:16(2010), pp. 6188-6197. [10.1021/jm1005868]
Novel octreotide dicarba-analogues with high affinity and different selectivity for somatostatin receptors
CAROTENUTO, ALFONSO
;BRANCACCIO, DIEGO;NOVELLINO, ETTORE;
2010
Abstract
Novel octreotide dicarba-analogues were synthesized and their affinity towards somatostatin receptors was tested. The correlation between conformation families and affinity data strongly indicates that the sst5 selectivity is favored by a helical conformation involving the C-terminus triad, while a pan-SRIF mimic activity is based mainly on a conformational equilibrium between extended and folded conformational states.| File | Dimensione | Formato | |
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