Structure-Based Drug Design of Bisubstrate Inhibitors of Phenylethanolamine N -Methyltransferase Possessing Low Nanomolar Affinity at Both Substrate Binding Domains 1

The enzyme phenylethanolamine -methyltransferase (PNMT, EC 2.1.1.28) catalyzes the final step in the biosynthesis of epinephrine and is a potential drug target, primarily for the control of hypertension. Unfortunately, many potent PNMT inhibitors also possess significant affinity for the a -adrenoce...

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Veröffentlicht in:	Journal of medicinal chemistry 2020-11, Vol.63 (22), p.13878-13898
Hauptverfasser:	Lu, Jian, Bart, Aaron G, Wu, Qian, Criscione, Kevin R, McLeish, Michael J, Scott, Emily E, Grunewald, Gary L
Format:	Artikel
Sprache:	eng
Schlagworte:	Adenosine - chemistry Adenosine - pharmacology Binding Sites Crystallography, X-Ray Drug Design Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology Humans Isoquinolines - metabolism Models, Molecular Phenylethanolamine N-Methyltransferase - chemistry Phenylethanolamine N-Methyltransferase - metabolism Protein Domains S-Adenosylmethionine - metabolism Structure-Activity Relationship
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