In this study, a multimodal analysis, including metabolic imaging using hyperpolarized pyruvate, points to reduced oxidative flux due to NAD + depletion after β-lapachone treatment of NQO1+ human pancreatic cancer cells.

Jul 19, 2019 · We discovered that after activation by NQO1, β-lap caused tumor-selective cell death and induced innate sensing for adaptive antitumor immunity.

Jun 2, 2017 · As a NQO1 activator, β-lap exhibited a novel anti-cancer activity in NQO1-postive breast cancer cells. Additionally, β-lap inhibited breast cancer cell proliferation, invasion and migration.

Sep 1, 2022 · NQO1 activatable drugs, such as β-lap, could achieve tumor-selective killing while sparing normal cells lacking NQO1 expression in vitro and showing tumor inhibition in pancreatic cancer mouse models in considerable preclinical research.

Jul 10, 2007 · Here, we generated isogenically matched NQO1 + and NQO1 − human H596 NSCLC cells and demonstrated that β-lap induces PARP-1-mediated cell death in an NQO1-dependent manner, an exploitable pathway for selective therapy of NSCLCs.

Jun 4, 2024 · NAD(P)H:quinone oxidoreductase 1 (NQO1) is overexpressed in most solid cancers, emerging as a promising target for tumor-selective killing. β-Lapachone (β-Lap), an NQO1 bioactivatable drug, exhibits significant antitumor effects on NQO1-positive cancer cells by inducing immunogenic cell death (ICD) …

We show that the NAD (P)H:quinone oxidoreductase 1 (NQO1) bioactivatable drug, β-lapachone (ARQ761, ArQule, in clinical form), capitalizes on elevated NQO1:CAT ratios in recalcitrant pancreatic, non-small-cell lung cancer (NSCLC) and breast cancer to elicit tumor-selective programmed necrosis.

Jun 15, 2024 · Based on this finding, we utilized β-Lapachone (β-Lap), an NQO1 bioactivatable drug, to suppress lung tumorigenesis. In this study, the efficacy and safety of low-dose β-Lap were demonstrated in preventing lung tumorigenesis in vivo.

Dec 12, 2016 · NAD (P)H:quinone oxidoreductase 1 (NQO1) bioactivatable drugs have the potential to deliver tumor-selective DNA damage and cell death. They are a unique class of rare quinones that include β-lapachone (β-lap, ARQ761 in clinical form) and deoxynyboquinone (Huang et al., 2012).

NQO1 can be important biomarker since NQO1 is essential and sufficient for β-lap-mediated specific innate sensing and adaptive T cell responses. β-lap is currently being tested in monotherapy or in combination with the other chemodrugs in patients with NQO1 + solid tumors.