Targeting IKKβ in Cancer: Challenges and Opportunities for the Therapeutic Utilisation of IKKβ Inhibitors

IKK1/2 protect human cells from TNF-mediated RIPK1-dependent apoptosis in an NF-κB-independent manner

(2018) Carsten Slotta et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH

Dual Targeting of Oncogenic Activation and Inflammatory Signaling Increases Therapeutic Efficacy in Myeloproliferative Neoplasms

(2018) Maria Kleppe et al.   CANCER CELL

IκB Kinase α Is Required for Development and Progression ofKRAS-Mutant Lung Adenocarcinoma

(2018) Malamati Vreka et al.   CANCER RESEARCH

Simultaneous targeting therapy for lung metastasis and breast tumor by blocking the NF-κB signaling pathway using Celastrol-loaded micelles

(2018) Yue Zhao et al.   DRUG DELIVERY

NF-κB in the crosshairs: Rethinking an old riddle

(2018) Jason Bennett et al.   INTERNATIONAL JOURNAL OF BIOCHEMISTRY & CELL BIOLOGY

Dimethyl fumarate potentiates oncolytic virotherapy through NF-κB inhibition

(2018) Mohammed Selman et al.   Science Translational Medicine

A novel allosteric inhibitor that prevents IKKβ activation

(2018) Hongbo Liu et al.   MedChemComm

The p55TNFR-IKK2-Ripk3 axis orchestrates arthritis by regulating death and inflammatory pathways in synovial fibroblasts

(2018) Marietta Armaka et al.   Nature Communications

Myeloid-derived interleukin-1β drives oncogenic KRAS-NF-κΒ addiction in malignant pleural effusion

(2018) Antonia Marazioti et al.   Nature Communications

An NF-κB Transcription-Factor-Dependent Lineage-Specific Transcriptional Program Promotes Regulatory T Cell Identity and Function

(2017) Hyunju Oh et al.   IMMUNITY

Inhibitory Kappa B Kinase α (IKKα) Inhibitors That Recapitulate Their Selectivity in Cells against Isoform-Related Biomarkers

(2017) Nahoum G. Anthony et al.   JOURNAL OF MEDICINAL CHEMISTRY

Proteasome inhibitors in cancer therapy

(2017) Elisabet E. Manasanch et al.   Nature Reviews Clinical Oncology

IκB kinase inhibition as a potential treatment of osteoarthritis – results of a clinical proof-of-concept study

(2017) K. Grothe et al.   OSTEOARTHRITIS AND CARTILAGE

Inflammation and the Metabolic Syndrome: The Tissue-Specific Functions of NF-κB

(2017) Leen Catrysse et al.   TRENDS IN CELL BIOLOGY

4-Hydroxy-N-[3,5-bis(trifluoromethyl)phenyl]-1,2,5-thiadiazole-3-carboxamide: a novel inhibitor of the canonical NF-κB cascade

(2017) Agnese C. Pippione et al.   MedChemComm

TNFα blockade overcomes resistance to anti-PD-1 in experimental melanoma

(2017) Florie Bertrand et al.   Nature Communications

Prolonged IKKβ Inhibition Improves Ongoing CTL Antitumor Responses by Incapacitating Regulatory T Cells

(2017) Christoph Heuser et al.   Cell Reports

Inhibition of IκB Kinase at 24 Hours After Acute Kidney Injury Improves Recovery of Renal Function and Attenuates Fibrosis

(2017) Florence L. Johnson et al.   Journal of the American Heart Association

Immune System, Friend or Foe of Oncolytic Virotherapy?

(2017) Anna C. Filley et al.   Frontiers in Oncology

Deubiquitination and Stabilization of PD-L1 by CSN5

(2016) Seung-Oe Lim et al.   CANCER CELL

NF-κB Restricts Inflammasome Activation via Elimination of Damaged Mitochondria

(2016) Zhenyu Zhong et al.   CELL

The effect of an IκB-kinase-β(IKKβ) inhibitor on tobacco smoke-induced pulmonary inflammation

(2016) Sue In Choi et al.   EXPERIMENTAL LUNG RESEARCH

IKK inhibitor suppresses epithelial-mesenchymal transition and induces cell death in prostate cancer

(2016) Hao Ping et al.   ONCOLOGY REPORTS

Super-resolution microscopy reveals a preformed NEMO lattice structure that is collapsed in incontinentia pigmenti

(2016) Janine Scholefield et al.   Nature Communications

PI3K/Akt promotes feedforward mTORC2 activation through IKKα

(2016) Han C. Dan et al.   Oncotarget

Neutrophil-Derived IL-1β Impairs the Efficacy of NF-κB Inhibitors against Lung Cancer

(2016) Allyson G. McLoed et al.   Cell Reports

Structural Basis for the Activation of IKK1/α

(2016) Smarajit Polley et al.   Cell Reports

The Regulation of NF-κB Subunits by Phosphorylation

(2016) Frank Christian et al.   Cells

Inhibition of Canonical NF-κB Signaling by a Small Molecule Targeting NEMO-Ubiquitin Interaction

(2016) Michelle Vincendeau et al.   Scientific Reports

Chemotherapy Induces Programmed Cell Death-Ligand 1 Overexpression via the Nuclear Factor- B to Foster an Immunosuppressive Tumor Microenvironment in Ovarian Cancer

(2015) J. Peng et al.   CANCER RESEARCH

Withaferin A disrupts ubiquitin-based NEMO reorganization induced by canonical NF-κB signaling

(2015) Shawn S. Jackson et al.   EXPERIMENTAL CELL RESEARCH

Novel NF-κB inhibitors: a patent review (2011 – 2014)

(2015) Sateesh Kumar Arepalli et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Nuclear factor kappa B-mediated CD47 up-regulation promotes sorafenib resistance and its blockade synergizes the effect of sorafenib in hepatocellular carcinoma in mice

(2015) Jessica Lo et al.   HEPATOLOGY

Talimogene Laherparepvec Improves Durable Response Rate in Patients With Advanced Melanoma

(2015) Robert H.I. Andtbacka et al.   JOURNAL OF CLINICAL ONCOLOGY

IKKβ acts as a tumor suppressor in cancer-associated fibroblasts during intestinal tumorigenesis

(2015) Charles K. Pallangyo et al.   JOURNAL OF EXPERIMENTAL MEDICINE

IKKβ in intestinal mesenchymal cells promotes initiation of colitis-associated cancer

(2015) Vasiliki Koliaraki et al.   JOURNAL OF EXPERIMENTAL MEDICINE

SnapShot: Kinase Inhibitors II

(2015) Jinhua Wang et al.   MOLECULAR CELL

Unknown

(2015) Regina Sordi et al.   MOLECULAR MEDICINE

Ectopic lymphoid structures function as microniches for tumor progenitor cells in hepatocellular carcinoma

(2015) Shlomi Finkin et al.   NATURE IMMUNOLOGY

Ibrutinib in Previously Treated Waldenström’s Macroglobulinemia

(2015) Steven P. Treon et al.   NEW ENGLAND JOURNAL OF MEDICINE

A set of NF-κB–regulated microRNAs induces acquired TRAIL resistance in Lung cancer

(2015) Young-Jun Jeon et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

EGFR and NF-κB: partners in cancer

(2015) Kateryna Shostak et al.   TRENDS IN MOLECULAR MEDICINE

Breaking resistance of pancreatic cancer cells to an attenuated vesicular stomatitis virus through a novel activity of IKK inhibitor TPCA-1

(2015) Marcela Cataldi et al.   VIROLOGY

Ainsliadimer A selectively inhibits IKKα/β by covalently binding a conserved cysteine

(2015) Ting Dong et al.   Nature Communications

T cell-NF-κB activation is required for tumor control in vivo

(2015) Sarah E Barnes et al.   Journal for ImmunoTherapy of Cancer

IKK2 Inhibition Using TPCA-1-Loaded PLGA Microparticles Attenuates Laser-Induced Choroidal Neovascularization and Macrophage Recruitment

(2015) Subhash Gaddipati et al.   PLoS One

PD-L1 and Survival in Solid Tumors: A Meta-Analysis

(2015) Pin Wu et al.   PLoS One

Inducible but Not Constitutive Expression of PD-L1 in Human Melanoma Cells Is Dependent on Activation of NF-κB

(2015) Kavitha Gowrishankar et al.   PLoS One

An unexpected twist to the activation of IKKβ: TAK1 primes IKKβ for activation by autophosphorylation

(2014) Jiazhen Zhang et al.   BIOCHEMICAL JOURNAL

Withaferin A inhibits NF-kappaB activation by targeting cysteine 179 in IKKβ

(2014) Karen Heyninck et al.   BIOCHEMICAL PHARMACOLOGY

Receptor proximal kinases in NF-κB signaling as potential therapeutic targets in cancer and inflammation

(2014) Lynn Verstrepen et al.   BIOCHEMICAL PHARMACOLOGY

A nonsense mutation in IKBKB causes combined immunodeficiency

(2014) T. Mousallem et al.   BLOOD

Molecular targets of aspirin and cancer prevention

(2014) L Alfonso et al.   BRITISH JOURNAL OF CANCER

Myeloid IKK  Promotes Antitumor Immunity by Modulating CCL11 and the Innate Immune Response

(2014) J. Yang et al.   CANCER RESEARCH

The Novel IKK2 Inhibitor LY2409881 Potently Synergizes with Histone Deacetylase Inhibitors in Preclinical Models of Lymphoma through the Downregulation of NF- B

(2014) C. Deng et al.   CLINICAL CANCER RESEARCH

Regulatory T cells in cancer immunotherapy

(2014) Hiroyoshi Nishikawa et al.   CURRENT OPINION IN IMMUNOLOGY

Immunodeficiency and disseminated mycobacterial infection associated with homozygous nonsense mutation of IKKβ

(2014) Siobhan O. Burns et al.   JOURNAL OF ALLERGY AND CLINICAL IMMUNOLOGY

Akt-dependent Activation of mTORC1 Complex Involves Phosphorylation of mTOR (Mammalian Target of Rapamycin) by IκB Kinase α (IKKα)

(2014) Han C. Dan et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Immunodeficiency Associated with a Nonsense Mutation of IKBKB

(2014) Christian Nielsen et al.   JOURNAL OF CLINICAL IMMUNOLOGY

Improvement of ventilation-induced lung injury in a rodent model by inhibition of inhibitory κB kinase

(2014) Yu-Sheng Shu et al.   Journal of Trauma and Acute Care Surgery

TPCA-1 Is a Direct Dual Inhibitor of STAT3 and NF- B and Regresses Mutant EGFR-Associated Human Non-Small Cell Lung Cancers

(2014) J. Nan et al.   MOLECULAR CANCER THERAPEUTICS

NF-κB Directs Dynamic Super Enhancer Formation in Inflammation and Atherogenesis

(2014) Jonathan D. Brown et al.   MOLECULAR CELL

Inhibition of IκB Kinase (IKK) Protects Against Peripheral Nerve Dysfunction of Experimental Diabetes

(2014) Geeta Negi et al.   MOLECULAR NEUROBIOLOGY

An integrin β3–KRAS–RalB complex drives tumour stemness and resistance to EGFR inhibition

(2014) Laetitia Seguin et al.   NATURE CELL BIOLOGY

Inhibitors of NF-kappaB reverse cellular invasion and target gene upregulation in an experimental model of aggressive oral squamous cell carcinoma

(2014) Jeff Johnson et al.   ORAL ONCOLOGY

IKK2 Inhibition Attenuates Laser-Induced Choroidal Neovascularization

(2014) Huayi Lu et al.   PLoS One

A Phase I Clinical Trial of Systemically Delivered NEMO Binding Domain Peptide in Dogs with Spontaneous Activated B-Cell like Diffuse Large B-Cell Lymphoma

(2014) Georges Habineza Ndikuyeze et al.   PLoS One

NF- B, an Active Player in Human Cancers

(2014) Y. Xia et al.   Cancer Immunology Research

Molecular Basis of NF-κB Signaling

(2013) Johanna Napetschnig et al.   Annual Review of Biophysics

The anti-inflammatory drug BAY 11-7082 suppresses the MyD88-dependent signalling network by targeting the ubiquitin system

(2013) Sam Strickson et al.   BIOCHEMICAL JOURNAL

SC-514, a selective inhibitor of IKKβ attenuates RANKL-induced osteoclastogenesis and NF-κB activation

(2013) Qian Liu et al.   BIOCHEMICAL PHARMACOLOGY

Mesenchymal Differentiation Mediated by NF-κB Promotes Radiation Resistance in Glioblastoma

(2013) Krishna P.L. Bhat et al.   CANCER CELL

A mechanistic study of the proapoptotic effect of tolfenamic acid: involvement of NF- B activation

(2013) J. B. Jeong et al.   CARCINOGENESIS

Sulindac activates NF-κB signaling in colon cancer cells

(2013) Dessislava Mladenova et al.   Cell Communication and Signaling

Inhibition of I B kinase reduces the multiple organ dysfunction caused by sepsis in the mouse

(2013) S. M. Coldewey et al.   Disease Models & Mechanisms

Crystal Structure of a Human IκB Kinase β Asymmetric Dimer

(2013) Shenping Liu et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Deficiency of Innate and Acquired Immunity Caused by an IKBKB Mutation

(2013) Ulrich Pannicke et al.   NEW ENGLAND JOURNAL OF MEDICINE

Targeting BTK with Ibrutinib in Relapsed or Refractory Mantle-Cell Lymphoma

(2013) Michael L. Wang et al.   NEW ENGLAND JOURNAL OF MEDICINE

Aberrant IKKα and IKKβ cooperatively activate NF-κB and induce EGFR/AP1 signaling to promote survival and migration of head and neck cancer

(2013) L K Nottingham et al.   ONCOGENE

A Structural Basis for IκB Kinase 2 Activation Via Oligomerization-Dependent Trans Auto-Phosphorylation

(2013) Smarajit Polley et al.   PLOS BIOLOGY

Targeting Nuclear Factor-Kappa B to Overcome Resistance to Chemotherapy

(2013) P. Godwin et al.   Frontiers in Oncology

Myeloid-Specific IκB Kinase β Deficiency Decreases Atherosclerosis in Low-Density Lipoprotein Receptor–Deficient Mice

(2012) Se-Hyung Park et al.   ARTERIOSCLEROSIS THROMBOSIS AND VASCULAR BIOLOGY

Molecular insight in the multifunctional activities of Withaferin A

(2012) Wim Vanden Berghe et al.   BIOCHEMICAL PHARMACOLOGY

KrasG12D-Induced IKK2/β/NF-κB Activation by IL-1α and p62 Feedforward Loops Is Required for Development of Pancreatic Ductal Adenocarcinoma

(2012) Jianhua Ling et al.   CANCER CELL

Activity of the selective IκB kinase inhibitor BMS-345541 against T-cell acute lymphoblastic leukemia

(2012) Francesca Buontempo et al.   CELL CYCLE

NF- B, the first quarter-century: remarkable progress and outstanding questions

(2012) M. S. Hayden et al.   GENES & DEVELOPMENT

Somatic mutations in the notch, NF-KB, PIK3CA, and hedgehog pathways in human breast cancers

(2012) Xiang Jiao et al.   GENES CHROMOSOMES & CANCER

IKK biology

(2012) Fei Liu et al.   IMMUNOLOGICAL REVIEWS

NF-κB and the link between inflammation and cancer

(2012) Joseph A. DiDonato et al.   IMMUNOLOGICAL REVIEWS

An NF-κB pathway–mediated positive feedback loop amplifies Ras activity to pathological levels in mice

(2012) Jaroslaw Daniluk et al.   JOURNAL OF CLINICAL INVESTIGATION

Inhibition of Type I Interferon-Mediated Antiviral Action in Human Glioma Cells by the IKK Inhibitors BMS-345541 and TPCA-1

(2012) Ziyun Du et al.   JOURNAL OF INTERFERON AND CYTOKINE RESEARCH

Reduced cell proliferation by IKK2 depletion in a mouse lung-cancer model

(2012) Yifeng Xia et al.   NATURE CELL BIOLOGY

Screening for Novel LRRK2 Inhibitors Using a High-Throughput TR-FRET Cellular Assay for LRRK2 Ser935 Phosphorylation

(2012) Spencer B. Hermanson et al.   PLoS One

Molecular Marker Identification for Relapse Prediction in 5-FU-Based Adjuvant Chemotherapy in Gastric and Colorectal Cancers

(2012) Kazushige Ishida et al.   PLoS One

Novel cross-talk within the IKK family controls innate immunity

(2011) Kristopher Clark et al.   BIOCHEMICAL JOURNAL

An IκB kinase 2 inhibitor IMD-0354 suppresses the survival of adult T-cell leukemia cells

(2011) Shin Uota et al.   CANCER SCIENCE

Hallmarks of Cancer: The Next Generation

(2011) Douglas Hanahan et al.   CELL

FAS and NF-κB signalling modulate dependence of lung cancers on mutant EGFR

(2011) Trever G. Bivona et al.   NATURE

Comprehensive analysis of kinase inhibitor selectivity

(2011) Mindy I Davis et al.   NATURE BIOTECHNOLOGY

Inflammation meets cancer, with NF-κB as the matchmaker

(2011) Yinon Ben-Neriah et al.   NATURE IMMUNOLOGY

The novel NF-κB inhibitor IMD-0354 induces apoptosis in chronic lymphocytic leukemia

(2011) M Kanduri et al.   Blood Cancer Journal

Response and Resistance to NF- B Inhibitors in Mouse Models of Lung Adenocarcinoma

(2011) W. Xue et al.   Cancer Discovery

Cell-Selective Inhibition of NF- B Signaling Improves Therapeutic Index in a Melanoma Chemotherapy Model

(2011) T. Enzler et al.   Cancer Discovery

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

(2010) Subash C. Gupta et al.   Biochimica et Biophysica Acta-Gene Regulatory Mechanisms

Classical and/or alternative NF- B pathway activation in multiple myeloma

(2010) Y. N. Demchenko et al.   BLOOD

Cancer-Associated Fibroblasts Are Activated in Incipient Neoplasia to Orchestrate Tumor-Promoting Inflammation in an NF-κB-Dependent Manner

(2010) Neta Erez et al.   CANCER CELL

Requirement of the NF-κB Subunit p65/RelA for K-Ras–Induced Lung Tumorigenesis

(2010) Daniela S. Bassères et al.   CANCER RESEARCH

Non-canonical NF-κB signaling pathway

(2010) Shao-Cong Sun   CELL RESEARCH

Discovery of non-ETS gene fusions in human prostate cancer using next-generation RNA sequencing

(2010) D. Pflueger et al.   GENOME RESEARCH

Conditional ablation of Ikkb inhibits melanoma tumor development in mice

(2010) Jinming Yang et al.   JOURNAL OF CLINICAL INVESTIGATION

Inhibition of I B Kinase-  Protects Dopamine Neurons Against Lipopolysaccharide-Induced Neurotoxicity

(2010) F. Zhang et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

I-kappa-kinase-2 (IKK-2) inhibition potentiates vincristine cytotoxicity in non-Hodgkin's lymphoma

(2010) Ayad Al-Katib et al.   Molecular Cancer

IL-1β-driven neutrophilia preserves antibacterial defense in the absence of the kinase IKKβ

(2010) Li-Chung Hsu et al.   NATURE IMMUNOLOGY

NFKBIADeletion in Glioblastomas

(2010) Markus Bredel et al.   NEW ENGLAND JOURNAL OF MEDICINE

NF-κB addiction and its role in cancer: ‘one size does not fit all’

(2010) M M Chaturvedi et al.   ONCOGENE

IKKα and IKKβ Each Function to Regulate NF-κB Activation in the TNF-Induced/Canonical Pathway

(2010) Mazhar Adli et al.   PLoS One

Anti-inflammatory effect of a selective IκB kinase-beta inhibitor in rat lung in response to LPS and cigarette smoke

(2010) Saravanan Rajendrasozhan et al.   PULMONARY PHARMACOLOGY & THERAPEUTICS

Oncogenic Activation of NF- B

(2010) L. M. Staudt   Cold Spring Harbor Perspectives in Biology

Regulation of macrophage function in tumors: the multifaceted role of NF- B

(2009) T. Hagemann et al.   BLOOD

The proteasome load versus capacity balance determines apoptotic sensitivity of multiple myeloma cells to proteasome inhibition

(2009) G. Bianchi et al.   BLOOD

NF-κB, a Potential Therapeutic Target for the Treatment of Multiple Sclerosis

(2009) J. Yan et al.   CNS & Neurological Disorders-Drug Targets

Combined use of pharmacokinetic modeling and a steady-state delivery approach allows early assessment of IκB kinase-2 (IKK-2) target safety and efficacy

(2009) Po-Chang Chiang et al.   JOURNAL OF PHARMACEUTICAL SCIENCES

Novel Tight-Binding Inhibitory Factor- B Kinase (IKK-2) Inhibitors Demonstrate Target-Specific Anti-Inflammatory Activities in Cellular Assays and following Oral and Local Delivery in an in Vivo Model of Airway Inflammation

(2009) C. D. Sommers et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

A Novel, Highly Selective, Tight Binding I B Kinase-2 (IKK-2) Inhibitor: A Tool to Correlate IKK-2 Activity to the Fate and Functions of the Components of the Nuclear Factor- B Pathway in Arthritis-Relevant Cells and Animal Models

(2009) G. Mbalaviele et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Systematic RNA interference reveals that oncogenic KRAS-driven cancers require TBK1

(2009) David A. Barbie et al.   NATURE

Requirement for NF-κB signalling in a mouse model of lung adenocarcinoma

(2009) Etienne Meylan et al.   NATURE

Mutations of multiple genes cause deregulation of NF-κB in diffuse large B-cell lymphoma

(2009) Mara Compagno et al.   NATURE

Interactions between PD-1 and PD-L1 promote tolerance by blocking the TCR–induced stop signal

(2009) Brian T Fife et al.   NATURE IMMUNOLOGY

Activation of the NLRP3 inflammasome in dendritic cells induces IL-1β–dependent adaptive immunity against tumors

(2009) François Ghiringhelli et al.   NATURE MEDICINE

The NF-κB-independent functions of IKK subunits in immunity and cancer

(2009) Alain Chariot   TRENDS IN CELL BIOLOGY

The NF- B Family of Transcription Factors and Its Regulation

(2009) A. Oeckinghaus et al.   Cold Spring Harbor Perspectives in Biology

Berberine Modifies Cysteine 179 of I B  Kinase, Suppresses Nuclear Factor- B-Regulated Antiapoptotic Gene Products, and Potentiates Apoptosis

(2008) M. K. Pandey et al.   CANCER RESEARCH

Endothelial Cell-Specific NF-κB Inhibition Protects Mice from Atherosclerosis

(2008) Ralph Gareus et al.   Cell Metabolism

“Re-educating” tumor-associated macrophages by targeting NF-κB

(2008) Thorsten Hagemann et al.   JOURNAL OF EXPERIMENTAL MEDICINE

NF-κB in inflammatory bowel disease

(2008) I. Atreya et al.   JOURNAL OF INTERNAL MEDICINE

Benzoxathiole Derivative Blocks Lipopolysaccharide-Induced Nuclear Factor- B Activation and Nuclear Factor- B-Regulated Gene Transcription through Inactivating Inhibitory  B Kinase  

(2008) B. H. Kim et al.   MOLECULAR PHARMACOLOGY

Compensatory IKK  activation of classical NF- B signaling during IKK  inhibition identified by an RNA interference sensitization screen

(2008) L. T. Lam et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Molecular subtypes of diffuse large B-cell lymphoma arise by distinct genetic pathways

(2008) G. Lenz et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Cooperative signaling through the signal transducer and activator of transcription 3 and nuclear factor- B pathways in subtypes of diffuse large B-cell lymphoma

(2007) L. T. Lam et al.   BLOOD