Pharmacology of smac mimetics; chemotype differentiation based on physical association with caspase regulators and cellular transport
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- 作者：Randy L. Talbott ; Randy.Talbott@BMS.Com" class="auth_mail" title="E-mail the corresponding author ; Robert M. Borzilleri ; Charu Chaudhry ; Joseph Fargnoli ; Henry Shen ; Craig Fairchild ; Bryan Barnhart ; Marie Ortega ; Thomas E. McDonagh ; Ragini Vuppugalla ; Gregory D. Vite ; John T. Hunt ; Marco Gottardis ; Joseph G. Naglich
- 关键词：SM ; smac mimetic ; IAP ; inhibitor of apoptosis protein ; BIR ; baculoviral IAP repeat ; PCD ; programmed cell death ; TNF ; tumor necrosis factor ; TRAIL ; tumor necrosis factor-related apoptosis-inducing ligand ; Cyt c ; cytochrome c ; Smac/DIABLO ; second mitochondrial activator of caspases/direct IAP binding protein with low isoelectric point ; RING ; really interesting new gene ; XIAP ; X-Chromosome-linked Inhibitor of Apoptosis Protein ; NIK ; NF-魏B-inducing kinase ; MAP3K14 ; RIPK1 ; receptor interacting protei
- 刊名：Experimental Cell Research
- 出版年：2015
- 出版时间：1 November 2015
- 年：2015
- 卷：338
- 期：2
- 页码：251-260
- 全文大小：1496 K
文摘
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We report a novel series of dimeric IAP antagonists with potent antitumor activities.
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One chemotype induced markers of apoptosis and had antitumor activity in different tumor types.
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Another chemotype demonstrated efficacy in a tumor model with elevated ABCB1 levels.