Details of the Target

General Information of Target

Target ID LDTP00264
Target Name cGMP-dependent 3',5'-cyclic phosphodiesterase (PDE2A)
Gene Name PDE2A
Gene ID 5138
Synonyms
cGMP-dependent 3',5'-cyclic phosphodiesterase; EC 3.1.4.17; Cyclic GMP-stimulated phosphodiesterase; CGS-PDE; cGSPDE
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MGQACGHSILCRSQQYPAARPAEPRGQQVFLKPDEPPPPPQPCADSLQDALLSLGSVIDI
SGLQRAVKEALSAVLPRVETVYTYLLDGESQLVCEDPPHELPQEGKVREAIISQKRLGCN
GLGFSDLPGKPLARLVAPLAPDTQVLVMPLADKEAGAVAAVILVHCGQLSDNEEWSLQAV
EKHTLVALRRVQVLQQRGPREAPRAVQNPPEGTAEDQKGGAAYTDRDRKILQLCGELYDL
DASSLQLKVLQYLQQETRASRCCLLLVSEDNLQLSCKVIGDKVLGEEVSFPLTGCLGQVV
EDKKSIQLKDLTSEDVQQLQSMLGCELQAMLCVPVISRATDQVVALACAFNKLEGDLFTD
EDEHVIQHCFHYTSTVLTSTLAFQKEQKLKCECQALLQVAKNLFTHLDDVSVLLQEIITE
ARNLSNAEICSVFLLDQNELVAKVFDGGVVDDESYEIRIPADQGIAGHVATTGQILNIPD
AYAHPLFYRGVDDSTGFRTRNILCFPIKNENQEVIGVAELVNKINGPWFSKFDEDLATAF
SIYCGISIAHSLLYKKVNEAQYRSHLANEMMMYHMKVSDDEYTKLLHDGIQPVAAIDSNF
ASFTYTPRSLPEDDTSMAILSMLQDMNFINNYKIDCPTLARFCLMVKKGYRDPPYHNWMH
AFSVSHFCYLLYKNLELTNYLEDIEIFALFISCMCHDLDHRGTNNSFQVASKSVLAALYS
SEGSVMERHHFAQAIAILNTHGCNIFDHFSRKDYQRMLDLMRDIILATDLAHHLRIFKDL
QKMAEVGYDRNNKQHHRLLLCLLMTSCDLSDQTKGWKTTRKIAELIYKEFFSQGDLEKAM
GNRPMEMMDREKAYIPELQISFMEHIAMPIYKLLQDLFPKAAELYERVASNREHWTKVSH
KFTIRGLPSNNSLDFLDEEYEVPDLDGTRAPINGCCSLDAE
Target Type
Clinical trial
Target Bioclass
Enzyme
Family
Cyclic nucleotide phosphodiesterase family, PDE2 subfamily
Subcellular location
Cytoplasm; Mitochondrion; Mitochondrion matrix; Cell membrane
Function
cGMP-activated cyclic nucleotide phosphodiesterase with a dual-specificity for the second messengers cAMP and cGMP, which are key regulators of many important physiological processes. Has a higher efficiency with cGMP compared to cAMP. Plays a role in cell growth and migration.; [Isoform PDE2A2]: Regulates mitochondrial cAMP levels and respiration. Involved in the regulation of mitochondria morphology/dynamics and apoptotic cell death via local modulation of cAMP/PKA signaling in the mitochondrion, including the monitoring of local cAMP levels at the outer mitochondrial membrane and of PKA-dependent phosphorylation of DNM1L.
TTD ID
T77400
Uniprot ID
O00408
DrugMap ID
TTJGW1Z
Ensemble ID
ENST00000334456.10
HGNC ID
HGNC:8777
ChEMBL ID
CHEMBL2652

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
A375 SNV: p.M626I .
CAL27 SNV: p.R204G .
CHL1 SNV: p.D408N .
COLO320 SNV: p.A595G .
DU145 SNV: p.T340N .
G361 SNV: p.G927S .
HCT15 SNV: p.V93M .
LS123 SNV: p.Q875P .
MCC13 SNV: p.S313F .
NB1 SNV: p.C119Ter .
NCIH358 SNV: p.L413M .
PF382 SNV: p.L231I .
REH SNV: p.K385R .
SUPT1 SNV: p.A823V .
TE4 SNV: p.Q103E; p.R887S .

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  		C504(2.91)  LDD3342  [1]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0308  AC46 PaTu 8988t C391(0.92); C393(0.92)  LDD1187  [2]
 LDCM0309  AC47 PaTu 8988t C391(0.87); C393(0.87)  LDD1188  [2]
 LDCM0310  AC48 PaTu 8988t C391(0.79); C393(0.79)  LDD1189  [2]
 LDCM0311  AC49 PaTu 8988t C391(0.76); C393(0.76)  LDD1190  [2]
 LDCM0313  AC50 PaTu 8988t C391(0.79); C393(0.79)  LDD1192  [2]
 LDCM0314  AC51 PaTu 8988t C391(0.20); C393(0.20)  LDD1193  [2]
 LDCM0315  AC52 PaTu 8988t C391(0.82); C393(0.82)  LDD1194  [2]
 LDCM0316  AC53 PaTu 8988t C391(0.82); C393(0.82)  LDD1195  [2]
 LDCM0317  AC54 PaTu 8988t C391(0.81); C393(0.81)  LDD1196  [2]
 LDCM0318  AC55 PaTu 8988t C391(0.66); C393(0.66)  LDD1197  [2]
 LDCM0319  AC56 PaTu 8988t C391(0.72); C393(0.72)  LDD1198  [2]
 LDCM0392  CL121 PaTu 8988t C391(0.92); C393(0.92)  LDD1271  [2]
 LDCM0393  CL122 PaTu 8988t C391(0.84); C393(0.84)  LDD1272  [2]
 LDCM0394  CL123 PaTu 8988t C391(0.82); C393(0.82)  LDD1273  [2]
 LDCM0395  CL124 PaTu 8988t C391(0.86); C393(0.86)  LDD1274  [2]
 LDCM0436  CL46 PaTu 8988t C391(0.96); C393(0.96)  LDD1315  [2]
 LDCM0437  CL47 PaTu 8988t C391(0.85); C393(0.85)  LDD1316  [2]
 LDCM0438  CL48 PaTu 8988t C391(0.88); C393(0.88)  LDD1317  [2]
 LDCM0439  CL49 PaTu 8988t C391(0.94); C393(0.94)  LDD1318  [2]
 LDCM0441  CL50 PaTu 8988t C391(0.87); C393(0.87)  LDD1320  [2]
 LDCM0442  CL51 PaTu 8988t C391(0.95); C393(0.95)  LDD1321  [2]
 LDCM0443  CL52 PaTu 8988t C391(0.95); C393(0.95)  LDD1322  [2]
 LDCM0444  CL53 PaTu 8988t C391(0.92); C393(0.92)  LDD1323  [2]
 LDCM0445  CL54 PaTu 8988t C391(0.81); C393(0.81)  LDD1324  [2]
 LDCM0446  CL55 PaTu 8988t C391(0.76); C393(0.76)  LDD1325  [2]
 LDCM0447  CL56 PaTu 8988t C391(0.46); C393(0.46)  LDD1326  [2]
 LDCM0448  CL57 PaTu 8988t C391(1.12); C393(1.12)  LDD1327  [2]
 LDCM0449  CL58 PaTu 8988t C391(0.84); C393(0.84)  LDD1328  [2]
 LDCM0450  CL59 PaTu 8988t C391(1.13); C393(1.13)  LDD1329  [2]
 LDCM0452  CL60 PaTu 8988t C391(0.84); C393(0.84)  LDD1331  [2]
 LDCM0453  CL61 PaTu 8988t C391(0.97); C393(0.97)  LDD1332  [2]
 LDCM0454  CL62 PaTu 8988t C391(0.72); C393(0.72)  LDD1333  [2]
 LDCM0455  CL63 PaTu 8988t C391(0.77); C393(0.77)  LDD1334  [2]
 LDCM0456  CL64 PaTu 8988t C391(0.85); C393(0.85)  LDD1335  [2]
 LDCM0457  CL65 PaTu 8988t C391(0.83); C393(0.83)  LDD1336  [2]
 LDCM0458  CL66 PaTu 8988t C391(0.86); C393(0.86)  LDD1337  [2]
 LDCM0459  CL67 PaTu 8988t C391(0.86); C393(0.86)  LDD1338  [2]
 LDCM0460  CL68 PaTu 8988t C391(0.80); C393(0.80)  LDD1339  [2]
 LDCM0461  CL69 PaTu 8988t C391(0.99); C393(0.99)  LDD1340  [2]
 LDCM0463  CL70 PaTu 8988t C391(0.93); C393(0.93)  LDD1342  [2]
 LDCM0464  CL71 PaTu 8988t C391(0.73); C393(0.73)  LDD1343  [2]
 LDCM0465  CL72 PaTu 8988t C391(0.89); C393(0.89)  LDD1344  [2]
 LDCM0466  CL73 PaTu 8988t C391(0.75); C393(0.75)  LDD1345  [2]
 LDCM0467  CL74 PaTu 8988t C391(0.95); C393(0.95)  LDD1346  [2]
 LDCM0469  CL76 PaTu 8988t C391(0.97); C393(0.97)  LDD1348  [2]
 LDCM0470  CL77 PaTu 8988t C391(0.98); C393(0.98)  LDD1349  [2]
 LDCM0471  CL78 PaTu 8988t C391(1.07); C393(1.07)  LDD1350  [2]
 LDCM0472  CL79 PaTu 8988t C391(1.13); C393(1.13)  LDD1351  [2]
 LDCM0474  CL80 PaTu 8988t C391(0.96); C393(0.96)  LDD1353  [2]
 LDCM0475  CL81 PaTu 8988t C391(1.03); C393(1.03)  LDD1354  [2]
 LDCM0476  CL82 PaTu 8988t C391(0.99); C393(0.99)  LDD1355  [2]
 LDCM0477  CL83 PaTu 8988t C391(1.10); C393(1.10)  LDD1356  [2]
 LDCM0478  CL84 PaTu 8988t C391(1.07); C393(1.07)  LDD1357  [2]
 LDCM0479  CL85 PaTu 8988t C391(0.94); C393(0.94)  LDD1358  [2]
 LDCM0480  CL86 PaTu 8988t C391(0.98); C393(0.98)  LDD1359  [2]
 LDCM0481  CL87 PaTu 8988t C391(1.02); C393(1.02)  LDD1360  [2]
 LDCM0482  CL88 PaTu 8988t C391(1.01); C393(1.01)  LDD1361  [2]
 LDCM0483  CL89 PaTu 8988t C391(1.05); C393(1.05)  LDD1362  [2]
 LDCM0485  CL90 PaTu 8988t C391(1.21); C393(1.21)  LDD1364  [2]
 LDCM0468  Fragment33 PaTu 8988t C391(0.91); C393(0.91)  LDD1347  [2]
 LDCM0022  KB02 8305C C504(1.49)  LDD2248  [1]
 LDCM0023  KB03 8305C C504(2.51)  LDD2665  [1]
 LDCM0024  KB05 NCI-H1155 C504(2.91)  LDD3342  [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
2 Reimagining high-throughput profiling of reactive cysteines for cell-based screening of large electrophile libraries. Nat Biotechnol. 2021 May;39(5):630-641. doi: 10.1038/s41587-020-00778-3. Epub 2021 Jan 4.