Journal ArticleDOI
Eine neue Methode zur Synthese von Peptiden: Aktivierung der Carboxylgruppe mit Dicyclohexylcarbodiimid unter Zusatz von 1‐Hydroxy‐benzotriazolen
Wolfgang König,Rolf Geiger +1 more
TLDR
In this article, the authors show that 1-Hydroxy-benzotriazol and 1-hydroxy-acetyl carbodiimid-methode eignen sich als Zusatze bei der Dicyclohexylcarbodiimids-Methode zur Synthese von Peptiden, verhindern die N-Acyl-harnstoffbildung and fuhren in hoher Ausbeute.Abstract:
1-Hydroxy-benzotriazol sowie verschiedene kernsubstituierte 1-Hydroxy-benzotriazole eignen sich als Zusatze bei der Dicyclohexylcarbodiimid-Methode zur Synthese von Peptiden. Ihr Einflus auf die Racemisierung bei Peptidsynthesen wurde unter Anwendung des gaschromatographischen Racemisierungstests von Weygand u. Mitarbb.2) untersucht. Die neuen Zusatze senken die Racemisierung, verhindern die N-Acyl-harnstoffbildung und fuhren in hoher Ausbeute zu sehr reinen Peptiden.read more
Citations
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The role of the C-terminus of the insulin B-chain in modulating structural and functional properties of the hormone.
Sigmar Leyer,Hans-Gregor Gattner,Margot Leithäuser,Brandenburg D,Axel Wollmer,Hartwig Höcker +5 more
TL;DR: The backbone-modified insulin derivative [SarB26]des-(B27-B30)-insulin-B26-amide (sarcosine = N-methylglycine) exhibits an unexpectedly high receptor affinity of 1100% which demonstrates that the B 26-amide hydrogen of the native hormone is not important for receptor binding.
Journal ArticleDOI
Short-chain analogs of luteinizing hormone-releasing hormone containing cytotoxic moieties.
Tamás Janáky,Anna Juhász,Zoltan Rekasi,P. Serfozo,Jacek Pinski,L Bokser,Gordan Srkalovic,Slobodan Milovanovic,Tommie W. Redding,Gabor Halmos +9 more
TL;DR: These analogs showed a wide range of receptor-binding affinities to rat pituitaries and cell membranes of human breast cancer and rat Dunning prostate cancer and several of these conjugates exerted some cytotoxic effects on MCF-7 breast cancer cell line.
Patent
Pyrazole derivatives as modulators of the 5-ht2a serotonin receptor useful for the treatment of disorders related thereto
Yifeng Xiong,Martin C. Cherrier,Choi Jin Sun Karoline,Peter I. Dosa,Brian M. Smith,Sonja Strah-Pleynet,Brett Ullman,Bradley Teegarden +7 more
TL;DR: In this paper, the 5-HT2A serotonin receptor mediated disorders in combination with other pharmaceutical agents administered separately or together are discussed. And the present invention relates to certain pyrazole derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5HT2a serotonin receptor.
Journal ArticleDOI
Anwendung von 4-Polystyryltriphenylmethylchlorid zur Synthese von Peptiden und Aminosäure-Derivaten
TL;DR: Application of 4-Polystyryltriphenylmethyl Chloride to the Syntheses of Peptides and Amino Acid Derivatives is discussed in this article, where the use of polymer-bound trityl chloride as an α-amino protecting group of amino acids allows simple and high yield syntheses of amino acid derivatives and peptides.
Journal ArticleDOI
Lipoconjugates: structure-activity studies for pheromone analogues of Ustilago maydis with varied lipophilicity.
TL;DR: It is concluded that the lipomodification in mating pheromones of U. maydis acts to increase the effective concentration of the drug in the target cell membrane without additional structure-inducing or receptor-binding effects.
References
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Journal ArticleDOI
The Use of Esters of N-Hydroxysuccinimide in Peptide Synthesis
Journal ArticleDOI
t-Butyl Esters of Amino Acids and Peptides and their Use in Peptide Synthesis1
Journal ArticleDOI
Zur Synthese des Glucagons, X. Darstellung der Sequenz 22–29
Erich Wünsch,Fritz Drees +1 more
TL;DR: In this paper, the geschutzte Teilsequenz 22-29 des Glucagons, wird auf zwei verschiedenen Wegen synthetisiert.