Id: acc2435
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: Lung Cancer
Disease Subtype: NSCLC
Disease Cellline: A549
Disease Info:
Drug: TRAIL
Drug Info: "TRAIL (TNF-related apoptosis-inducing ligand), a member of the tumor necrosis factor (TNF) superfamily, selectively induces apoptosis in tumor cells while exhibiting minimal toxicity to normal cells, primarily through binding to death receptors DR4 and DR5."
Effect: inhibit
Effect Info: Telmisartan can sensitize TRAIL and enhance the death of NSCLC tumor cells by blocking AMPK phosphorylation.
Note:
Score: 5.0
Pubmed(PMID): 29929000
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: