Abstract
The new decapeptide SB-75 (INN: Cetrorelix) has been characterized as a potent antagonist of luteinizing-hormone releasing hormone (LH-RH). Such derivatives are of great medicinal interest owing to their potential application in areas such as hormone-dependent tumors, uterine fibroids, and in diseases and conditions which result from inappropriate hormone levels or which can be treated by suppression of estrogens. SB-75 is the subject of intensive ongoing clinical evaluation and is an accepted standard for the design of new LH-RH antagonists. We characterized SB-75 by means of modern MS and NMR techniques to demonstrate the significance of both sequencing methods on a complicated unnatural decapeptide. Our structural elucidations with nuclear Overhauser (NOE) experiments revealed clear evidence for a highly flexible molecule with no single predominant conformation even in sodium dodecyl sulfate (SDS) mimicking a cellular membrane.
| Original language | English (US) |
|---|---|
| Pages (from-to) | 264-270 |
| Number of pages | 7 |
| Journal | International journal of peptide and protein research |
| Volume | 43 |
| Issue number | 3 |
| DOIs | |
| State | Published - Mar 1994 |
| Externally published | Yes |
Keywords
- Cetrorelix
- LH‐RH
- NMR spectroscopy
- NOE
- antagonist
- conformation
- decapeptide
- mass spectrometry
ASJC Scopus subject areas
- Biochemistry