Id: | acc1359 |
Group: | 2sens |
Protein: | AMPK |
Gene Symbol: | PRKAA2 |
Protein Id: | P54646 |
Protein Name: | AAPK2_HUMAN |
PTM: | phosphorylation |
Site: | Thr172 |
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: | 27557496_11-12 |
Sentence: | AMPK-mediated raptor phosphorylation further reduced mTOR's kinase function and mTORC1 activity. Our novel finding on dual inhibition of AR and mTORC1 suggests that salinomycin is potentially active as monotherapy against advanced prostate cancer. |
Sequence & Structure:
MAEKQKHDGRVKIGHYVLGDTLGVGTFGKVKIGEHQLTGHKVAVKILNRQKIRSLDVVGKIKREIQNLKLFRHPHIIKLYQVISTPTDFFMVMEYVSGGELFDYICKHGRVEEMEARRLFQQILSAVDYCHRHMVVHRDLKPENVLLDAHMNAKIADFGLSNMMSDGEFLRTSCGSPNYAAPEVISGRLYAGPEVDIWSCGVILYALLCGTLPFDDEHVPTLFKKIRGGVFYIPEYLNRSVATLLMHMLQVDPLKRATIKDIREHEWFKQDLPSYLFPEDPSYDANVIDDEAVKEVCEKFECTESEVMNSLYSGDPQDQLAVAYHLIIDNRRIMNQASEFYLASSPPSGSFMDDSAMHIPPGLKPHPERMPPLIADSPKARCPLDALNTTKPKSLAVKKAKWHLGIRSQSKPYDIMAEVYRAMKQLDFEWKVVNAYHLRVRRKNPVTGNYVKMSLQLYLVDNRSYLLDFKSIDDEVVEQRSGSSTPQRSCSAAGLHRPRSSFDSTTAESHSLSGSLTGSLTGSTLSSVSPRLGSHTMDFFEMCASLITTLAR
Select PDB:
Target | Drug name | MOA | Phase | Status | Disease | Source |
---|---|---|---|---|---|---|
PRKAA2 | ACADESINE | AMP-activated protein kinase, AMPK activator | 3 | - | cardiovascular disease | ATC |
PRKAA2 | 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 TargetsPTM Intensity:
source: CPTACPRKAA2-Thr172 | |
---|---|
Cancer | Intensity |
BRCA | |
COAD | 0.934 |
HGSC | -1.055 |
ccRCC | |
GBM | |
HNSC | |
LUAD | |
LUSC | |
non_ccRCC | 0.121 |
PDAC | |
UCEC |
PTM-Disease Association:
source: PTMDNo data.
PTM-Drug Perturbation Response:
source: DecryptMNo data.
Function score:
source: funscoRNo data.