1. Academic Validation
  2. A novel somatostatin mimic with broad somatotropin release inhibitory factor receptor binding and superior therapeutic potential

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

  • J Med Chem. 2003 Jun 5;46(12):2334-44. doi: 10.1021/jm021093t.
Ian Lewis 1 Wilfried Bauer Rainer Albert Nagarajan Chandramouli Janos Pless Gisbert Weckbecker Christian Bruns
Affiliations

Affiliation

  • 1 Transplantation Research Department, Novartis Pharma, CH-4002 Basel, Switzerland. ian.lewis@pharma.novartis.com
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.

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