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Table 2 Small molecules modulators of both NF- κ B and p53 signaling pathways

From: Chronic inflammation and cancer: potential chemoprevention through nuclear factor kappa B and p53 mutual antagonism

Name of compounds

Structure of the compounds

Molecular weights

Signaling pathways affected

References

R-Roscovitine

354

a) Abrogates induction of NF- κ B by preventing I κ B kinase (IKK) kinase activity, NF- κ B /p65-536ser phosphorylation b) Induces p53 by disrupting p53-MDM2 interaction

[245–247]

Flavopiridol

438

a) Blocks steps in the NF- κ B activation pathway such as I κ B α kinase and p65 nuclear translocation, and p65-529-ser phosphorylation b) Reversibly activates p53 by inhibiting MDM2

[248–250]

Nutlin-3

581

a) Inhibits NF- κ B targets ICAM1 and MCP1 transcription in p53 dependent manner. b) Potent inducer of p53 by inhibiting MDM2 interaction

[251, 252]

Curcumin

368

a) Inhibits IKKkinase, promoinflammatory gene promoters such as TNF-2 α, COX-1, COX-2 b) p53 activation by inhibiting MDM2 c) modulation of other signaling pathways

[253–256]

Quinacrine

473

a) Inhibits both constitutive and inducible form of NF- κ B irrespective of the p53 status. b) Activates p53

[104, 167]

Curaxin (CBL 137)

338

a) Simultaneously suppress NF- κ B both basal and inducible states and activate p53 by targeting FACT b) Inhibits NF- κ B, activates p53 by inhibition of FACT complex

[103, 167, 257]

Benfur

322

Inhibits NF- κ B activity which is predominantly dependent on p53-mediated pathway

[258]

Resveratrol

228

Inhibits NF- κ B /p65 and p53 transcriptional functions by deacetylation of specific residues

[259–262]

Pifithrin- α

367

Activation of NF- κ B through blockade of p53-p300 interaction

[263, 264]

Bortezomib

384

Block of NF- κ B and stabilization of p53 by inhibiting E3 ubiquitin ligases

[265]

  1. Here only parents compounds were mentioned. Compounds are in dervatizations for better functional efficacies are described/referred in text/table.