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Using a novel NQO1 bioactivatable drug, beta-lapachone (ARQ761), to enhance chemotherapeutic effects by metabolic modulation in pancreatic cancer
Journal article   Peer reviewed

Using a novel NQO1 bioactivatable drug, beta-lapachone (ARQ761), to enhance chemotherapeutic effects by metabolic modulation in pancreatic cancer

Muhammad Shaalan Beg, Xiumei Huang, Molly A Silvers, David E Gerber, Joyce Bolluyt, Venetia Sarode, Farjana Fattah, Ralph J Deberardinis, Matthew E Merritt, Xian-Jin Xie, …
Journal of surgical oncology, Vol.116(1), pp.83-88
07/2017
DOI: 10.1002/jso.24624
PMCID: PMC5509448
PMID: 28346693
url
https://www.ncbi.nlm.nih.gov/pmc/articles/5509448View
Open Access

Abstract

Novel, tumor-selective therapies are needed to increase the survival rate of pancreatic cancer patients. K-Ras-mutant-driven NAD(P)H:quinone oxidoreductase 1 (NQO1) is over-expressed in pancreatic tumor versus associated normal tissue, while catalase expression is lowered compared to levels in associated normal pancreas tissue. ARQ761 undergoes a robust, futile redox cycle in NQO1+ cancer cells, producing massive hydrogen peroxide (H O ) levels; normal tissues are spared by low NQO1 and high catalase expression. DNA damage created by ARQ761 in pancreatic cancer cells "hyperactivates" PARP1, causing metabolic catastrophe and NAD ± keresis cell death. NQO1: catalase levels (high in tumor, low in normal tissue) are an attractive therapeutic window to treat pancreatic cancer. Based on a growing body of literature, we are leading a clinical trial to evaluate the combination of ARQ761 and chemotherapy in patients with pancreatic cancer.
Pancreatic Neoplasms - drug therapy Albumins - pharmacology Paclitaxel - pharmacology Pancreatic Neoplasms - metabolism Humans NAD(P)H Dehydrogenase (Quinone) - metabolism Deoxycytidine - pharmacology Naphthoquinones - pharmacology Clinical Trials, Phase I as Topic Deoxycytidine - analogs & derivatives NAD(P)H Dehydrogenase (Quinone) - antagonists & inhibitors Antineoplastic Combined Chemotherapy Protocols - pharmacology

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