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Fluorescence-Based Detection of FEN1 Nuclease Activity and Screening of Small-Molecule Inhibitors
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ENOX2 target for the anticancer isoflavone ME-143
D James Morré1, Theodore Korty, Christiaan Meadows
1Mor-NuCo, Inc., West Lafayette, IN, USA.
Oncology Research
|February 21, 2015
Summary
ME-143, a synthetic isoflavone, effectively inhibits cancer cell growth by targeting the ENOX2 protein, which is crucial for cancer cell proliferation. This compound demonstrates high binding affinity to ENOX2, offering a promising therapeutic avenue for various cancers.
Area of Science:
- Biochemistry
- Molecular Biology
- Oncology
Background:
- The ECTO-NOX (ENOX) protein family includes ENOX2 (tNOX), a cancer-specific cell surface protein implicated in tumor growth.
- Synthetic isoflavones are being investigated for their anticancer properties.
- ME-143 (NV-143) is a synthetic isoflavone undergoing clinical evaluation for cancer treatment.
Purpose of the Study:
- To investigate the molecular mechanism of ME-143's anticancer activity.
- To determine ME-143's effect on ENOX2 protein activity and binding.
- To assess ME-143's impact on cancer cell growth and cell cycle progression.
Main Methods:
- Assessed the inhibitory effects of ME-143 on ENOX2's oxidative and protein disulfide-thiol interchange activities.
- Measured the binding affinity (Kd) of ME-143 to purified recombinant ENOX2.
- Evaluated ME-143's impact on cancer cell growth (EC50) and cell cycle traversal.
- Compared ME-143's effects on ENOX2 with its effects on the constitutive ENOX1 (CNOX) protein.
Main Results:
- ME-143 inhibited ENOX2 activity with EC50s in the range of 20-50 nM.
- ME-143 bound to ENOX2 with a dissociation constant (Kd) of 43 nM.
- Inhibition of ENOX2's protein disulfide-thiol interchange activity correlated with suppressed cancer cell enlargement and cell cycle progression.
- ME-143 did not affect the activity of ENOX1 (CNOX) in either cancer or non-cancer cells.
Conclusions:
- ME-143 is a potent inhibitor of the cancer-specific ENOX2 protein.
- The binding affinity of ME-143 to ENOX2 is significantly higher than that of phenoxodiol.
- ME-143's inhibition of ENOX2 activity underlies its efficacy in inhibiting cancer cell growth and progression.
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