Property Summary

NCBI Gene PubMed Count 181
Grant Count 230
R01 Count 141
Funding $19,868,330.97
PubMed Score 820.70
PubTator Score 408.44

Knowledge Summary

Patent

No data available

Expression

  Differential Expression (3)

Disease log2 FC p
osteosarcoma -1.006 0.005
astrocytoma 1.100 0.002
lung cancer 1.600 0.000

Synonym

Accession Q14145 B3KPD5 Q6LEP0 Q8WTX1 Q9BPY9
Symbols INrf2
KLHL19

Gene

PDB

2FLU   3ZGC   4IFL   1U6D   1ZGK   3VNG   3VNH   3ZGD   4CXI   4CXJ   4CXT   4IFJ   4IFN   4IN4   4IQK   4L7B   4L7C   4L7D   4N1B   4XMB   5DAD   5DAF  

MLP Assay (12)

AID Type Active / Inconclusive / Inactive Description
504523 screening 489 / 288 / 336339 Fluorescence polarization to screen for inhibitors that disrupt the protein-protein interaction between Keap1 and Nrf2 Measured in Biochemical System Using Plate Reader - 2119-01_Inhibitor_SinglePoint_HTS_Activity
504540 summary 1 / 0 / 0 Broad Institute HTS fluorescence polarization assay for inhibitors of Keap1-Nrf2 interaction Inhibitor Probe Project
588683 confirmatory 76 / 0 / 324 Fluorescence polarization to screen for inhibitors that disrupt the protein-protein interaction between Keap1 and Nrf2 Measured in Biochemical System Using Plate Reader - 2119-01_Inhibitor_Dose_CherryPick_Activity
651798 confirmatory 15 / 0 / 77 Fluorescence polarization to screen for inhibitors that disrupt the protein-protein interaction between Keap1 and Nrf2 Measured in Biochemical System Using Plate Reader - 2119-01_Inhibitor_Dose_DryPowder_Activity
651801 confirmatory 15 / 0 / 77 Fluorescence polarization to screen for inhibitors that disrupt the protein-protein interaction between Keap1 and Nrf2 Measured in Biochemical System Using Plate Reader - 2119-01_Inhibitor_Dose_DryPowder_Activity_Set2
651806 confirmatory 9 / 0 / 83 Fluorescence polarization to screen for inhibitors that disrupt the protein-protein interaction between Keap1 and Nrf2 Measured in Biochemical System Using Plate Reader - 2119-01_Inhibitor_Dose_DryPowder_Activity_Set3
651823 confirmatory 31 / 0 / 369 Thermal shift assay to identify compound binding to Kelch domain of Keap1 protein Measured in Biochemical System Using RT-PCR - 2119-02_Inhibitor_Dose_CherryPick_Activity
651829 confirmatory 27 / 0 / 65 Thermal shift assay to identify compound binding to Kelch domain of Keap1 protein Measured in Biochemical System Using RT-PCR - 2119-02_Inhibitor_Dose_DryPowder_Activity
651833 confirmatory 13 / 0 / 79 Nrf2 PathHunter Nuclear Translocation assay in U2OS cells Measured in Cell-Based System Using Plate Reader - 2119-04_Inhibitor_Dose_DryPowder_Activity
651834 confirmatory 1 / 0 / 13 Fluorescence polarization to screen for inhibitors that disrupt the protein-protein interaction between Keap1 and Nrf2 Measured in Biochemical System Using Plate Reader - 2119-01_Inhibitor_Dose_DryPowder_Activity_Set4
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Gene RIF (156)

PMID Text
26987716 expression of Nrf2-Keap1 is abnormal in osteosarcoma tissue and shows significant clinical relevance for determining the prognosis of osteosarcoma
26602019 findings reveal that Keap1 regulates cell migration by affecting the subcellular localization and activity of cortactin independently of its role in oxidant stress responses.
26551706 Accumulating evidence suggests that dysregulation of Keap1-Nrf2 pathway resulting in constitutively active Nrf2 and increased expression of cytoprotective Nrf2 target genes, has a pivotal role in cancer. [review]
26551704 Studies propose that Keap1 activity and Nrf2 are regulated by interactions of Trx1 system enzymes with oxidants. [review]
26551700 Studies demonstrate that Keap1-Nrf2 pathway is important to orchestrate an elaborate genetic program that enhances the intrinsic cytoprotective functions, including drug metabolizing, antioxidant and antiinflammatory networks. [review]
26527616 Keap1 utilizes multiple cysteine residues specifically and/or collaboratively as sensors for the detection of a wide range of environmental stresses.
26453926 that targeted repression of Keap1 and activation of Nrf2 pathway, in part, underlies the protective effects of miR-7 against 1-methyl-4-phenylpyridinium (MPP+)-induced toxicity in SH-SY5Y
26350055 Up-regulation of KEAP1 is associated with carcinogenesis and progression of Salivary Adenoid Cystic Carcinoma.
26301506 In cells with functional KEAP1, RTA 405 increased NRF2 levels, but not IKKbeta or BCL2 levels, and did not increase cell proliferation or survival.
26233704 The Nrf2-Keap1 pathway is the major regulator of cytoprotective responses to oxidative and electrophilic stress. (Review)
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AA Sequence

MQPDPRPSGAGACCRFLPLQSQCPEGAGDAVMYASTECKAEVTPSQHGNRTFSYTLEDHTKQAFGIMNEL      1 - 70
RLSQQLCDVTLQVKYQDAPAAQFMAHKVVLASSSPVFKAMFTNGLREQGMEVVSIEGIHPKVMERLIEFA     71 - 140
YTASISMGEKCVLHVMNGAVMYQIDSVVRACSDFLVQQLDPSNAIGIANFAEQIGCVELHQRAREYIYMH    141 - 210
FGEVAKQEEFFNLSHCQLVTLISRDDLNVRCESEVFHACINWVKYDCEQRRFYVQALLRAVRCHSLTPNF    211 - 280
LQMQLQKCEILQSDSRCKDYLVKIFEELTLHKPTQVMPCRAPKVGRLIYTAGGYFRQSLSYLEAYNPSDG    281 - 350
TWLRLADLQVPRSGLAGCVVGGLLYAVGGRNNSPDGNTDSSALDCYNPMTNQWSPCAPMSVPRNRIGVGV    351 - 420
IDGHIYAVGGSHGCIHHNSVERYEPERDEWHLVAPMLTRRIGVGVAVLNRLLYAVGGFDGTNRLNSAECY    421 - 490
YPERNEWRMITAMNTIRSGAGVCVLHNCIYAAGGYDGQDQLNSVERYDVETETWTFVAPMKHRRSALGIT    491 - 560
VHQGRIYVLGGYDGHTFLDSVECYDPDTDTWSEVTRMTSGRSGVGVAVTMEPCRKQIDQQNCTC          561 - 624
//

Text Mined References (189)

PMID Year Title
26987716 2016 Expression of the Nrf2 and Keap1 proteins and their clinical significance in osteosarcoma.
26602019 2015 The subcellular localization and activity of cortactin is regulated by acetylation and interaction with Keap1.
26551706 2015 Dysregulation of the Keap1-Nrf2 pathway in cancer.
26551704 2015 Interplay between cytosolic disulfide reductase systems and the Nrf2/Keap1 pathway.
26551700 2015 The spatiotemporal regulation of the Keap1-Nrf2 pathway and its importance in cellular bioenergetics.
26527616 2015 Characterizations of Three Major Cysteine Sensors of Keap1 in Stress Response.
26453926 2015 MicroRNA-7 activates Nrf2 pathway by targeting Keap1 expression.
26350055 2016 Expression of LC3, LAMP2, KEAP1 and NRF2 in Salivary Adenoid Cystic Carcinoma.
26301506 2015 Cancer Cell Growth Is Differentially Affected by Constitutive Activation of NRF2 by KEAP1 Deletion and Pharmacological Activation of NRF2 by the Synthetic Triterpenoid, RTA 405.
26233704 2015 Antioxidant responses and cellular adjustments to oxidative stress.
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