Id: | acc0932 |
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: | Prostate Cancer |
Disease Subtype: | |
Disease Cellline: | PC3 |
Disease Info: | |
Drug: | delta-T |
Drug Info: | - |
Effect: | modulate |
Effect Info: | "Delta-T induces the phosphorylation of AKT at T308 through the activation of PIK3, thereby attenuating the EGF/IGF-induced AKT activation and subsequently inhibiting tumors." |
Note: | |
Score: | 4.0 |
Pubmed(PMID): | 26465359 |
Sentence Index: | 26465359_7-8 |
Sentence: | "Further study on the activation of AKT by EGFR and IGFR revealed that delta-T attenuated the EGF/IGF-induced activation of AKT (via the phosphorylation of AKT on T308 induced by the activation of PIK3). Expression of dominant active PIK3 and AKT in prostate cancer cell line DU145 in which PIK3, AKT, and PTEN are wild type caused the cells to be reflectory to the inhibition of delta-T, supporting that delta-T inhibits the PIK3-mediated activation of AKT." |
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.