Id: acc1360
Group: 2sens
Protein: AMPK
Gene Symbol: PRKAA1
Protein Id: Q13131
Protein Name: AAPK1_HUMAN
PTM: phosphorylation
Site: Thr183
Site Sequence: MMSDGEFLRTSCGSPNYAAPE
Disease Category: Cancer
Disease: Prostate Cancer
Disease Subtype: CRPC
Disease Cellline: C4-2
Disease Info:
Drug: salinomycin
Drug Info: "Salinomycin is a polyether ionophore antibiotic primarily used as an anticoccidial agent in poultry and as a growth promoter in livestock, with emerging research interest in its potential anticancer properties. "
Effect: modulate
Effect Info: "Salinomycin inhibits AR phosphorylation and promotes AMPK phosphorylation. The activation of AMPK leads to an increase in the phosphorylation of Raptor and TSC2 at Ser1387. Meanwhile, salinomycin also blocks the inhibitory phosphorylation of TSC2 (Ser939/Thr1462) by AKT, thus inhibiting both AR and mTORC1. "
Note:
Score: 4.0
Pubmed(PMID): 27557496
Sentence Index:
Sentence:

Sequence & Structure:

MRRLSSWRKMATAEKQKHDGRVKIGHYILGDTLGVGTFGKVKVGKHELTGHKVAVKILNRQKIRSLDVVGKIRREIQNLKLFRHPHIIKLYQVISTPSDIFMVMEYVSGGELFDYICKNGRLDEKESRRLFQQILSGVDYCHRHMVVHRDLKPENVLLDAHMNAKIADFGLSNMMSDGEFLRTSCGSPNYAAPEVISGRLYAGPEVDIWSSGVILYALLCGTLPFDDDHVPTLFKKICDGIFYTPQYLNPSVISLLKHMLQVDPMKRATIKDIREHEWFKQDLPKYLFPEDPSYSSTMIDDEALKEVCEKFECSEEEVLSCLYNRNHQDPLAVAYHLIIDNRRIMNEAKDFYLATSPPDSFLDDHHLTRPHPERVPFLVAETPRARHTLDELNPQKSKHQGVRKAKWHLGIRSQSRPNDIMAEVCRAIKQLDYEWKVVNPYYLRVRRKNPVTSTYSKMSLQLYQVDSRTYLLDFRSIDDEITEAKSGTATPQRSGSVSNYRSCQRSDSDAEAQGKSSEVSLTSSVTSLDSSPVDLTPRPGSHTIEFFEMCANLIKILAQ

Select PDB:

Known Drugs:

source: Multi-Sources

(see table)

Target Drug name MOA Phase Status Disease Source
PRKAA1 ACADESINE AMP-activated protein kinase, AMPK activator 3 - cardiovascular disease ATC
PRKAA1 ACADESINE AMP-activated protein kinase, AMPK activator 1 Completed chronic lymphocytic leukemia 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
PRKAA1-Thr183
Cancer Intensity
BRCA
COAD 0.707
HGSC -0.707
ccRCC
GBM
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC

PTM-Disease Association:

source: PTMD
Residue Position State Disease Class PMID
T 183 D Colon cancer/carcinoma Phosphorylation 25679763
T 183 U Breast cancer Phosphorylation 30413706

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: