The Superior Therapeutic Properties of SOM230 Originate from Unique Structural Elements

A rational drug design approach involving transposition of functional groups from SRIF into a reduced size cyclohexapeptide template has led to the discovery of SOM230, a novel, stable cyclohexapeptide somatostatin mimic which exhibits unique high affinity binding to human somatostatin receptors (ss...

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Veröffentlicht in:Chimia 2004-04, Vol.58 (4), p.222
Hauptverfasser: Lewis, Ian, Weckbecker, Gisbert, Schmid, Herbert A., Lamberts, Steven W.J., Boerlin, Viktor, Van der Hoek, Joost, Bovermann, Günter, Oberer, Lukas, Pless, Janos, Chandramouli, Nagarajan, Bauer, Wilfried, Albert, Rainer, Bruns, Christian
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Sprache:eng
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Zusammenfassung:A rational drug design approach involving transposition of functional groups from SRIF into a reduced size cyclohexapeptide template has led to the discovery of SOM230, a novel, stable cyclohexapeptide somatostatin mimic which exhibits unique high affinity binding to human somatostatin receptors (sst1-5). 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 II clinical trials.
ISSN:0009-4293
2673-2424
DOI:10.2533/000942904777677902