Id: acc0703
Group: 1sens
Protein: AKT
Gene Symbol: AKT1
Protein Id: P31749
Protein Name: AKT1_HUMAN
PTM: ubiquitination
Site: unclear
Site Sequence:
Disease Category: Cancer
Disease: Gastric Cancer
Disease Subtype:
Disease Cellline: MGC803
Disease Info:
Drug: Estradiol cypionate
Drug Info: "Estradiol cypionate is a synthetic, long-acting estrogen ester, specifically the 17beta-cyclopentylpropionate ester of estradiol, that acts via estrogen receptors to inhibit ET-1 synthesis and is primarily used for research purposes, not clinical applications."
Effect: modulate
Effect Info: Estradiol cypionate inhibits the proliferation and promotes the apoptosis of gastric cancer by increasing AKT ubiquitination.
Note:
Score: 4.0
Pubmed(PMID): 37392652
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 data.

PTM-Disease Association:

source: PTMD
Residue Position State Disease Class PMID
- - D Laryngeal cancer Phosphorylation 23886414
- - D Sepsis Acetylation 37211747
- - D Oral squamous cell carcinoma Phosphorylation 23723304
- - D Myelodysplasia Phosphorylation 12529294
- - D Glioma/adult gliomas Phosphorylation 12839945
- - P Cancer SUMOylation 23884910
- - P Acute monocytic leukemia Phosphorylation 24422998
S - P Colon cancer/carcinoma Phosphorylation 24464560
- - P Glioblastoma Phosphorylation 23262078
- - P Embryonal central nervous system tumor Phosphorylation 16230398
- - P Brain cancer Phosphorylation 12388552
- - U Endometrial cancer Phosphorylation 12888921
- - U Thyroid cancer Phosphorylation 12788904
- - U Cervical cancer/carcinoma Phosphorylation 10853013
- - U Prostate cancer/carcinoma/adenocarcinoma Phosphorylation 10853013
- - U Marek's disease Phosphorylation 35795905
- - U Prostate cancer/carcinoma/adenocarcinoma Phosphorylation 23785446
- - U Gastric cancer Phosphorylation 23898095
- - U Renal cell carcinoma Phosphorylation 34257606
- - U Hepatocellular carcinoma Acetylation 31842909
- - U Pancreatic cancer Phosphorylation 31765735
- - U Colorectal cancer Phosphorylation 35110545
- - U Gastric cancer Phosphorylation 36604355
- - U Urothelial bladder cancer Phosphorylation 35691981
- - U Epithelial ovarian cancer Phosphorylation 35105347
- - U Tongue cancer Phosphorylation 37132640
- - U Papillary thyroid cancer Acetylation 37696385

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: