SOM230: A New Therapeutic Modality for Cushing's Disease | Zendy

Ian Lewis | Zendy; Herbert Schmid | Zendy; Rainer Kneuer | Zendy; Daniël Hoyer | Zendy; Antonio P. Silva | Zendy; Gisbert Weckbecker | Zendy; Christian Bruns | Zendy; Janos Pless | Zendy

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SOM230: A New Therapeutic Modality for Cushing's Disease

Author(s) -

Ian Lewis,

Herbert Schmid,

Rainer Kneuer,

Daniël Hoyer,

Antonio P. Silva,

Gisbert Weckbecker,

Christian Bruns,

Janos Pless

Publication year - 2014

Publication title -

chimia international journal for chemistry

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.387

H-Index - 55

eISSN - 2673-2424

pISSN - 0009-4293

DOI - 10.2533/chimia.2014.483

Subject(s) - somatostatin receptor , somatostatin , modality (human–computer interaction) , medicine , receptor , pharmacology , computer science , human–computer interaction

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). This unique receptor subtype binding profile, in particular the exceptional high affinity binding to sst5, led to SOM230 being approved by EMEA and FDA in 2012 as the first effective pituitary directed therapeutic modality for Cushing's disease.

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