Id: | acc1562 |
Group: | 2sens |
Protein: | AKT |
Gene Symbol: | AKT1 |
Protein Id: | P31749 |
Protein Name: | AKT1_HUMAN |
PTM: | phosphorylation |
Site: | Thr308 |
Site Sequence: | GIKDGATMKTFCGTPEYLAPE |
Disease Category: | Cancer |
Disease: | Merkel Cell Carcinoma |
Disease Subtype: | MCC |
Disease Cellline: | MGH-mcc1 |
Disease Info: | |
Drug: | ZST474 |
Drug Info: | - |
Effect: | modulate |
Effect Info: | Drugs reduce protein phosphorylation and inhibit tumors. |
Note: | |
Score: | 4.0 |
Pubmed(PMID): | 22261808 |
Sentence Index: | 22261808_9-10 |
Sentence: | "We observed that signaling through the PI3K/pAKT pathway was active in one MCPyV-positive and in all MCPyV-negative MCC cell lines, as evidenced by AKT phosphorylation. Importantly, the presence of a PIK3CA-activating mutation was associated with sensitivity to treatment with ZST474, a specific phosphoinositide 3-kinase (PI3K) inhibitor, and to NVP-BEZ235, a dual PI3K/mTOR inhibitor, targeted agents under active clinical development." |
Sequence & Structure:
MSDVAIVKEGWLHKRGEYIKTWRPRYFLLKNDGTFIGYKERPQDVDQREAPLNNFSVAQCQLMKTERPRPNTFIIRCLQWTTVIERTFHVETPEEREEWTTAIQTVADGLKKQEEEEMDFRSGSPSDNSGAEEMEVSLAKPKHRVTMNEFEYLKLLGKGTFGKVILVKEKATGRYYAMKILKKEVIVAKDEVAHTLTENRVLQNSRHPFLTALKYSFQTHDRLCFVMEYANGGELFFHLSRERVFSEDRARFYGAEIVSALDYLHSEKNVVYRDLKLENLMLDKDGHIKITDFGLCKEGIKDGATMKTFCGTPEYLAPEVLEDNDYGRAVDWWGLGVVMYEMMCGRLPFYNQDHEKLFELILMEEIRFPRTLGPEAKSLLSGLLKKDPKQRLGGGSEDAKEIMQHRFFAGIVWQHVYEKKLSPPFKPQVTSETDTRYFDEEFTAQMITITPPDQDDSMECVDSERRPHFPQFSYSASGTA
Select PDB:
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 TargetsPTM Intensity:
source: CPTACAKT1-Thr308 | |
---|---|
Cancer | Intensity |
BRCA | |
COAD | |
HGSC | |
ccRCC | |
GBM | |
HNSC | |
LUAD | |
LUSC | |
non_ccRCC | |
PDAC | |
UCEC |
PTM-Disease Association:
source: PTMDResidue | Position | State | Disease | Class | PMID |
---|---|---|---|---|---|
T | 308 | D | Ovarian cancer/carcinoma | Phosphorylation | 20153512 |
T | 308 | D | Type 2 diabetes | Phosphorylation | 15919790 ;  15919790 |
T | 308 | D | Head and neck squamous cell carcinoma | Phosphorylation | 21281788 |
T | 308 | D | Diabetes mellitus | Phosphorylation | 17272402 ;  20938636 ;  15919790 |
T | 308 | P | Non-small cell lung cancer/carcinoma | Phosphorylation | 23091605 |
T | 308 | U | Chronic lymphocytic leukemia | Phosphorylation | 16940331 |
T | 308 | U | Melanoma | Phosphorylation | 19996208 |
T | 308 | U | Multiple myeloma | Phosphorylation | 37781194 |
T | 308 | U | Neuroblastoma | Phosphorylation | 17234785 |
T | 308 | U | Pancreatic cancer/carcinoma/adenocarcinoma | Phosphorylation | 26676747 |
T | 308 | U | Rhabdomyosarcoma | Phosphorylation | 17848913 |
T | 308 | U | Breast cancer | Phosphorylation | 33571243 |
T | 308 | U | Acute myeloid leukemia/acute myelogenous leukemia | Phosphorylation | 12750723 |
T | 308 | U | Cholangiocarcinoma | Phosphorylation | 37752233 |
T | 308 | U | Lymphocytic leukemia | Phosphorylation | 20576813 |
T | 308 | U | Obesity | Phosphorylation | 35413055 |
T | 308 | U | Sjogren's syndrome | Phosphorylation | 34948236 |
T | 308 | U | Endometrial cancer | Phosphorylation | 35253622 |
T | 308 | U | Esophageal squamous cell carcinoma | Phosphorylation | 36995521 |
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: DecryptMNo data.
Function score:
source: funscoRNo data.