Inhibiting NF-κB Activation by Small Molecules As a Therapeutic Strategy
By Subash C. Gupta, C. Sundaram, Simone Reuter, Bharat B. Aggarwal. Biochimica et Biophysica Acta, 2010
776 citations recorded by the source corpus.
Because nuclear factor-κB (NF-κB) is a ubiquitously expressed proinflammatory transcription factor that regulates the expression of over 500 genes involved in cellular transformation, survival, proliferation, invasion, angiogenesis, metastasis, and inflammation, the NF-κB signaling pathway has become a potential target for pharmacological intervention. A wide variety of agents can activate NF-κB through canonical and noncanonical pathways. Canonical pathway involves various steps including the phosphorylation, ubiquitnation, and degradation of the inhibitor of NF-κB (IκBα), which leads to the nuclear translocation of the p50- p65 subunits of NF-κB followed by p65 phosphorylation, acetylation and methylation, DNA binding, and gene transcription. Thus, agents that can inhibit protein kinases, protein phosphatases, proteasomes, ubiquitnation, acetylation, methylation, and DNA binding steps have been identified as NF-κB inhibitors. Here, we review the small molecules that suppress NF-κB activation and thus may have therapeutic potential.
Subfields: Cancer Research, Molecular Biology, Oncology
View Paper: https://www.semanticscholar.org/paper/0f5bd830a3a94e621fc29c52b92aa9f3fc23b0f2
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Citations in the corpus
- NF‐κB and the link between inflammation and cancer (2012, background): “Other than aspirin, the likely preventatives will not be pharmaceutical drugs but instead be dietary and natural products; many such anti-inflammatory and NF-jB inhibiting natural compounds and small molecules have been identified (213).”
- Roles of NF-κB in Cancer and Inflammatory Diseases and Their Therapeutic Approaches (2016, background): “The COX independent anti-inflammatory effects of NSAIDs include the inhibition of the cyclin-dependent kinase, Mitogen-Activated Protein (MAP) kinases and IkB kinase (IKK) that results in the inhibition of transcription dependent on NF-kB [99].”
- Regulation of survival, proliferation, invasion, angiogenesis, and metastasis of tumor cells through modulation of inflammatory pathways by nutraceuticals (2010, background): “More than 700 inhibitors of the NF-κB activation pathway have been reported, including antioxidants, peptides, small RNA/DNA, microbial and viral proteins, small molecules, and engineered dominant-negative or constitutively active polypeptides [29].”
- Corticosteroid resistance in patients with asthma and chronic obstructive pulmonary disease. (2013, background): “Blocking NF-kB with selective inhibitors of inhibitor of NF-kB kinase (IKKb) is another way of treating corticosteroidresistant inflammation, but it is likely that these drugs will have toxicity and side effects and therefore might only be suitable for topical application.(90)”