Design and Synthesis of an Orally Bioavailable and Selective Peptide Epoxyketone Proteasome Inhibitor (PR-047)

Proteasome inhibition has been validated as a therapeutic modality in the treatment of multiple myeloma and Non-Hodgkin’s lymphoma. Carfilzomib, an epoxyketone currently undergoing clinical trials in malignant diseases, is a highly selective inhibitor of the chymotrypsin-like (CT-L) activity of the...

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Veröffentlicht in:	Journal of medicinal chemistry 2009-05, Vol.52 (9), p.3028-3038
Hauptverfasser:	Zhou, Han-Jie, Aujay, Monette A, Bennett, Mark K, Dajee, Maya, Demo, Susan D, Fang, Ying, Ho, Mark N, Jiang, Jing, Kirk, Christopher J, Laidig, Guy J, Lewis, Evan R, Lu, Yan, Muchamuel, Tony, Parlati, Francesco, Ring, Eileen, Shenk, Kevin D, Shields, Jamie, Shwonek, Peter J, Stanton, Timothy, Sun, Congcong M, Sylvain, Catherine, Woo, Tina M, Yang, Jinfu
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral Animals Antineoplastic agents Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Biological and medical sciences Biological Availability Cell Line Dipeptides - chemical synthesis Dipeptides - chemistry Dipeptides - pharmacokinetics Dipeptides - pharmacology Drug Design Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacokinetics Enzyme Inhibitors - pharmacology General aspects Humans Kinetics Medical sciences Mice Oligopeptides - chemical synthesis Oligopeptides - chemistry Oligopeptides - pharmacokinetics Oligopeptides - pharmacology Pharmacology. Drug treatments Proteasome Inhibitors Structure-Activity Relationship Substrate Specificity Thiazoles - chemical synthesis Thiazoles - chemistry Thiazoles - pharmacokinetics Thiazoles - pharmacology
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