Small structural changes on a hydroquinone scaffold determine the complex I inhibition or uncoupling of tumoral oxidative phosphorylation
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- 作者：Fé ; lix A. Urraa ; felix.urra@qf.uchile.cl" class="auth_mail" title="E-mail the corresponding author ; Miguel Có ; rdova-Delgadob ; Michel Lapiera ; Andrea Orellana-Manzanoa ; Luis Acevedo-Aré ; valob ; Herná ; n Pessoa-Mahanab ; Jaime M. Gonzá ; lez-Vivancob ; Maximiliano Martí ; nez-Cifuentesc ; Oney Ramí ; rez-Rodrí ; guezb ; Juan Pablo Millas-Vargasb ; Boris Weiss-Ló ; pezd ; Mario Pavania ; Jorge Ferreiraa ; jferreir@med.uchile.cl" class="auth_mail" title="E-mail the corresponding author ; Ramiro Araya-Maturanac ; raraya@utalca.cl" class="auth_mail" title="E-mail the corresponding author
- 关键词：ROS ; reactive oxygen species ; OXPHOS ; oxidative phosphorylation ; ANT ; adenine nucleotide translocator ; CCCP ; carbonyl cyanide m-chlorophenylhydrazone ; RCR ; respiratory control ratio ; ETC ; electon transport chain ; ; ∆ ; Ψm ; mitochondrial membrane potential ; OCR ; oxygen consumption rate ; NAC ; N-acetyl l-cysteine ; RRI ; relative resistance index ; mPTP ; mitochondrial permeability transition pore ; TMPD ; N ; N ; N&prime ; N&prime ; -tetramethyl-p-phenylenediamine
- 刊名：Toxicology and Applied Pharmacology
- 出版年：2016
- 出版时间：15 January 2016
- 年：2016
- 卷：291
- 期：Complete
- 页码：46-57
- 全文大小：1647 K
文摘
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Small changes on a hydroquinone scaffold modify the action on OXPHOS of cancer cells.
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Complex I Inhibitors, uncoupler of OXPHOS and agents with dual action are described.
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Cpd. 9 is an uncoupler agent of OXPHOS with selective anti-proliferative effects.
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Useful information to design agents with a selective mechanism on OXPHOS is provided.