Development of Angiotensin IV Analogs as Hepatocyte Growth Factor/Met Modifiers

Development of Angiotensin IV Analogs as Hepatocyte Growth Factor/Met Modifiers

The 6-AH family [d-Nle-X-Ile-NH-(CH2)5-CONH2; where X = various amino acids] of angiotensin IV (Ang IV) analogs binds directly to hepatocyte growth factor (HGF) and inhibit HGF’s ability to form functional dimers. The metabolically stabilized 6-AH family member, d-Nle-Tyr-Ile-NH-(CH2)5-CONH2, had a...

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Veröffentlicht in:The Journal of pharmacology and experimental therapeutics 2012-03, Vol.340 (3), p.539-548
Hauptverfasser: Kawas, Leen H., McCoy, Alene T., Yamamoto, Brent J., Wright, John W., Harding, Joseph W.
Format: Artikel
Sprache:eng
Schlagworte:
Angiotensin II - analogs & derivatives
Angiotensin II - pharmacology
Animals
Cell Proliferation
Cells, Cultured
Dogs
Hepatocyte Growth Factor - antagonists & inhibitors
Hepatocyte Growth Factor - chemistry
Hepatocyte Growth Factor - metabolism
Humans
Male
Melanoma, Experimental - pathology
Mice
Mice, Inbred C57BL
Oligopeptides - pharmacology
Protein Multimerization
Proto-Oncogene Proteins c-met - physiology
Rats
Rats, Sprague-Dawley
Signal Transduction - drug effects
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Zusammenfassung:The 6-AH family [d-Nle-X-Ile-NH-(CH2)5-CONH2; where X = various amino acids] of angiotensin IV (Ang IV) analogs binds directly to hepatocyte growth factor (HGF) and inhibit HGF’s ability to form functional dimers. The metabolically stabilized 6-AH family member, d-Nle-Tyr-Ile-NH-(CH2)5-CONH2, had a t1/2 in blood of 80 min compared with the parent compound norleual [Nle-Tyr-Leu-Ψ-(CH2-NH2)3-4-His-Pro-Phe], which had a t1/2 in blood of
ISSN:0022-3565
1521-0103
DOI:10.1124/jpet.111.188136