Document Report Card

ID: ALA1145006

Journal: J Med Chem

Title: A novel somatostatin mimic with broad somatotropin release inhibitory factor receptor binding and superior therapeutic potential.

Authors: Lewis I, Bauer W, Albert R, Chandramouli N, Pless J, Weckbecker G, Bruns C.

Abstract: A rational drug design approach, capitalizing on structure-activity relationships and involving transposition of functional groups from somatotropin release inhibitory factor (SRIF) into a reduced size cyclohexapeptide template, has led to the discovery of SOM230 (25), a novel, stable cyclohexapeptide somatostatin mimic that exhibits unique high-affinity binding to human somatostatin receptors (subtypes sst1-sst5). SOM230 has potent, long-lasting inhibitory effects on growth hormone and insulin-like growth factor-1 release and is a promising development candidate currently under evaluation in phase I clinical trials.

CiteXplore: 12773038

DOI: 10.1021/jm021093t