Cited by 771NF-κB Signaling PathwaysNatural Compounds in Disease TreatmentSignaling Pathways in Disease

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Inhibiting NF-κB activation by small molecules as a therapeutic strategy

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Gupta, Subash C., Sundaram, Chitra, Reuter, Simone, Aggarwal, Bharat B.·2010·Biochimica et Biophysica Acta (BBA) - Gene Regulatory Mechanisms

DOI 10.1016/j.bbagrm.2010.05.004PMC PMC2955987

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Abstract

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, ubiquitination, 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, ubiquitination, acetylation, methylation, and DNA binding steps have been identified as NF-κB inhibitors. Because of the critical role of NF-κB in cancer and various chronic diseases, numerous inhibitors of NF-κB have been identified. In this review, however, we describe only small molecules that suppress NF-κB activation, and the mechanism by which they block this pathway.

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RETRACTED ARTICLE: Local administration of transcription factor decoy oligonucleotides to nuclear factor-κB prevents carrageenin-induced inflammation in rat hind paw
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Authors: Gupta, S. C., Sundaram, C., Reuter, S., & Aggarwal, B. B.
Affiliations: The University of Texas MD Anderson Cancer Center (US)
Corresponding author: Aggarwal, Bharat B.
ORCID: Gupta, Subash C.
Aggarwal, Bharat B.
Venue: Biochimica et Biophysica Acta (BBA) - Gene Regulatory Mechanisms
Publisher: Elsevier BV
Published: 2010-10
Volume: 1799
Issue: 10-12
Pages: 775-787
ISSN: 1874-9399 (ISSN-L)
DOI: 10.1016/j.bbagrm.2010.05.004
PMC: PMC2955987
OpenAlex: W1973354681
Cited by: 762
References: 232
Citations by year: 2026: 38 · 2025: 32 · 2024: 39 · 2023: 36 · 2022: 42 · 2021: 59 · 2020: 63 · 2019: 66 · 2018: 70 · 2017: 63 · 2016: 45 · 2015: 45 · 2014: 41 · 2013: 50 · 2012: 35
FWCI: 3.26
Type: journal article
Language: en
Open access: green
www.ncbi.nlm.nih.gov
Licence: www.elsevier.com/tdm/userlicense/1.0/ (tdm)
Locations: Biochimica et Biophysica Acta (BBA) - Gene Regulatory Mechanisms (publishedVersion)
PubMed (publishedVersion)
PubMed Central (acceptedVersion)
Funders: National Cancer Institute (CA-16672, P01CA091844, P01CA124787, CA-124787-01A2, P30CA016672)
Topics: Life Sciences › Biochemistry, Genetics and Molecular Biology › Cancer Research › NF-κB Signaling Pathways
Health Sciences › Medicine › Complementary and alternative medicine › Natural Compounds in Disease Treatment
Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Signaling Pathways in Disease
Keywords: NF-κB signaling, NF-κB inhibitors, small molecules, canonical NF-κB pathway, non-canonical NF-κB signaling, protein kinases, proteasome inhibitors, protein phosphatase, inflammation, cancer, chronic disease
MeSH terms: Animals, Cell Survival, Cell Transformation, Neoplastic, Gene Expression Regulation, Humans, Inflammation, Neoplasm Invasiveness, Neoplasm Metastasis, Neoplasms, Phosphorylation, Signal Transduction, NF-kappa B, Neovascularization, Physiologic, Cell Proliferation, I-kappa B Kinase

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Inhibiting NF-κB activation by small molecules as a therapeutic strategy

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