Id: acc2527
Group: 2sens
Protein: Nrf2
Gene Symbol: NFE2L2
Protein Id: Q16236
Protein Name: NF2L2_HUMAN
PTM: phosphorylation
Site: unclear
Site Sequence:
Disease Category: Cancer
Disease: Neuroblastoma
Disease Subtype:
Disease Cellline: IMR-32
Disease Info:
Drug: DMAT(CK2 inhibitor)
Drug Info: "DMAT is a potent and specific CK2 inhibitor with an IC50 value of 130 nM, primarily used for scientific research and not approved for clinical applications. "
Effect: relate
Effect Info: DMAT inhibits the growth or drug resistance of tumor cells by suppressing the phosphorylation of Nrf2.
Note:
Score: 5.0
Pubmed(PMID): 18273910
Sentence Index:
Sentence:

Sequence & Structure:

MMDLELPPPGLPSQQDMDLIDILWRQDIDLGVSREVFDFSQRRKEYELEKQKKLEKERQEQLQKEQEKAFFAQLQLDEETGEFLPIQPAQHIQSETSGSANYSQVAHIPKSDALYFDDCMQLLAQTFPFVDDNEVSSATFQSLVPDIPGHIESPVFIATNQAQSPETSVAQVAPVDLDGMQQDIEQVWEELLSIPELQCLNIENDKLVETTMVPSPEAKLTEVDNYHFYSSIPSMEKEVGNCSPHFLNAFEDSFSSILSTEDPNQLTVNSLNSDATVNTDFGDEFYSAFIAEPSISNSMPSPATLSHSLSELLNGPIDVSDLSLCKAFNQNHPESTAEFNDSDSGISLNTSPSVASPEHSVESSSYGDTLLGLSDSEVEELDSAPGSVKQNGPKTPVHSSGDMVQPLSPSQGQSTHVHDAQCENTPEKELPVSPGHRKTPFTKDKHSSRLEAHLTRDELRAKALHIPFPVEKIINLPVVDFNEMMSKEQFNEAQLALIRDIRRRGKNKVAAQNCRKRKLENIVELEQDLDHLKDEKEKLLKEKGENDKSLHLLKKQLSTLYLEVFSMLRDEDGKPYSPSEYSLQQTRDGNVFLVPKSKKPDVKKN

Select PDB:

Known Drugs:

source: Multi-Sources

(see table)

Target Drug name MOA Phase Status Disease Source
NFE2L2 OMAVELOXOLONE Nuclear factor erythroid 2-related factor 2 activator 4 - Friedreich ataxia FDA
NFE2L2 BARDOXOLONE METHYL Keap1/Nrf2 inhibitor 3 Terminated diabetic nephropathy ClinicalTrials
NFE2L2 BARDOXOLONE METHYL Keap1/Nrf2 inhibitor 3 Terminated Autosomal dominant polycystic kidney disease ClinicalTrials
NFE2L2 BARDOXOLONE METHYL Keap1/Nrf2 inhibitor 3 Terminated pulmonary hypertension ClinicalTrials
NFE2L2 BARDOXOLONE METHYL Keap1/Nrf2 inhibitor 2 Completed diabetic nephropathy ClinicalTrials
NFE2L2 BARDOXOLONE METHYL Keap1/Nrf2 inhibitor 2 Withdrawn melanoma ClinicalTrials
NFE2L2 BARDOXOLONE METHYL Keap1/Nrf2 inhibitor 2 Completed pulmonary arterial hypertension ClinicalTrials
NFE2L2 BARDOXOLONE METHYL Keap1/Nrf2 inhibitor 2 Completed chronic kidney disease ClinicalTrials
NFE2L2 OMAVELOXOLONE Nuclear factor erythroid 2-related factor 2 activator 2 Completed breast cancer ClinicalTrials
NFE2L2 BARDOXOLONE METHYL Keap1/Nrf2 inhibitor 2 Completed Alport syndrome ClinicalTrials
NFE2L2 OMAVELOXOLONE Nuclear factor erythroid 2-related factor 2 activator 2 Active, not recruiting Friedreich ataxia ClinicalTrials
NFE2L2 BARDOXOLONE METHYL Keap1/Nrf2 inhibitor 2 Completed COVID-19 ClinicalTrials
NFE2L2 BARDOXOLONE METHYL Keap1/Nrf2 inhibitor 1 Completed neoplasm ClinicalTrials
ClinicalTrials
NFE2L2 OMAVELOXOLONE Nuclear factor erythroid 2-related factor 2 activator 1 Completed melanoma ClinicalTrials
NFE2L2 BARDOXOLONE METHYL Keap1/Nrf2 inhibitor 1 Completed liver disease ClinicalTrials
NFE2L2 BARDOXOLONE METHYL Keap1/Nrf2 inhibitor 1 Completed lymphoid neoplasm ClinicalTrials
ClinicalTrials
NFE2L2 BARDOXOLONE METHYL Keap1/Nrf2 inhibitor 1 Terminated liver disease ClinicalTrials
NFE2L2 OMAVELOXOLONE Nuclear factor erythroid 2-related factor 2 activator 1 Completed liver disease ClinicalTrials
NFE2L2 BARDOXOLONE METHYL Keap1/Nrf2 inhibitor 1 Terminated pancreatic carcinoma ClinicalTrials
NFE2L2 OMAVELOXOLONE Nuclear factor erythroid 2-related factor 2 activator 1 Not yet recruiting Friedreich ataxia ClinicalTrials

Note: Only show clinically investigational or approved drugs with protein targets.

Protein Tractability:

source: Open Targets
Small molecule
Antibody
PROTAC
Other modalities
Approved Drug
Advanced Clinical
Phase 1 Clinical
Structure with Ligand
High-Quality Ligand
High-Quality Pocket
Med-Quality Pocket
Druggable Family
Approved Drug
Advanced Clinical
Phase 1 Clinical
UniProt loc high conf
GO CC high conf
UniProt loc med conf
UniProt SigP or TMHMM
GO CC med conf
Human Protein Atlas loc
Approved Drug
Advanced Clinical
Phase 1 Clinical
Literature
UniProt Ubiquitination
Database Ubiquitination
Half-life Data
Small Molecule Binder
Approved Drug
Advanced Clinical
Phase 1 Clinical

PTM Intensity:

source: CPTAC

No intensity data of this site,
show all other sites!

NFE2L2-Ser199
Cancer Intensity
BRCA
COAD
HGSC
ccRCC 0.409
GBM
HNSC 0.933
LUAD -0.702
LUSC -1.39
non_ccRCC
PDAC 1.168
UCEC -0.418
NFE2L2-Ser417
Cancer Intensity
BRCA
COAD
HGSC
ccRCC 0.728
GBM
HNSC -0.056
LUAD -1.197
LUSC -1.225
non_ccRCC
PDAC 0.88
UCEC 0.87
NFE2L2-Thr194
Cancer Intensity
BRCA
COAD
HGSC
ccRCC
GBM
HNSC -0.617
LUAD -0.536
LUSC
non_ccRCC
PDAC
UCEC 1.154
NFE2L2-Thr195
Cancer Intensity
BRCA
COAD
HGSC
ccRCC -0.712
GBM
HNSC -0.212
LUAD -0.543
LUSC
non_ccRCC
PDAC
UCEC 1.467

PTM-Disease Association:

source: PTMD
Residue Position State Disease Class PMID
- - D Clear cell renal cell carcinoma Ubiquitination 32128917
- - D Gastric cancer Ubiquitination 32605589
- - P Esophageal squamous cell carcinoma Phosphorylation 33390848
- - U Clear cell renal cell carcinoma Phosphorylation 32128917
- - U Cervical cancer Ubiquitination 36527747

State Note: Based on the distinct PTM states in diseases, PTMD classified all disease-associated PTMs into six classes, including whether the up-regulation (U) or down-regulation (D) of PTM levels, the absence (A) or presence (P) of PTMs, and the creation (C) or disruption (N) of PTM sites are associated with diseases.

PTM-Drug Perturbation Response:

source: DecryptM

No data.

Function score:

source: funscoR

No data.

Cross Links: