Fragment-Based Drug Discovery Targeting Inhibitor of Apoptosis Proteins: Discovery of a Non-Alanine Lead Series with Dual Activity Against cIAP1 and XIAP

Inhibitor of apoptosis proteins (IAPs) are important regulators of apoptosis and pro-survival signaling pathways whose deregulation is often associated with tumor genesis and tumor growth. IAPs have been proposed as targets for anticancer therapy, and a number of peptidomimetic IAP antagonists have...

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Veröffentlicht in:	Journal of medicinal chemistry 2015-08, Vol.58 (16), p.6574-6588
Hauptverfasser:	Chessari, Gianni, Buck, Ildiko M, Day, James E. H, Day, Philip J, Iqbal, Aman, Johnson, Christopher N, Lewis, Edward J, Martins, Vanessa, Miller, Darcey, Reader, Michael, Rees, David C, Rich, Sharna J, Tamanini, Emiliano, Vitorino, Marc, Ward, George A, Williams, Pamela A, Williams, Glyn, Wilsher, Nicola E, Woolford, Alison J.-A
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Antineoplastic Agents - chemical synthesis Antineoplastic Agents - pharmacokinetics Antineoplastic Agents - pharmacology Cell Proliferation - drug effects Computational Biology Drug Design Drug Discovery High-Throughput Screening Assays Humans Inhibitor of Apoptosis Proteins - antagonists & inhibitors Inhibitor of Apoptosis Proteins - drug effects Mice Mice, Inbred BALB C Models, Molecular Peptide Fragments - chemical synthesis Peptide Fragments - pharmacokinetics Peptide Fragments - pharmacology Piperazines - chemical synthesis Piperazines - pharmacology X-Linked Inhibitor of Apoptosis Protein - antagonists & inhibitors Xenograft Model Antitumor Assays
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