General Information of Target

Target ID LDTP13229
Target Name 5'-AMP-activated protein kinase subunit gamma-2 (PRKAG2)
Gene Name PRKAG2
Gene ID 51422
Synonyms
5'-AMP-activated protein kinase subunit gamma-2; AMPK gamma2; AMPK subunit gamma-2; H91620p
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MEPGLEHALRRTPSWSSLGGSEHQEMSFLEQENSSSWPSPAVTSSSERIRGKRRAKALRW
TRQKSVEEGEPPGQGEGPRSRPAAESTGLEATFPKTTPLAQADPAGVGTPPTGWDCLPSD
CTASAAGSSTDDVELATEFPATEAWECELEGLLEERPALCLSPQAPFPKLGWDDELRKPG
AQIYMRFMQEHTCYDAMATSSKLVIFDTMLEIKKAFFALVANGVRAAPLWDSKKQSFVGM
LTITDFILVLHRYYRSPLVQIYEIEQHKIETWREIYLQGCFKPLVSISPNDSLFEAVYTL
IKNRIHRLPVLDPVSGNVLHILTHKRLLKFLHIFGSLLPRPSFLYRTIQDLGIGTFRDLA
VVLETAPILTALDIFVDRRVSALPVVNECGQVVGLYSRFDVIHLAAQQTYNHLDMSVGEA
LRQRTLCLEGVLSCQPHESLGEVIDRIAREQVHRLVLVDETQHLLGVVSLSDILQALVLS
PAGIDALGA
Target Bioclass
Enzyme
Family
5'-AMP-activated protein kinase gamma subunit family
Function
AMP/ATP-binding subunit of AMP-activated protein kinase (AMPK), an energy sensor protein kinase that plays a key role in regulating cellular energy metabolism. In response to reduction of intracellular ATP levels, AMPK activates energy-producing pathways and inhibits energy-consuming processes: inhibits protein, carbohydrate and lipid biosynthesis, as well as cell growth and proliferation. AMPK acts via direct phosphorylation of metabolic enzymes, and by longer-term effects via phosphorylation of transcription regulators. Also acts as a regulator of cellular polarity by remodeling the actin cytoskeleton; probably by indirectly activating myosin. Gamma non-catalytic subunit mediates binding to AMP, ADP and ATP, leading to activate or inhibit AMPK: AMP-binding results in allosteric activation of alpha catalytic subunit (PRKAA1 or PRKAA2) both by inducing phosphorylation and preventing dephosphorylation of catalytic subunits. ADP also stimulates phosphorylation, without stimulating already phosphorylated catalytic subunit. ATP promotes dephosphorylation of catalytic subunit, rendering the AMPK enzyme inactive.
Uniprot ID
Q9UGJ0
Ensemble ID
ENST00000287878.9
HGNC ID
HGNC:9386
ChEMBL ID
CHEMBL2453

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
A673 SNV: p.S226C .
AN3CA SNV: p.R148G .
HCT15 SNV: p.F293L .
KMS12BM SNV: p.R302Q .
KYSE410 SNV: p.M242I .
L428 SNV: p.V14I .
MDAMB436 SNV: p.L428R .
MOLT4 SNV: p.P416S .
NALM6 SNV: p.S124N .
RKO SNV: p.Y353H .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info 
C29(2.54)  LDD3310  [1]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 A-172 C29(2.44)  LDD2251  [1]
 LDCM0023  KB03 A-172 C29(3.87)  LDD2668  [1]
 LDCM0024  KB05 COLO792 C29(2.54)  LDD3310  [1]

References

1 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840