Modified peptides which display potent and specific inhibition of human renin

A new class of angiotensinogen analogues which contain heteroatom-methylene and retro-inverso amide bond replacements was synthesized and evaluated for renin inhibition. Selected compounds in the series were specific for renin over other aspartic proteinases, and the most potent inhibitor demonstrat...

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Veröffentlicht in:	Biochemical and biophysical research communications 1987-02, Vol.143 (1), p.44-51
Hauptverfasser:	Luly, Jay R., Plattner, Jacob J., Stein, Herman, Yi, Nwe, Soderquist, Jeffrey, Marcotte, Patrick A., Kleinert, Hollis D., Perun, Thomas J.
Format:	Artikel
Sprache:	eng
Schlagworte:	Angiotensins - chemical synthesis Angiotensins - pharmacology Applied sciences Exact sciences and technology Humans Indicators and Reagents Oligopeptides - chemical synthesis Oligopeptides - pharmacology Other techniques and industries Renin - antagonists & inhibitors Renin-Angiotensin System - drug effects Structure-Activity Relationship
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Beschreibung
Zusammenfassung:	A new class of angiotensinogen analogues which contain heteroatom-methylene and retro-inverso amide bond replacements was synthesized and evaluated for renin inhibition. Selected compounds in the series were specific for renin over other aspartic proteinases, and the most potent inhibitor demonstrated hypotensive activity in a salt depleted monkey.
ISSN:	0006-291X 1090-2104
DOI:	10.1016/0006-291X(87)90627-9