Id: acc2575
Group: 1sens
Protein: Akt
Gene Symbol: AKT1
Protein Id: P31749
Protein Name: AKT1_HUMAN
PTM: phosphorylation
Site: Ser473
Site Sequence: ERRPHFPQFSYSASGTA----
Disease Category: Cancer
Disease: Gastric Cancer
Disease Subtype:
Disease Cellline: HGC-27
Disease Info:
Drug: N-acetylcysteine(NAC)
Drug Info: "N-Acetylcysteine (NAC) is a mucolytic agent and antioxidant that works by breaking down disulfide bonds in mucus proteins to reduce viscosity, and it is also used as an antidote for acetaminophen overdose by replenishing glutathione stores to prevent hepatotoxicity."
Effect: modulate
Effect Info: The drug inhibits the proliferation and migration of gastric cancer cells and simultaneously inhibits protein phosphorylation.
Note:
Score: 4.0
Pubmed(PMID): 32021099
Sentence Index:
Sentence:

Sequence & Structure:

MSDVAIVKEGWLHKRGEYIKTWRPRYFLLKNDGTFIGYKERPQDVDQREAPLNNFSVAQCQLMKTERPRPNTFIIRCLQWTTVIERTFHVETPEEREEWTTAIQTVADGLKKQEEEEMDFRSGSPSDNSGAEEMEVSLAKPKHRVTMNEFEYLKLLGKGTFGKVILVKEKATGRYYAMKILKKEVIVAKDEVAHTLTENRVLQNSRHPFLTALKYSFQTHDRLCFVMEYANGGELFFHLSRERVFSEDRARFYGAEIVSALDYLHSEKNVVYRDLKLENLMLDKDGHIKITDFGLCKEGIKDGATMKTFCGTPEYLAPEVLEDNDYGRAVDWWGLGVVMYEMMCGRLPFYNQDHEKLFELILMEEIRFPRTLGPEAKSLLSGLLKKDPKQRLGGGSEDAKEIMQHRFFAGIVWQHVYEKKLSPPFKPQVTSETDTRYFDEEFTAQMITITPPDQDDSMECVDSERRPHFPQFSYSASGTA

Select PDB:

Known Drugs:

source: Multi-Sources

(see table)

Target Drug name MOA Phase Status Disease Source
AKT1 IPATASERTIB Serine/threonine-protein kinase AKT inhibitor 3 Completed metastatic prostate cancer ClinicalTrials
AKT1 CAPIVASERTIB Serine/threonine-protein kinase AKT inhibitor 3 Active, not recruiting breast neoplasm ClinicalTrials
AKT1 IPATASERTIB Serine/threonine-protein kinase AKT inhibitor 3 Completed triple-negative breast cancer ClinicalTrials
AKT1 IPATASERTIB Serine/threonine-protein kinase AKT inhibitor 3 Recruiting cancer ClinicalTrials
AKT1 IPATASERTIB Serine/threonine-protein kinase AKT inhibitor 3 Active, not recruiting breast cancer ClinicalTrials
AKT1 IPATASERTIB Serine/threonine-protein kinase AKT inhibitor 3 Completed breast cancer ClinicalTrials
AKT1 IPATASERTIB Serine/threonine-protein kinase AKT inhibitor 3 Terminated breast cancer ClinicalTrials
AKT1 AFURESERTIB Serine/threonine-protein kinase AKT inhibitor 3 Recruiting breast cancer ClinicalTrials
AKT1 CAPIVASERTIB Serine/threonine-protein kinase AKT inhibitor 3 Active, not recruiting breast cancer ClinicalTrials
AKT1 CAPIVASERTIB Serine/threonine-protein kinase AKT inhibitor 3 Recruiting breast cancer ClinicalTrials
AKT1 CAPIVASERTIB Serine/threonine-protein kinase AKT inhibitor 3 Recruiting prostate cancer ClinicalTrials
AKT1 CAPIVASERTIB Serine/threonine-protein kinase AKT inhibitor 3 Active, not recruiting prostate cancer ClinicalTrials
AKT1 MK-2206 Serine/threonine-protein kinase AKT inhibitor 2 Completed hepatocellular carcinoma ClinicalTrials
AKT1 MK-2206 Serine/threonine-protein kinase AKT inhibitor 2 Completed head and neck squamous cell carcinoma ClinicalTrials
AKT1 CAPIVASERTIB Serine/threonine-protein kinase AKT inhibitor 2 Active, not recruiting neoplasm of mature B-cells ClinicalTrials
AKT1 UPROSERTIB Serine/threonine-protein kinase AKT inhibitor 2 Terminated acute myeloid leukemia ClinicalTrials
AKT1 CAPIVASERTIB Serine/threonine-protein kinase AKT inhibitor 2 Active, not recruiting adenocarcinoma ClinicalTrials
AKT1 MK-2206 Serine/threonine-protein kinase AKT inhibitor 2 Completed breast carcinoma ClinicalTrials
AKT1 MK-2206 Serine/threonine-protein kinase AKT inhibitor 2 Terminated breast carcinoma ClinicalTrials
AKT1 MK-2206 Serine/threonine-protein kinase AKT inhibitor 2 Completed adenosquamous lung carcinoma ClinicalTrials
AKT1 UPROSERTIB Serine/threonine-protein kinase AKT inhibitor 2 Completed breast carcinoma ClinicalTrials
AKT1 MK-2206 Serine/threonine-protein kinase AKT inhibitor 2 Completed bronchoalveolar adenocarcinoma ClinicalTrials
AKT1 MK-2206 Serine/threonine-protein kinase AKT inhibitor 2 Completed diffuse large B-cell lymphoma ClinicalTrials
AKT1 MK-2206 Serine/threonine-protein kinase AKT inhibitor 2 Terminated diffuse large B-cell lymphoma ClinicalTrials
AKT1 CAPIVASERTIB Serine/threonine-protein kinase AKT inhibitor 2 Terminated gastric adenocarcinoma 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!

AKT1-Ser124
Cancer Intensity
BRCA
COAD -0.707
HGSC 0.707
ccRCC
GBM
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC
AKT1-Ser126
Cancer Intensity
BRCA
COAD -0.707
HGSC 0.707
ccRCC
GBM
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC
AKT1-Ser129
Cancer Intensity
BRCA
COAD -0.707
HGSC 0.707
ccRCC
GBM
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC
AKT1-Thr448
Cancer Intensity
BRCA
COAD
HGSC -0.707
ccRCC
GBM
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC 0.707
AKT1-Thr450
Cancer Intensity
BRCA
COAD -0.936
HGSC -1.526
ccRCC 0.252
GBM 0.594
HNSC
LUAD 0.617
LUSC
non_ccRCC
PDAC
UCEC 0.999
AKT1-Tyr315
Cancer Intensity
BRCA 0.788
COAD
HGSC
ccRCC
GBM
HNSC
LUAD -1.125
LUSC 0.336
non_ccRCC
PDAC
UCEC
AKT1S1-Ser183
Cancer Intensity
BRCA 1.667
COAD 0.891
HGSC 0.725
ccRCC -1.189
GBM 0.792
HNSC 0.064
LUAD -0.194
LUSC -0.266
non_ccRCC -1.722
PDAC -0.879
UCEC 0.11
AKT1S1-Ser202
Cancer Intensity
BRCA -0.344
COAD -0.013
HGSC -2.725
ccRCC -0.093
GBM -0.249
HNSC 0.707
LUAD 0.324
LUSC 0.615
non_ccRCC 0.322
PDAC 0.379
UCEC 1.076
AKT1S1-Ser203
Cancer Intensity
BRCA -0.189
COAD 0.095
HGSC -2.902
ccRCC 0.277
GBM 0.142
HNSC 0.479
LUAD 0.265
LUSC 0.603
non_ccRCC 0.04
PDAC 0.419
UCEC 0.771
AKT1S1-Ser211
Cancer Intensity
BRCA -1.13
COAD 0.333
HGSC -2.178
ccRCC 0.627
GBM 0.09
HNSC 1.177
LUAD -0.47
LUSC 0.383
non_ccRCC
PDAC 0.715
UCEC 0.451
AKT1S1-Ser212
Cancer Intensity
BRCA -1.05
COAD 0.546
HGSC -2.08
ccRCC -0.197
GBM 0.641
HNSC 1.003
LUAD -0.628
LUSC 0.311
non_ccRCC
PDAC 0.36
UCEC 1.094
AKT1S1-Ser247
Cancer Intensity
BRCA
COAD -1.124
HGSC
ccRCC
GBM 0.791
HNSC 0.334
LUAD
LUSC
non_ccRCC
PDAC
UCEC
AKT1S1-Ser88
Cancer Intensity
BRCA -1.265
COAD -0.583
HGSC
ccRCC -0.267
GBM 0.344
HNSC 2.36
LUAD -0.052
LUSC 0.649
non_ccRCC -0.088
PDAC -0.187
UCEC -0.912
AKT1S1-Ser92
Cancer Intensity
BRCA -1.122
COAD -0.689
HGSC
ccRCC 0.068
GBM -0.037
HNSC 2.235
LUAD 0.28
LUSC 0.221
non_ccRCC -0.997
PDAC 0.777
UCEC -0.735
AKT1S1-Thr198
Cancer Intensity
BRCA
COAD
HGSC
ccRCC -0.647
GBM
HNSC
LUAD -0.505
LUSC
non_ccRCC
PDAC
UCEC 1.152
AKT1S1-Thr246
Cancer Intensity
BRCA
COAD -0.468
HGSC 0.953
ccRCC
GBM -1.179
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC 0.694
AKT1S1-Thr90
Cancer Intensity
BRCA
COAD 0.347
HGSC -1.784
ccRCC 0.431
GBM
HNSC 0.542
LUAD 0.465
LUSC
non_ccRCC
PDAC
UCEC
AKT1S1-Thr97
Cancer Intensity
BRCA 1.061
COAD -1.872
HGSC
ccRCC 0.814
GBM -0.592
HNSC 0.541
LUAD 0.201
LUSC
non_ccRCC
PDAC
UCEC -0.152

PTM-Disease Association:

source: PTMD
Residue Position State Disease Class PMID
S 473 D Oral squamous cell carcinoma Phosphorylation 31889370
S 473 D Triple-negative breast cancer Phosphorylation 34077419
S 473 D Bladder cancer Phosphorylation 23799035
S 473 D Pancreatic cancer Phosphorylation 28363942 ;  15467756
S 473 D Colon cancer Phosphorylation 35190555
S 473 D Head and neck squamous cell carcinoma Phosphorylation 21281788
S 473 P Acute myeloid leukemia/acute myelogenous leukemia Phosphorylation 18056483
S 473 P Gastric cancer Phosphorylation 23969493 ;  23440515
S 473 P Ovarian cancer/carcinoma Phosphorylation 23877012
S 473 P Breast cancer Phosphorylation 36632451
S 473 P Anaplastic astrocytoma Phosphorylation 23596468
S 473 P Esophageal squamous cell carcinoma Phosphorylation 23510069
S 473 P Non-small cell lung cancer/carcinoma Phosphorylation 23091605
S 473 P Prostate cancer/carcinoma/adenocarcinoma Phosphorylation 23732709
S 473 U Pancreatic cancer Phosphorylation 15467756 ;  28363942
S 473 U Uveal melanoma Phosphorylation 34918581
S 473 U Osteosarcoma Phosphorylation 34476004
S 473 U Cancer Phosphorylation 34767444
S 473 U Cervical cancer Phosphorylation 32047568
S 473 U Acute myeloid leukemia/acute myelogenous leukemia Phosphorylation 15289327
S 473 U Breast cancer Phosphorylation 17545609 ;  12244301 ;  12244301 ;  17545609 ;  21743495 ;  30413706
S 473 U Chronic lymphocytic leukemia Phosphorylation 16940331
S 473 U Esophageal squamous cell carcinoma Phosphorylation 31897228
S 473 U Gallbladder cancer Phosphorylation 33407730
S 473 U Hepatocellular carcinoma Phosphorylation 37573318 ;  36348350
S 473 U Multiple myeloma Phosphorylation 37781194
S 473 U Pancreatic cancer/carcinoma/adenocarcinoma Phosphorylation 15467756 ;  21474066 ;  28363942
S 473 U Rhabdomyosarcoma Phosphorylation 17848913
S 473 U Synovial sarcoma Phosphorylation 35556229
S 473 U HER2-positive breast cancer Phosphorylation 36314765
S 473 U Thymic carcinoma Phosphorylation 20597130
S 473 U Systemic lupus erythematosus Phosphorylation 23735868 ;  34522717 ;  23735868
S 473 U Squamous cell carcinoma Phosphorylation 21795477 ;  37109043
S 473 U Sjogren's syndrome Phosphorylation 34948236
S 473 U Breast cancer/tumor/carcinoma Phosphorylation 17545609 ;  12244301 ;  22476852
S 473 U Cancer Phosphorylation 21795477
S 473 U Cholangiocarcinoma Phosphorylation 37752233
S 473 U Colon cancer/carcinoma Phosphorylation 22975685
S 473 U Colorectal cancer Phosphorylation 37430297
S 473 U Diabetes mellitus Phosphorylation 35835217
S 473 U Glioma Phosphorylation 33820494
S 473 U Renal cancer/carcinoma Phosphorylation 19118035 ;  16247451 ;  12649200
S 473 U Kidney cancer Phosphorylation 12649200 ;  12649200 ;  22580611
S 473 U Liver cancer Phosphorylation 15684384
S 473 U Lymphocytic leukemia Phosphorylation 20576813
S 473 U Melanoma Phosphorylation 19996208 ;  12499277 ;  12499277 ;  19996208 ;  12499277
S 473 U Neuroblastoma Phosphorylation 17234785
S 473 U Non-small cell squamous cell lung carcinoma Phosphorylation 20008839
S 473 U Obesity Phosphorylation 35413055
S 473 U Ovarian cancer Phosphorylation 15208673
S 473 U Ovarian epithelial carcinoma Phosphorylation 32194423
S 473 U Urethral cancer Phosphorylation 22975685
S 473 U Parkinson's disease Phosphorylation 19800394 ;  19800394 ;  21658387

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: