PMADS

Id:	acc3074
Group:	2sens
Protein:	AMPK
Gene Symbol:	PRKAA1
Protein Id:	Q13131
Protein Name:	AAPK1_HUMAN
PTM:	phosphorylation
Site:	Thr172
Site Sequence:	NAKIADFGLSNMMSDGEFLRT
Disease Category:	Cancer
Disease:	Cancer
Disease Subtype:
Disease Cellline:	"MCF-7,T98G,U87MG,K-562,CEM T"
Disease Info:
Drug:	AICAR
Drug Info:	"AICAR is a drug that has been studied for its potential in various medical applications, including its effects on metabolism."
Effect:	modulate
Effect Info:	"AICAR activates AMPK, inhibits Akt phosphorylation, blocks the cell cycle, and inhibits the proliferation of tumor cells."
Note:
Score:	4.0
Pubmed(PMID):	16176927
Sentence Index:	16176927_4-5
Sentence:	"Anti-proliferative effect of AICAR is mediated through activated AMP-activated protein kinase (AMPK) as iodotubericidin and dominant-negative AMPK expression vector reversed the AICAR-mediated growth arrest. Moreover, constitutive active AMPK arrested the cells in S-phase by inducing the expression of p21, p27, and p53 proteins and inhibiting Akt phosphorylation, suggesting the involvement of AMPK."

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

No intensity data of this site,
show all other sites!

PRKAA1-Ser176
Cancer	Intensity
BRCA
COAD	0.707
HGSC	-0.707
ccRCC
GBM
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC

PRKAA1-Ser39
Cancer	Intensity
BRCA
COAD	0.642
HGSC
ccRCC	0.505
GBM
HNSC
LUAD	0.342
LUSC
non_ccRCC	-1.489
PDAC
UCEC

PRKAA1-Ser460
Cancer	Intensity
BRCA	-0.513
COAD
HGSC
ccRCC	-0.062
GBM
HNSC	-0.258
LUAD	-0.383
LUSC	-0.353
non_ccRCC	2.395
PDAC	-0.013
UCEC	-0.813

PRKAA1-Ser468
Cancer	Intensity
BRCA
COAD
HGSC
ccRCC	-0.048
GBM	1.318
HNSC	0.263
LUAD	-0.054
LUSC
non_ccRCC
PDAC
UCEC	-1.479

PRKAA1-Ser470
Cancer	Intensity
BRCA	-1.641
COAD
HGSC
ccRCC	-0.308
GBM	0.511
HNSC	-0.178
LUAD	0.348
LUSC	0.565
non_ccRCC	1.902
PDAC	-0.335
UCEC	-0.865

PRKAA1-Ser480
Cancer	Intensity
BRCA
COAD
HGSC
ccRCC	0.126
GBM
HNSC	1.104
LUAD	-0.663
LUSC	0.891
non_ccRCC
PDAC	0.127
UCEC	-1.586

PRKAA1-Ser482
Cancer	Intensity
BRCA	-0.341
COAD
HGSC
ccRCC	-0.727
GBM	-0.577
HNSC	0.18
LUAD	0.063
LUSC	-0.503
non_ccRCC	2.553
PDAC	-0.373
UCEC	-0.276

PRKAA1-Ser486
Cancer	Intensity
BRCA
COAD	0.707
HGSC	-0.707
ccRCC
GBM
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC

PRKAA1-Ser496
Cancer	Intensity
BRCA
COAD	-0.707
HGSC	0.707
ccRCC
GBM
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC

PRKAA1-Ser498
Cancer	Intensity
BRCA
COAD	-0.581
HGSC	1.155
ccRCC	-0.574
GBM
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC

PRKAA1-Ser508
Cancer	Intensity
BRCA
COAD	-0.707
HGSC	0.707
ccRCC
GBM
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC

PRKAA1-Thr183
Cancer	Intensity
BRCA
COAD	0.707
HGSC	-0.707
ccRCC
GBM
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC

PRKAA1-Thr356
Cancer	Intensity
BRCA
COAD
HGSC
ccRCC
GBM	-1.152
HNSC
LUAD
LUSC	0.647
non_ccRCC	0.505
PDAC
UCEC

PRKAA1-Thr362
Cancer	Intensity
BRCA
COAD
HGSC
ccRCC	-0.408
GBM
HNSC	0.145
LUAD	-1.522
LUSC	-0.112
non_ccRCC	0.409
PDAC	-0.307
UCEC	1.795

PRKAA1-Thr382
Cancer	Intensity
BRCA
COAD	0.707
HGSC	-0.707
ccRCC
GBM
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC

PRKAA1-Thr464
Cancer	Intensity
BRCA
COAD
HGSC
ccRCC
GBM
HNSC
LUAD
LUSC
non_ccRCC
PDAC	0.707
UCEC	-0.707

PRKAA1-Thr490
Cancer	Intensity
BRCA
COAD	0.707
HGSC	-0.707
ccRCC
GBM
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC

PRKAA1-Tyr500
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	172	P	Pancreatic cancer/carcinoma/adenocarcinoma	Phosphorylation	23663483
T	172	U	Ovarian epithelial carcinoma	Phosphorylation	26068970
T	172	U	Breast cancer/tumor/carcinoma	Phosphorylation	24403860 ; 23794518

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:

CTD
DMRdb