Id: acc3296
Group: 1sens
Protein: AKT2
Gene Symbol: AKT2
Protein Id: P31751
Protein Name: AKT2_HUMAN
PTM: phosphorylation
Site: Ser474
Site Sequence: DQRTHFPQFSYSASIRE----
Disease Category: Endocrine and metabolic diseases
Disease: Obese
Disease Subtype:
Disease Cellline:
Disease Info:
Drug: Insulin
Drug Info: Insulin is a hormone that regulates blood sugar levels and is commonly used in the treatment of diabetes.
Relation:
Insulin
➜
AKT2-Ser474 DOWN
➜
Obese Aggravate
Effect: modulate
Effect Info: "Insulin can stimulate the phosphorylation of Akt–1 and Akt–2 in the absence of hyperglycemia. However, in the state of hyperglycemia, the expression and stimulatory ability of Akt–2 are impaired in obese patients. The decreased expression of Akt–2 is accompanied by a reduction in GLUT4 protein expression and an increase in the expression of insulin antagonistic enzymes."
Note:
Score: 4.0
Pubmed(PMID): 15010337
Sentence Index:
Sentence:

Sequence & Structure:

MNEVSVIKEGWLHKRGEYIKTWRPRYFLLKSDGSFIGYKERPEAPDQTLPPLNNFSVAECQLMKTERPRPNTFVIRCLQWTTVIERTFHVDSPDEREEWMRAIQMVANSLKQRAPGEDPMDYKCGSPSDSSTTEEMEVAVSKARAKVTMNDFDYLKLLGKGTFGKVILVREKATGRYYAMKILRKEVIIAKDEVAHTVTESRVLQNTRHPFLTALKYAFQTHDRLCFVMEYANGGELFFHLSRERVFTEERARFYGAEIVSALEYLHSRDVVYRDIKLENLMLDKDGHIKITDFGLCKEGISDGATMKTFCGTPEYLAPEVLEDNDYGRAVDWWGLGVVMYEMMCGRLPFYNQDHERLFELILMEEIRFPRTLSPEAKSLLAGLLKKDPKQRLGGGPSDAKEVMEHRFFLSINWQDVVQKKLLPPFKPQVTSEVDTRYFDDEFTAQSITITPPDRYDSLGLLELDQRTHFPQFSYSASIRE

Select PDB:

Known Drugs:

source: Multi-Sources

(see table)

Target Drug name MOA Phase Status Disease Source
AKT2 IPATASERTIB Serine/threonine-protein kinase AKT inhibitor 3 Completed metastatic prostate cancer ClinicalTrials
AKT2 CAPIVASERTIB Serine/threonine-protein kinase AKT inhibitor 3 Active, not recruiting breast neoplasm ClinicalTrials
AKT2 IPATASERTIB Serine/threonine-protein kinase AKT inhibitor 3 Completed triple-negative breast cancer ClinicalTrials
AKT2 IPATASERTIB Serine/threonine-protein kinase AKT inhibitor 3 Recruiting cancer ClinicalTrials
AKT2 IPATASERTIB Serine/threonine-protein kinase AKT inhibitor 3 Active, not recruiting breast cancer ClinicalTrials
AKT2 AFURESERTIB Serine/threonine-protein kinase AKT inhibitor 3 Recruiting breast cancer ClinicalTrials
AKT2 CAPIVASERTIB Serine/threonine-protein kinase AKT inhibitor 3 Active, not recruiting breast cancer ClinicalTrials
AKT2 IPATASERTIB Serine/threonine-protein kinase AKT inhibitor 3 Completed breast cancer ClinicalTrials
AKT2 IPATASERTIB Serine/threonine-protein kinase AKT inhibitor 3 Terminated breast cancer ClinicalTrials
AKT2 CAPIVASERTIB Serine/threonine-protein kinase AKT inhibitor 3 Recruiting breast cancer ClinicalTrials
AKT2 CAPIVASERTIB Serine/threonine-protein kinase AKT inhibitor 3 Active, not recruiting prostate cancer ClinicalTrials
AKT2 CAPIVASERTIB Serine/threonine-protein kinase AKT inhibitor 3 Recruiting prostate cancer ClinicalTrials
AKT2 CAPIVASERTIB Serine/threonine-protein kinase AKT inhibitor 2 Active, not recruiting neoplasm of mature B-cells ClinicalTrials
AKT2 MK-2206 Serine/threonine-protein kinase AKT inhibitor 2 Completed head and neck squamous cell carcinoma ClinicalTrials
AKT2 MK-2206 Serine/threonine-protein kinase AKT inhibitor 2 Completed hepatocellular carcinoma ClinicalTrials
AKT2 UPROSERTIB Serine/threonine-protein kinase AKT inhibitor 2 Terminated acute myeloid leukemia ClinicalTrials
AKT2 CAPIVASERTIB Serine/threonine-protein kinase AKT inhibitor 2 Active, not recruiting adenocarcinoma ClinicalTrials
AKT2 MK-2206 Serine/threonine-protein kinase AKT inhibitor 2 Completed adenosquamous lung carcinoma ClinicalTrials
AKT2 MK-2206 Serine/threonine-protein kinase AKT inhibitor 2 Completed breast carcinoma ClinicalTrials
AKT2 MK-2206 Serine/threonine-protein kinase AKT inhibitor 2 Terminated breast carcinoma ClinicalTrials
AKT2 MK-2206 Serine/threonine-protein kinase AKT inhibitor 2 Completed bronchoalveolar adenocarcinoma ClinicalTrials
AKT2 UPROSERTIB Serine/threonine-protein kinase AKT inhibitor 2 Completed breast carcinoma ClinicalTrials
AKT2 MK-2206 Serine/threonine-protein kinase AKT inhibitor 2 Completed diffuse large B-cell lymphoma ClinicalTrials
AKT2 MK-2206 Serine/threonine-protein kinase AKT inhibitor 2 Terminated diffuse large B-cell lymphoma ClinicalTrials
AKT2 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
AKT2-Ser474
Cancer Intensity
BRCA 1.332
COAD
HGSC -0.527
ccRCC -0.286
GBM -1.647
HNSC -0.277
LUAD 0.915
LUSC 0.49
non_ccRCC
PDAC
UCEC

PTM-Disease Association:

source: PTMD
Residue Position State Disease Class PMID
S 474 U Ovarian cancer/carcinoma Phosphorylation 14597629
S 474 U Breast cancer Phosphorylation 11507039
S 474 U Ovarian cancer Phosphorylation 10822383 ;  10822383

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: