| Id: | acc2434 |
| 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: | 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: | 29929000_5-6 |
| Sentence: | "Herein, we demonstrated that telmisartan could sensitize TRAIL and enhance NSCLC tumor cell death. The molecular mechanism includes the blocking of AMPK phosphorylation causes inhibition of autophagy flux by telmisartan resulting in ROS generation leading to death receptor (DR5) upregulation and subsequent activation of the caspase cascade by TRAIL treatment." |
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: CPTAC| PRKAA2-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.
