Novel Selective Quinazoline Inhibitors of Endothelin Converting Enzyme-1

PD 069185 is a highly selective and structurally novel inhibitor of endothelin converting enzyme-1 (ECE-1). PD 069185 is a trisubstituted quinazoline with an IC50value of 0.9 ± 0.1 μM for inhibition of human ECE-1 from the solubilized membrane fraction of CHO cells stably transfected with human ECE-...

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Veröffentlicht in:	Biochemical and biophysical research communications 1998-02, Vol.243 (1), p.184-190
Hauptverfasser:	Ahn, Kyunghye, Sisneros, Andre M., Herman, Sarah B., Pan, Sharon M., Hupe, Donald, Lee, Chitase, Nikam, Sham, Cheng, Xue-Min, Doherty, Annette M., Schroeder, Richard L., Haleen, Stephen J., Kaw, Semiko, Emoto, Noriaki, Yanagisawa, Masashi
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Aspartic Acid Endopeptidases - antagonists & inhibitors Aspartic Acid Endopeptidases - genetics big endothelin CHO Cells Cricetinae endothelin endothelin converting enzyme Endothelin-1 Endothelin-Converting Enzymes Endothelins - metabolism Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology Humans In Vitro Techniques Kinetics Male Mesenteric Arteries - drug effects Mesenteric Arteries - physiology Metalloendopeptidases Perfusion Pressure Protein Precursors - metabolism quinazoline Quinazolines - chemistry Quinazolines - pharmacology Rats Rats, Sprague-Dawley Transfection
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