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pubmed-article:8005749pubmed:abstractTextThe 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.lld:pubmed
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pubmed-article:8005749pubmed:statusMEDLINElld:pubmed
pubmed-article:8005749pubmed:monthMarlld:pubmed
pubmed-article:8005749pubmed:issn0367-8377lld:pubmed
pubmed-article:8005749pubmed:authorpubmed-author:SchallyA VAVlld:pubmed
pubmed-article:8005749pubmed:authorpubmed-author:EngelJJlld:pubmed
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pubmed-article:8005749pubmed:authorpubmed-author:BuskerEElld:pubmed
pubmed-article:8005749pubmed:authorpubmed-author:BernaJJlld:pubmed
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pubmed-article:8005749pubmed:volume43lld:pubmed
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pubmed-article:8005749pubmed:pagination264-70lld:pubmed
pubmed-article:8005749pubmed:dateRevised2006-11-15lld:pubmed
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pubmed-article:8005749pubmed:year1994lld:pubmed
pubmed-article:8005749pubmed:articleTitleStructural investigation of Cetrorelix, a new potent and long-acting LH-RH antagonist.lld:pubmed
pubmed-article:8005749pubmed:affiliationDegussa AG, Hanau-Wolfgang, Germany.lld:pubmed
pubmed-article:8005749pubmed:publicationTypeJournal Articlelld:pubmed