Solid phase synthesis and biological evaluation of probestin as an angiogenesis inhibitor

Probestin is a potent aminopeptidase N (APN) inhibitor originally isolated from the bacterial culture broth. Here, we report probestin synthesis by solid phase peptide synthesis (SPPS) method and evaluated its activity to inhibit angiogenesis using a chicken embryo chorioallantoic membrane (CAM) ass...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2013-06, Vol.23 (12), p.3561-3564
Hauptverfasser:	Pathuri, Gopal, Thorpe, Jessica E., Disch, Bryan C., Bailey-Downs, Lora C., Ihnat, Michael A., Gali, Hariprasad
Format:	Artikel
Sprache:	eng
Schlagworte:	Aminopeptidase N angiogenesis Angiogenesis Inhibitors - chemical synthesis Angiogenesis Inhibitors - chemistry Angiogenesis Inhibitors - pharmacology Animals APN Breast Neoplasms - blood supply Breast Neoplasms - drug therapy CD13 CD13 Antigens - antagonists & inhibitors Cell Line, Tumor chemistry Chick Embryo chickens chorioallantoic membrane Chorioallantoic Membrane - blood supply culture media Female Humans membrane alanyl aminopeptidase Mice, Inbred BALB C Neovascularization, Physiologic - drug effects Oligopeptides - chemical synthesis Oligopeptides - chemistry Oligopeptides - pharmacology Probestin Solid-Phase Synthesis Techniques - methods Tumor angiogenesis Xenograft Model Antitumor Assays
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Zusammenfassung:	Probestin is a potent aminopeptidase N (APN) inhibitor originally isolated from the bacterial culture broth. Here, we report probestin synthesis by solid phase peptide synthesis (SPPS) method and evaluated its activity to inhibit angiogenesis using a chicken embryo chorioallantoic membrane (CAM) assay and a CAM tumor xenograft model. Results from these studies demonstrate that probestin inhibits the angiogenic activity and tumor growth.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2013.04.031