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. 2013 Dec 10;3(4):149–162. doi: 10.5681/bi.2013.036

Table 2 . Selected inhibitors involved in inhibition of NAD biosynthesis/function.

Inhibitor Pharmacological effect(s) Reference
FK866/K22.175, inhibitor of nicotinamide phosphoribosyltransferase (NamPRT) Potent antiangiogenic effects in murine renal cell carcinoma 38
APO866, inhibitor of NamPRT Potent inhibition of most cancer cells (acute myeloid leukemia [AML], acute lymphoblastic leukemia [ALL], mantle cell lymphoma [MCL], chronic lymphocytic leukemia [CLL], and T-cell lymphoma) 39
GMX1778, inhibitor of NamPRT Neuroblastoma regression and vessel maturation without inducing drug resistance in engrafted mice 40
Beta-lapachone, an orthonaphthoquinone Induction of cell death by activation of a futile cycling of the drug by the cytoplasmic two-electron reductaseNAD(P) H: quinone oxidoreductase (NQO1), DT-diaphorase and Xip3. Production of reactive oxygen species (ROS) at higher drug concentrations 41
Retinoic acid Induction of apoptosis by all-trans-retinoic acid and N-(4-hydroxyphenyl)retinamide in MCF7 cancer cells through transient increase in NADH level and mitochondrial oxidative turnover and a slow decline in reduced thiol level and mitochondrial membrane potential 42
Mycophenolic acid, a inhibitor of inosine 5'-monophosphate dehydrogenase (IMPDH) Enhanced cytotoxicity in tumor cell lines by binding to IMPDH at the nicotinamide sub-site of the NAD cofactor binding domain 43
Dicumarol, a NQO1 inhibitor Inhibition of NADPH: quinone oxidoreductase induces growth inhibition of pancreatic cancer via a superoxide-mediated mechanism 44
Sirtinol, a SIRT1 inhibitor Induction of senescence-like growth arrest, increased expression of plasminogen activator inhibitor, and impaired activation of mitogen-activated protein kinase (MAPK) pathways in human breast cancer MCF-7 cells and lung cancer H1299 cells. 45
Sulindac Induction of carcinogen metabolizing enzymes in human colon cancer cells 46
Salermide, a Sirtuin inhibitor Induction of cancer-specific proapoptotic effect in cancer cell s and mice by inhibiting SIRT1 and SIRT2 47