Details of the Target

General Information of Target

Target ID LDTP05797
Target Name cGMP-dependent protein kinase 2 (PRKG2)
Gene Name PRKG2
Gene ID 5593
Synonyms
PRKGR2; cGMP-dependent protein kinase 2; cGK 2; cGK2; EC 2.7.11.12; cGMP-dependent protein kinase II; cGKII
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MGNGSVKPKHSKHPDGHSGNLTTDALRNKVTELERELRRKDAEIQEREYHLKELREQLSK
QTVAIAELTEELQNKCIQLNKLQDVVHMQGGSPLQASPDKVPLEVHRKTSGLVSLHSRRG
AKAGVSAEPTTRTYDLNKPPEFSFEKARVRKDSSEKKLITDALNKNQFLKRLDPQQIKDM
VECMYGRNYQQGSYIIKQGEPGNHIFVLAEGRLEVFQGEKLLSSIPMWTTFGELAILYNC
TRTASVKAITNVKTWALDREVFQNIMRRTAQARDEQYRNFLRSVSLLKNLPEDKLTKIID
CLEVEYYDKGDYIIREGEEGSTFFILAKGKVKVTQSTEGHDQPQLIKTLQKGEYFGEKAL
ISDDVRSANIIAEENDVACLVIDRETFNQTVGTFEELQKYLEGYVANLNRDDEKRHAKRS
MSNWKLSKALSLEMIQLKEKVARFSSSSPFQNLEIIATLGVGGFGRVELVKVKNENVAFA
MKCIRKKHIVDTKQQEHVYSEKRILEELCSPFIVKLYRTFKDNKYVYMLLEACLGGELWS
ILRDRGSFDEPTSKFCVACVTEAFDYLHRLGIIYRDLKPENLILDAEGYLKLVDFGFAKK
IGSGQKTWTFCGTPEYVAPEVILNKGHDFSVDFWSLGILVYELLTGNPPFSGVDQMMTYN
LILKGIEKMDFPRKITRRPEDLIRRLCRQNPTERLGNLKNGINDIKKHRWLNGFNWEGLK
ARSLPSPLQRELKGPIDHSYFDKYPPEKGMPPDELSGWDKDF
Target Type
Literature-reported
Target Bioclass
Enzyme
Family
Protein kinase superfamily, AGC Ser/Thr protein kinase family, cGMP subfamily
Subcellular location
Apical cell membrane
Function
Crucial regulator of intestinal secretion and bone growth. Phosphorylates and activates CFTR on the plasma membrane. Plays a key role in intestinal secretion by regulating cGMP-dependent translocation of CFTR in jejunum. Acts downstream of NMDAR to activate the plasma membrane accumulation of GRIA1/GLUR1 in synapse and increase synaptic plasticity. Phosphorylates GRIA1/GLUR1 at Ser-863. Acts as a regulator of gene expression and activator of the extracellular signal-regulated kinases MAPK3/ERK1 and MAPK1/ERK2 in mechanically stimulated osteoblasts. Under fluid shear stress, mediates ERK activation and subsequent induction of FOS, FOSL1/FRA1, FOSL2/FRA2 and FOSB that play a key role in the osteoblast anabolic response to mechanical stimulation.
TTD ID
T23606
Uniprot ID
Q13237
DrugMap ID
TTDWFCQ
Ensemble ID
ENST00000264399.6
HGNC ID
HGNC:9416
ChEMBL ID
CHEMBL2896

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
A172 SNV: p.L582Ter .
FUOV1 SNV: p.F741Y .
HCT15 SNV: p.L453I .
IPC298 SNV: p.R259Ter .
KU1919 Insertion: p.W634SfsTer10 .
LNCaP clone FGC Deletion: p.N474MfsTer8
SNV: p.T243I;p.V498A		 .
MCF7 SNV: p.R259Ter .
MDAMB468 SNV: p.H50N .
MEWO SNV: p.D681N .
MOLT4 SNV: p.L26M .
NCIH1793 SNV: p.R47L .
NCIH2172 SNV: p.G192R .
NCIH82 SNV: p.T519I .
OVCAR4 SNV: p.L534V .
SW620 SNV: p.G392S .
T98G SNV: p.K473Q .
VMRCRCW SNV: p.F280V .

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  		C240(1.04)  LDD1509  [1]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0226  AC11 HEK-293T C240(1.04)  LDD1509  [1]
 LDCM0278  AC19 HEK-293T C240(0.93)  LDD1517  [1]
 LDCM0287  AC27 HEK-293T C240(1.12)  LDD1526  [1]
 LDCM0290  AC3 HEK-293T C240(1.20)  LDD1529  [1]
 LDCM0296  AC35 HEK-293T C240(1.17)  LDD1535  [1]
 LDCM0305  AC43 HEK-293T C240(1.19)  LDD1544  [1]
 LDCM0314  AC51 HEK-293T C240(1.19)  LDD1553  [1]
 LDCM0322  AC59 HEK-293T C240(1.15)  LDD1561  [1]
 LDCM0369  CL100 HEK-293T C611(1.42)  LDD1573  [1]
 LDCM0373  CL104 HEK-293T C611(0.91)  LDD1577  [1]
 LDCM0377  CL108 HEK-293T C611(1.14)  LDD1581  [1]
 LDCM0382  CL112 HEK-293T C611(1.37)  LDD1586  [1]
 LDCM0386  CL116 HEK-293T C611(1.07)  LDD1590  [1]
 LDCM0391  CL120 HEK-293T C611(1.20)  LDD1595  [1]
 LDCM0395  CL124 HEK-293T C611(1.08)  LDD1599  [1]
 LDCM0399  CL128 HEK-293T C611(1.34)  LDD1603  [1]
 LDCM0403  CL16 HEK-293T C611(1.28)  LDD1607  [1]
 LDCM0406  CL19 HEK-293T C240(1.25)  LDD1610  [1]
 LDCM0416  CL28 HEK-293T C611(1.00)  LDD1620  [1]
 LDCM0420  CL31 HEK-293T C240(1.08)  LDD1624  [1]
 LDCM0429  CL4 HEK-293T C611(1.49)  LDD1633  [1]
 LDCM0430  CL40 HEK-293T C611(0.97)  LDD1634  [1]
 LDCM0433  CL43 HEK-293T C240(1.33)  LDD1637  [1]
 LDCM0443  CL52 HEK-293T C611(1.17)  LDD1646  [1]
 LDCM0446  CL55 HEK-293T C240(1.50)  LDD1649  [1]
 LDCM0456  CL64 HEK-293T C611(1.13)  LDD1659  [1]
 LDCM0459  CL67 HEK-293T C240(1.34)  LDD1662  [1]
 LDCM0462  CL7 HEK-293T C240(1.09)  LDD1665  [1]
 LDCM0469  CL76 HEK-293T C611(1.43)  LDD1672  [1]
 LDCM0472  CL79 HEK-293T C240(1.11)  LDD1675  [1]
 LDCM0482  CL88 HEK-293T C611(1.13)  LDD1685  [1]
 LDCM0486  CL91 HEK-293T C240(1.20)  LDD1689  [1]

References

1 Accelerating multiplexed profiling of protein-ligand interactions: High-throughput plate-based reactive cysteine profiling with minimal input. Cell Chem Biol. 2024 Mar 21;31(3):565-576.e4. doi: 10.1016/j.chembiol.2023.11.015. Epub 2023 Dec 19.
Mass spectrometry data entry: PXD044402