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Table 1 Summary of direct TF inhibition strategies

From: Pharmacological manipulation of transcription factor protein-protein interactions: opportunities and obstacles

Mode of action Class of drug General benefits General drawbacks Examples/indication
Inhibition of TF gene expression Antisense mRNA, siRNA Selectivity Antisense mRNA and duplex unstable, poor cellular uptake, pro-inflammatory, resistance mechanisms (gene over-expression) K-Ras/cancer [67,68]
Binding to TF DNA-binding domain Decoy oligonucleotide Selectivity Low bioavailability, short half-life, poor cellular uptake Sp1, AP-1, STAT3, Ets-1/cancer [69]
Small molecule Bioavailability Off-target effects Human androgen receptor/cancer [70]
Small peptides and peptidomimetics Less or no side effect Low bioavailability, unstable, pro-inflammatory STAT3/cancer [71]
Disruption of protein-protein interaction Small molecule Bioavailability Off-target effects cMyc/Max, Max/Max, HDM2/p53, Bcl/Bax/cancer [17,60,72,73]
Small peptides and peptidomimetics Less or no side effect Low bioavailability, unstable, pro-inflammatory STAT3, MDMX/p53/cancer [74-76]