Id: acc1789
Group: 2sens
Protein: GSK3beta
Gene Symbol: GSK3B
Protein Id: P49841
Protein Name: GSK3B_HUMAN
PTM: phosphorylation
Site: Ser9
Site Sequence: -MSGRPRTTSFAESCKPVQQP
Disease Category: Cancer
Disease: Breast Cancer
Disease Subtype: tamoxifen-resistant
Disease Cellline: MCF7(TamR)
Disease Info:
Drug: tamoxifen
Drug Info: "Tamoxifen is a selective estrogen receptor modulator (SERM) used primarily for the treatment of estrogen receptor-positive breast cancer in women, including adjuvant therapy, advanced cases, and recurrent disease, by competitively inhibiting estrogen binding to its receptor and suppressing cancer cell proliferation."
Effect: modulate
Effect Info: "In breast cancer patients who eventually relapsed after tamoxifen treatment, the inhibitory phosphorylation of GSK3beta at serine 9 was significantly decreased, suggesting that the activation of GSK3beta may be associated with the tamoxifen - resistant phenotype."
Note:
Score: 4.0
Pubmed(PMID): 21044952
Sentence Index:
Sentence:

Sequence & Structure:

MSGRPRTTSFAESCKPVQQPSAFGSMKVSRDKDGSKVTTVVATPGQGPDRPQEVSYTDTKVIGNGSFGVVYQAKLCDSGELVAIKKVLQDKRFKNRELQIMRKLDHCNIVRLRYFFYSSGEKKDEVYLNLVLDYVPETVYRVARHYSRAKQTLPVIYVKLYMYQLFRSLAYIHSFGICHRDIKPQNLLLDPDTAVLKLCDFGSAKQLVRGEPNVSYICSRYYRAPELIFGATDYTSSIDVWSAGCVLAELLLGQPIFPGDSGVDQLVEIIKVLGTPTREQIREMNPNYTEFKFPQIKAHPWTKVFRPRTPPEAIALCSRLLEYTPTARLTPLEACAHSFFDELRDPNVKLPNGRDTPALFNFTTQELSSNPPLATILIPPHARIQAAASTPTNATAASDANTGDRGQTNNAASASASNST

Select PDB:

Known Drugs:

source: Multi-Sources

(see table)

Target Drug name MOA Phase Status Disease Source
GSK3B LITHIUM CARBONATE Glycogen synthase kinase-3 inhibitor 4 - bipolar I disorder DailyMed
DailyMed
DailyMed
GSK3B LITHIUM CARBONATE Glycogen synthase kinase-3 inhibitor 4 Completed bipolar I disorder ClinicalTrials
ClinicalTrials
GSK3B LITHIUM CARBONATE Glycogen synthase kinase-3 inhibitor 4 Withdrawn bipolar I disorder ClinicalTrials
GSK3B LITHIUM CARBONATE Glycogen synthase kinase-3 inhibitor 4 Unknown status bipolar I disorder ClinicalTrials
ClinicalTrials
GSK3B LITHIUM CITRATE Glycogen synthase kinase-3 inhibitor 4 - bipolar I disorder DailyMed
GSK3B LITHIUM CARBONATE Glycogen synthase kinase-3 inhibitor 4 Completed depressive disorder ClinicalTrials
ClinicalTrials
ClinicalTrials
ClinicalTrials
ClinicalTrials
ClinicalTrials
ClinicalTrials
GSK3B LITHIUM CARBONATE Glycogen synthase kinase-3 inhibitor 4 Terminated depressive disorder ClinicalTrials
GSK3B LITHIUM CARBONATE Glycogen synthase kinase-3 inhibitor 4 Unknown status depressive disorder ClinicalTrials
ClinicalTrials
ClinicalTrials
GSK3B LITHIUM CARBONATE Glycogen synthase kinase-3 inhibitor 4 - major depressive disorder DailyMed
GSK3B LITHIUM CARBONATE Glycogen synthase kinase-3 inhibitor 4 Recruiting depressive disorder ClinicalTrials
GSK3B LITHIUM CARBONATE Glycogen synthase kinase-3 inhibitor 4 Completed bipolar disorder ClinicalTrials
ClinicalTrials
ClinicalTrials
ClinicalTrials
ClinicalTrials
ClinicalTrials
ClinicalTrials
ClinicalTrials
ClinicalTrials
ClinicalTrials
ClinicalTrials
ClinicalTrials
ClinicalTrials
ClinicalTrials
ClinicalTrials
ClinicalTrials
ClinicalTrials
ClinicalTrials
ClinicalTrials
ClinicalTrials
ClinicalTrials
ClinicalTrials
ClinicalTrials
GSK3B LITHIUM CARBONATE Glycogen synthase kinase-3 inhibitor 4 Unknown status bipolar disorder ClinicalTrials
ClinicalTrials
ClinicalTrials
ClinicalTrials
GSK3B LITHIUM CARBONATE Glycogen synthase kinase-3 inhibitor 4 - bipolar disorder DailyMed
DailyMed
DailyMed
DailyMed
DailyMed
DailyMed
DailyMed
DailyMed
DailyMed
DailyMed
DailyMed
DailyMed
DailyMed
DailyMed
DailyMed
DailyMed
DailyMed
DailyMed
DailyMed
DailyMed
DailyMed
DailyMed
DailyMed
DailyMed
DailyMed
DailyMed
DailyMed
DailyMed
DailyMed
DailyMed
DailyMed
DailyMed
DailyMed
DailyMed
DailyMed
DailyMed
DailyMed
DailyMed
DailyMed
DailyMed
DailyMed
DailyMed
DailyMed
DailyMed
DailyMed
GSK3B LITHIUM CARBONATE Glycogen synthase kinase-3 inhibitor 4 Recruiting bipolar disorder ClinicalTrials
ClinicalTrials
GSK3B LITHIUM CARBONATE Glycogen synthase kinase-3 inhibitor 4 Terminated bipolar disorder ClinicalTrials
ClinicalTrials
ClinicalTrials
ClinicalTrials
GSK3B LITHIUM CARBONATE Glycogen synthase kinase-3 inhibitor 4 Withdrawn bipolar disorder ClinicalTrials
ClinicalTrials
GSK3B LITHIUM CARBONATE Glycogen synthase kinase-3 inhibitor 3 Completed stroke ClinicalTrials
GSK3B LITHIUM CARBONATE Glycogen synthase kinase-3 inhibitor 3 Recruiting internal carotid artery stenosis ClinicalTrials
GSK3B LITHIUM CARBONATE Glycogen synthase kinase-3 inhibitor 3 Completed aggressive behavior ClinicalTrials
GSK3B LITHIUM CARBONATE Glycogen synthase kinase-3 inhibitor 3 Recruiting carotid artery disease ClinicalTrials
GSK3B LITHIUM CARBONATE Glycogen synthase kinase-3 inhibitor 3 Active, not recruiting autism spectrum disorder ClinicalTrials
GSK3B LITHIUM CARBONATE Glycogen synthase kinase-3 inhibitor 3 Completed conduct disorder ClinicalTrials
GSK3B LITHIUM CARBONATE Glycogen synthase kinase-3 inhibitor 3 Terminated anxiety ClinicalTrials
GSK3B LITHIUM CARBONATE Glycogen synthase kinase-3 inhibitor 3 Completed treatment resistant depression ClinicalTrials
GSK3B LITHIUM CARBONATE Glycogen synthase kinase-3 inhibitor 3 Completed bipolar I disorder ClinicalTrials
ClinicalTrials
ClinicalTrials
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
GSK3B-Ser9
Cancer Intensity
BRCA
COAD -0.707
HGSC 0.707
ccRCC
GBM
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC

PTM-Disease Association:

source: PTMD
Residue Position State Disease Class PMID
S 9 D Diabetes mellitus Phosphorylation 15033922
S 9 D Pancreatic cancer/carcinoma/adenocarcinoma Phosphorylation 23408967
S 9 D Triple-negative breast cancer Phosphorylation 35090098
S 9 D Alzheimer's disease Phosphorylation 22278060
S 9 D Schizophrenia Phosphorylation 14745448
S 9 D Parkinson's disease Phosphorylation 27609071
S 9 P Breast cancer Phosphorylation 36632451
S 9 P Ovarian cancer/carcinoma Phosphorylation 23667667
S 9 P Lung cancer/carcinoma Phosphorylation 23149922
S 9 P Liver cancer Phosphorylation 23325562
S 9 P Gastric cancer Phosphorylation 23123500
S 9 U Lung adenocarcinoma Phosphorylation 33808696
S 9 U Hepatocellular carcinoma Phosphorylation 34484860
S 9 U Breast cancer Phosphorylation 17495324 ;  35173161 ;  17495324
S 9 U Non-small cell lung cancer Phosphorylation 36869126
S 9 U Lung cancer/carcinoma Phosphorylation 23514933
S 9 U Melanoma Phosphorylation 35347072
S 9 U Systemic scleroderma Phosphorylation 35853487
S 9 U Systemic lupus erythematosus Phosphorylation 23735868
S 9 U Squamous cell carcinoma Phosphorylation 18606491
S 9 U Skin cancer Phosphorylation 18606491
S 9 U Papillomas Phosphorylation 18606491
S 9 U Ovarian cancer Phosphorylation 15208673
S 9 U Neuroblastoma Phosphorylation 30154149
S 9 U Major depressive disorder Phosphorylation 22622071
S 9 U Lymphoma Phosphorylation 20224723
S 9 U Granulomatosis with polyangiitis Phosphorylation 37720230
S 9 U Dilated cardiomyopathy Phosphorylation 37852321
S 9 U Diabetes mellitus Phosphorylation 35835217
S 9 U Cardiomyopathy Phosphorylation 37852321
S 9 U Breast cancer/tumor/carcinoma Phosphorylation 17495324 ;  27494834
S 9 U Bipolar disorder Phosphorylation 16806104
S 9 U Alzheimer's disease Phosphorylation 22278060

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
Protein Gene PTM Position Modified sequence Cell Drug pEC50 Regulation Experiment
P49841 GSK3B P Ser9 TTS(ph)FAESCKPVQQPSAFGSMK HeLa CUDC101 1 up
P49841 GSK3B P Ser9 TTS(ph)FAESCKPVQQPSAFGSMK A459 MK2206 7.2049 down
P49841 GSK3B P Ser9 TTS(ph)FAESCKPVQQPSAFGSMK A459 SelumetinibMK2206-1to2 7.4614 down
P49841 GSK3B P Ser9 TTS(ph)FAESCKPVQQPSAFGSMK A459 SelumetinibMK2206-3to1 7.0611 down
P49841 GSK3B P Ser9 TTS(ph)FAESCKPVQQPSAFGSMK PC-9 GeftinibAZD4547-1to80 8.6743 down
P49841 GSK3B P Ser9 TTS(ph)FAESCKPVQQPSAFGSMK PC-9 Lapatinib 6.6407 down
P49841 GSK3B P Ser9 TTS(ph)FAESCKPVQQPSAFGSMK A459 MK2206 7.0039 -
P49841 GSK3B P Ser9 TTS(ph)FAESCKPVQQPSAFGSMK A459 Selumetinib 6.2144 -
P49841 GSK3B P Ser9 TTS(ph)FAESCKPVQQPSAFGSMK HeLa Curcumin 5.2589 -
P49841 GSK3B P Ser9 TTS(ph)FAESCKPVQQPSAFGSMK PC-9 AZD4547 5.5148 -
P49841 GSK3B P Ser9 TTS(ph)FAESCKPVQQPSAFGSMK PC-9 Gefitinib 8.2709 -

pEC50 Note: pEC50 is the negative logarithm of EC50 (half-maximal effective concentration, dosage unit Mol), calculated as pEC50 = -log10(EC50), which quantifies the potency of a drug or compound.

Function score:

source: funscoR

No data.

Cross Links: