PMADS

Id:	acc2179
Group:	2sens
Protein:	AMPKalpha1
Gene Symbol:	PRKAA1
Protein Id:	Q13131
Protein Name:	AAPK1_HUMAN
PTM:	phosphorylation
Site:	Thr467
Site Sequence:	MSLQLYQVDSRTYLLDFRSID
Disease Category:	Cancer
Disease:	Cervical Cancer
Disease Subtype:
Disease Cellline:	Ishikawa
Disease Info:
Drug:	SMI-4a + AICAR
Drug Info:	-
Effect:	modulate
Effect Info:	PIM2 binds to AMPKalpha1 and directly phosphorylates Thr467. The PIM2 inhibitor SMI - 4a and the AMPKalpha1 activator AICAR can effectively inhibit tumor growth.
Note:	drug comb
Score:	4.0
Pubmed(PMID):	31358902
Sentence Index:	31358902_4-5
Sentence:	"Specifically, we found that PIM2 bound to AMPKalpha1, and directly phosphorylated it on Thr467. Phosphorylation of AMPKalpha1 by PIM2 led to decreasing AMPKalpha1 kinase activity, which in turn promoted aerobic glycolysis and tumor growth."

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
S	467	P	Endometrial cancer	Phosphorylation	31358902

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