Id: acc2053
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: Lung Cancer
Disease Subtype:
Disease Cellline: HCC2450
Disease Info:
Drug: AZD6244
Drug Info: AZD6244 (Selumetinib) is a selective MEK1/MEK2 inhibitor developed by AstraZeneca for the treatment of neurofibromatosis type 1-associated plexiform neurofibromas and certain advanced cancers such as non-small cell lung cancer.
Effect: inhibit
Effect Info: "AKT phosphorylation may lead to the resistance of lung cancer cells to AZD6244, which is not mediated by the activity of MEK/ERK itself."
Note:
Score: 5.0
Pubmed(PMID): 19783898
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
AKT1-Thr308
Cancer Intensity
BRCA
COAD
HGSC
ccRCC
GBM
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC

PTM-Disease Association:

source: PTMD
Residue 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: DecryptM

No data.

Function score:

source: funscoR

No data.

Cross Links: