Id: acc2213
Group: 2sens
Protein: PRAS40
Gene Symbol: AKT1S1
Protein Id: Q96B36
Protein Name: AKTS1_HUMAN
PTM: phosphorylation
Site: Thr246
Site Sequence: GDLPRPRLNTSDFQKLKRKY-
Disease Category: Cancer
Disease: Prostate Cancer
Disease Subtype:
Disease Cellline: LNCaP
Disease Info:
Drug: AZD5363
Drug Info: "Capivasertib (AZD5363) is an orally active pan-AKT kinase inhibitor that inhibits Akt1, Akt2, and Akt3 with IC50 values of 3, 7, and 7 nM, respectively."
Effect: modulate
Effect Info: AZD5363 can effectively reduce the growth of multiple tumor models. AZD5363 effectively inhibits the phosphorylation of S6 and 4E - BP1 in these cell lines and simultaneously increases the phosphorylation of AKT at the ser473 and thr308 sites.
Note:
Score: 4.0
Pubmed(PMID): 22294718
Sentence Index:
Sentence:

Sequence & Structure:

MASGRPEELWEAVVGAAERFRARTGTELVLLTAAPPPPPRPGPCAYAAHGRGALAEAARRCLHDIALAHRAATAARPPAPPPAPQPPSPTPSPPRPTLAREDNEEDEDEPTETETSGEQLGISDNGGLFVMDEDATLQDLPPFCESDPESTDDGSLSEETPAGPPTCSVPPASALPTQQYAKSLPVSVPVWGFKEKRTEARSSDEENGPPSSPDLDRIAASMRALVLREAEDTQVFGDLPRPRLNTSDFQKLKRKY

Select PDB:

Known Drugs:

source: Multi-Sources

(see table)

No data.

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
AKT1S1-Thr246
Cancer Intensity
BRCA
COAD -0.468
HGSC 0.953
ccRCC
GBM -1.179
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC 0.694

PTM-Disease Association:

source: PTMD
Residue Position State Disease Class PMID
T 246 P Gastric cancer Phosphorylation 24701227
T 246 U Breast cancer Phosphorylation 36797347
T 246 U Cervical cancer/carcinoma Phosphorylation 16174443
T 246 U Sjogren's syndrome Phosphorylation 34948236
T 246 U Liver cancer Phosphorylation 35058442

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
Protein Gene PTM Position Modified sequence Cell Drug pEC50 Regulation Experiment
Q96B36 AKT1S1 P Thr246 LNT(ph)SDFQK A549 AZD8055 7.7295 down
Q96B36 AKT1S1 P Thr246 LNT(ph)SDFQK A549 Dactolisib 7.8299 down
Q96B36 AKT1S1 P Thr246 LNT(ph)SDFQK A549 Nintedanib 5.3092 down
Q96B36 AKT1S1 P Thr246 LNT(ph)SDFQK A549 Pictilisib 7.08 down
Q96B36 AKT1S1 P Thr246 LNT(ph)SDFQK A431 Dasatinib 6.2964 down
Q96B36 AKT1S1 P Thr246 LNT(ph)SDFQK SK-BR-3 Lapatinib 7.9773 down
Q96B36 AKT1S1 P Thr246 LNT(ph)SDFQK MDA-MB-175 Lapatinib 6.7493 down
Q96B36 AKT1S1 P Thr246 LNT(ph)SDFQK BT-474 Lapatinib 6.4247 down
Q96B36 AKT1S1 P Thr246 LNT(ph)SDFQK MDA-MB-175 Pertuzumab -4.554 down
Q96B36 AKT1S1 P Thr246 LNT(ph)SDFQK Ramos Rituximab -1.2537 -
Q96B36 AKT1S1 P Thr246 LNT(ph)SDFQK K562 Dasatinib 9.0864 -
Q96B36 AKT1S1 P Thr246 LNT(ph)SDFQK K562 Imatinib 7.5422 -
Q96B36 AKT1S1 P Thr246 LNT(ph)SDFQK KYSE-520 SHP099 6.7746 -
Q96B36 AKT1S1 P Thr246 LNT(ph)SDFQK MDA-MB-175 Trastuzumab -0.1496 -
Q96B36 AKT1S1 P Thr246 LNT(ph)SDFQK Ramos Rituximab -0.3957 -
Q96B36 AKT1S1 P Thr246 LNT(ph)SDFQK Ramos Rituximab -2.9741 -
Q96B36 AKT1S1 P Thr246 LNT(ph)SDFQK K562 Dasatinib 9.2526 -
Q96B36 AKT1S1 P Thr246 LNT(ph)SDFQK Ramos Rituximab -2.821 -
Q96B36 AKT1S1 P Thr246 LNT(ph)SDFQK SK-BR-3 Pertuzumab -2.9561 -
Q96B36 AKT1S1 P Thr246 LNT(ph)SDFQK SK-BR-3 Trastuzumab -2.2203 -
Q96B36 AKT1S1 P Thr246 LNT(ph)SDFQK SU-DHL-4 Rituximab -3.2261 -
Q96B36 AKT1S1 P Thr246 LNT(ph)SDFQK K562 Dasatinib 9.1109 -
Q96B36 AKT1S1 P Thr246 LNT(ph)SDFQK K562 Dasatinib 8.7719 -
Q96B36 AKT1S1 P Thr246 LNT(ph)SDFQK K562 Dasatinib 8.792 -
Q96B36 AKT1S1 P Thr246 LNT(ph)SDFQK K562 Dasatinib 12.9407 -
Q96B36 AKT1S1 P Thr246 LNT(ph)SDFQK HeLa SAHA 5.8683 -
Q96B36 AKT1S1 P Thr246 LNT(ph)SDFQK HeLa A486 5.2478 -
Q96B36 AKT1S1 P Thr246 LNT(ph)SDFQK HeLa A485 14 -
Q96B36 AKT1S1 P Thr246 LNT(ph)SDFQK BT-474 Trastuzumab -1.46 -
Q96B36 AKT1S1 P Thr246 LNT(ph)SDFQK BT-474 Pertuzumab -4.7058 -
Q96B36 AKT1S1 P Thr246 LNT(ph)SDFQK ARH-77 Rituximab -1.277 -
Q96B36 AKT1S1 P Thr246 LNT(ph)SDFQK ARH-77 Rituximab -1.235 -
Q96B36 AKT1S1 P Thr246 LNT(ph)SDFQK ARH-77 Rituximab -1.1261 -
Q96B36 AKT1S1 P Thr246 LNT(ph)SDFQK A549 Tideglusib 6.3981 -
Q96B36 AKT1S1 P Thr246 LNT(ph)SDFQK A549 Dasatinib 6.8808 -
Q96B36 AKT1S1 P Thr246 LNT(ph)SDFQK A431 Imatinib 16.5229 -

pEC50 Note: pEC50 is the negative logarithm of EC50 (half-maximal effective concentration, dosage unit Mol), calculated as pEC50 = -log10(EC50), which quantifies the potency of a drug or compound.

Function score:

source: funscoR

No data.

Cross Links: