Id: acc1647
Group: 2sens
Protein: STAT3
Gene Symbol: STAT3
Protein Id: P40763
Protein Name: STAT3_HUMAN
PTM: phosphorylation
Site: Tyr705
Site Sequence: EADPGSAAPYLKTKFICVTPT
Disease Category: Cancer
Disease: Lung Cancer
Disease Subtype: "LUAD, gefitinib-resistant"
Disease Cellline: PC9GR
Disease Info:
Drug: osimertinib
Drug Info: "Osimertinib is a third-generation, irreversible epidermal growth factor receptor tyrosine kinase inhibitor (EGFR TKI) approved for the treatment of metastatic non-small cell lung cancer (NSCLC) with EGFR T790M mutation and as first-line therapy for EGFR exon 19 deletions or exon 21 (L858R) substitution mutations."
Effect: inhibit
Effect Info: Gefitinib and osimertinib increased STAT3 phosphorylation (p-STAT3) in drug-resistant EGFRT790M and EGFRC797S tumor cells. The Notch inhibitor (DBZ) simultaneously induced a p-STAT3-dependent substantial decrease in the level of transcriptional repressor HES1 when used in combination with gefitinib or osimertinib treatment.
Note:
Score: 5.0
Pubmed(PMID): 31671073
Sentence Index:
Sentence:

Sequence & Structure:

MAQWNQLQQLDTRYLEQLHQLYSDSFPMELRQFLAPWIESQDWAYAASKESHATLVFHNLLGEIDQQYSRFLQESNVLYQHNLRRIKQFLQSRYLEKPMEIARIVARCLWEESRLLQTAATAAQQGGQANHPTAAVVTEKQQMLEQHLQDVRKRVQDLEQKMKVVENLQDDFDFNYKTLKSQGDMQDLNGNNQSVTRQKMQQLEQMLTALDQMRRSIVSELAGLLSAMEYVQKTLTDEELADWKRRQQIACIGGPPNICLDRLENWITSLAESQLQTRQQIKKLEELQQKVSYKGDPIVQHRPMLEERIVELFRNLMKSAFVVERQPCMPMHPDRPLVIKTGVQFTTKVRLLVKFPELNYQLKIKVCIDKDSGDVAALRGSRKFNILGTNTKVMNMEESNNGSLSAEFKHLTLREQRCGNGGRANCDASLIVTEELHLITFETEVYHQGLKIDLETHSLPVVVISNICQMPNAWASILWYNMLTNNPKNVNFFTKPPIGTWDQVAEVLSWQFSSTTKRGLSIEQLTTLAEKLLGPGVNYSGCQITWAKFCKENMAGKGFSFWVWLDNIIDLVKKYILALWNEGYIMGFISKERERAILSTKPPGTFLLRFSESSKEGGVTFTWVEKDISGKTQIQSVEPYTKQQLNNMSFAEIIMGYKIMDATNILVSPLVYLYPDIPKEEAFGKYCRPESQEHPEADPGSAAPYLKTKFICVTPTTCSNTIDLPMSPRTLDSLMQFGNNGEGAEPSAGGQFESLTFDMELTSECATSPM

Select PDB:

Known Drugs:

source: Multi-Sources

(see table)

Target Drug name MOA Phase Status Disease Source
STAT3 DANVATIRSEN STAT-3 mRNA 3'UTR antisense inhibitor 2 Recruiting head and neck squamous cell carcinoma ClinicalTrials
STAT3 DANVATIRSEN STAT-3 mRNA 3'UTR antisense inhibitor 2 Active, not recruiting non-small cell lung carcinoma ClinicalTrials
STAT3 DANVATIRSEN STAT-3 mRNA 3'UTR antisense inhibitor 2 Completed non-small cell lung carcinoma ClinicalTrials
STAT3 DANVATIRSEN STAT-3 mRNA 3'UTR antisense inhibitor 1 Completed hepatocellular carcinoma ClinicalTrials
STAT3 DANVATIRSEN STAT-3 mRNA 3'UTR antisense inhibitor 1 Active, not recruiting head and neck squamous cell carcinoma ClinicalTrials
STAT3 DANVATIRSEN STAT-3 mRNA 3'UTR antisense inhibitor 1 Completed diffuse large B-cell lymphoma ClinicalTrials
ClinicalTrials
STAT3 DANVATIRSEN STAT-3 mRNA 3'UTR antisense inhibitor 1 Active, not recruiting neoplasm ClinicalTrials
STAT3 DANVATIRSEN STAT-3 mRNA 3'UTR antisense inhibitor 1 Active, not recruiting non-small cell lung carcinoma ClinicalTrials
STAT3 DANVATIRSEN STAT-3 mRNA 3'UTR antisense inhibitor 1 Completed non-Hodgkins lymphoma ClinicalTrials
STAT3 DANVATIRSEN STAT-3 mRNA 3'UTR antisense inhibitor 1 Active, not recruiting urinary bladder cancer ClinicalTrials
STAT3 DANVATIRSEN STAT-3 mRNA 3'UTR antisense inhibitor 1 Completed cancer 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
STAT3-Tyr705
Cancer Intensity
BRCA 0.868
COAD
HGSC
ccRCC
GBM 0.383
HNSC
LUAD -0.032
LUSC
non_ccRCC -1.398
PDAC 1.121
UCEC -0.942

PTM-Disease Association:

source: PTMD
Residue Position State Disease Class PMID
Y 705 D Triple-negative breast cancer Phosphorylation 36017196
Y 705 D Inflammatory disease Phosphorylation 24063605
Y 705 N Bladder cancer Phosphorylation 18939995
Y 705 P Breast cancer/tumor/carcinoma Phosphorylation 23350355 ;  22374428 ;  23446809
Y 705 P Colon cancer/carcinoma Phosphorylation 22754353 ;  21840932
Y 705 U Experimental autoimmune encephalomyelitis Phosphorylation 32094172
Y 705 U Laryngeal cancer Phosphorylation 27181202
Y 705 U Lung cancer Phosphorylation 34543857
Y 705 U Malignant gliomas Phosphorylation 23740516
Y 705 U Multiple sclerosis Phosphorylation 32094172
Y 705 U Myeloma Phosphorylation 22210382
Y 705 U Neurofibromatosis Phosphorylation 23318430
Y 705 U Non-Hodgkin's lymphoma Phosphorylation 30054295
Y 705 U Prostate cancer Phosphorylation 19147545 ;  19147545
Y 705 U T-cell lymphoma Phosphorylation 35882439
Y 705 U Fibrosarcoma Phosphorylation 21575192
Y 705 U Head and neck squamous cell carcinoma Phosphorylation 21281788
Y 705 U Esophageal carcinoma Phosphorylation 33986510
Y 705 U Clear cell kidney cancer Phosphorylation 24615012
Y 705 U Acute myelogenous leukemia Phosphorylation 34525179
Y 705 U B-cell lymphoma Phosphorylation 22116549
Y 705 U Breast cancer Phosphorylation 17967179 ;  17967179 ;  18353781 ;  35927628
Y 705 U Esophageal squamous cell carcinoma Phosphorylation 23676499
Y 705 U Triple-negative breast cancer Phosphorylation 34066153 ;  35091679
Y 705 U Pancreatic cancer Phosphorylation 37548811 ;  36374556
Y 705 U Colorectal cancer Phosphorylation 36266267
Y 705 U Glioblastoma Phosphorylation 34411567 ;  20455003
Y 705 U Melanoma Phosphorylation 35184394 ;  22899991
Y 705 U Multiple myeloma Phosphorylation 34782371
Y 705 U Breast cancer/tumor/carcinoma Phosphorylation 24707243
Y 705 U Cancer Phosphorylation 23145121
Y 705 U Colon adenocarcinoma Phosphorylation 34270850
Y 705 U Hepatocellular carcinoma/hepatocarcinoma/hepatoma Phosphorylation 21311975
Y 705 U Pancreatic cancer/carcinoma/adenocarcinoma Phosphorylation 18519681
Y 705 U Prostate cancer/carcinoma/adenocarcinoma Phosphorylation 22307624 ;  19147545
Y 705 U Renal cancer/carcinoma Phosphorylation 22982675
Y 705 U Renal cell carcinoma Phosphorylation 22899991
Y 705 U Bladder cancer Phosphorylation 34326684
Y 705 U Glioblastoma multiforme Phosphorylation 35670018
Y 705 U Nasopharyngeal carcinoma Phosphorylation 33824475
Y 705 U Hepatocellular carcinoma Phosphorylation 22153071

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: