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NF-κB and Its Role in Checkpoint Control

Small Molecule NF-κB Pathway Inhibitors in Clinic

Institute of Molecular and Cell Biology (IMCB), Singapore 138673, Singapore
Department of Pathology, NUS, Singapore 117597, Singapore
Authors to whom correspondence should be addressed.
Int. J. Mol. Sci. 2020, 21(14), 5164;
Received: 12 June 2020 / Revised: 7 July 2020 / Accepted: 14 July 2020 / Published: 21 July 2020
(This article belongs to the Special Issue NF-κB and Disease)
Nuclear factor kappa B (NF-κB) signaling is implicated in all major human chronic diseases, with its role in transcription of hundreds of gene well established in the literature. This has propelled research into targeting the NF-κB pathways for modulating expression of those genes and the diseases mediated by them. In-spite of the critical, but often promiscuous role played by this pathway and the inhibition causing adverse drug reaction, currently many biologics, macromolecules, and small molecules that modulate this pathway are in the market or in clinical trials. Furthermore, many marketed drugs that were later found to also have NF-κB targeting activity were repurposed for new therapeutic interventions. Despite the rising importance of biologics in drug discovery, small molecules got around 76% of US-FDA (Food and Drug Administration-US) approval in the last decade. This encouraged us to review information regarding clinically relevant small molecule inhibitors of the NF-κB pathway from cell surface receptor stimulation to nuclear signaling. We have also highlighted the underexplored targets in this pathway that have potential to succeed in clinic. View Full-Text
Keywords: NF-κB pathway; small molecules; clinical trials; anti-cancer; anti-inflammatory; autoimmune disease NF-κB pathway; small molecules; clinical trials; anti-cancer; anti-inflammatory; autoimmune disease
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MDPI and ACS Style

Ramadass, V.; Vaiyapuri, T.; Tergaonkar, V. Small Molecule NF-κB Pathway Inhibitors in Clinic. Int. J. Mol. Sci. 2020, 21, 5164.

AMA Style

Ramadass V, Vaiyapuri T, Tergaonkar V. Small Molecule NF-κB Pathway Inhibitors in Clinic. International Journal of Molecular Sciences. 2020; 21(14):5164.

Chicago/Turabian Style

Ramadass, Venkataramanan, Thamilselvan Vaiyapuri, and Vinay Tergaonkar. 2020. "Small Molecule NF-κB Pathway Inhibitors in Clinic" International Journal of Molecular Sciences 21, no. 14: 5164.

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