Details of the Target

General Information of Target

Target ID LDTP13799
Target Name RAC-gamma serine/threonine-protein kinase (AKT3)
Gene Name AKT3
Gene ID 10000
Synonyms
PKBG; RAC-gamma serine/threonine-protein kinase; EC 2.7.11.1; Protein kinase Akt-3; Protein kinase B gamma; PKB gamma; RAC-PK-gamma; STK-2
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MLPCFQLLRIGGGRGGDLYTFHPPAGAGCTYRLGHRADLCDVALRPQQEPGLISGIHAEL
HAEPRGDDWRVSLEDHSSQGTLVNNVRLPRGHRLELSDGDLLTFGPEGPPGTSPSEFYFM
FQQVRVKPQDFAAITIPRSRGEARVGAGFRPMLPSQGAPQRPLSTFSPAPKATLILNSIG
SLSKLRPQPLTFSPSWGGPKSLPVPAPPGEMGTTPSAPPQRNRRKSVHRVLAELDDESEP
PENPPPVLMEPRKKLRVDKAPLTPTGNRRGRPRKYPVSAPMAPPAVGGGEPCAAPCCCLP
QEETVAWVQCDGCDVWFHVACVGCSIQAAREADFRCPGCRAGIQT
Target Type
Successful
Target Bioclass
Enzyme
Family
Protein kinase superfamily, AGC Ser/Thr protein kinase family, RAC subfamily
Subcellular location
Nucleus
Function
AKT3 is one of 3 closely related serine/threonine-protein kinases (AKT1, AKT2 and AKT3) called the AKT kinase, and which regulate many processes including metabolism, proliferation, cell survival, growth and angiogenesis. This is mediated through serine and/or threonine phosphorylation of a range of downstream substrates. Over 100 substrate candidates have been reported so far, but for most of them, no isoform specificity has been reported. AKT3 is the least studied AKT isoform. It plays an important role in brain development and is crucial for the viability of malignant glioma cells. AKT3 isoform may also be the key molecule in up-regulation and down-regulation of MMP13 via IL13. Required for the coordination of mitochondrial biogenesis with growth factor-induced increases in cellular energy demands. Down-regulation by RNA interference reduces the expression of the phosphorylated form of BAD, resulting in the induction of caspase-dependent apoptosis.
TTD ID
T71266
Uniprot ID
Q9Y243
DrugMap ID
TTAZ05C
Ensemble ID
ENST00000263826.12
HGNC ID
HGNC:393
ChEMBL ID
CHEMBL4816

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
COLO320 SNV: p.D32N .
ICC9 SNV: p.G265E .
IM95 SNV: p.T298A .
K562 SNV: p.G37Ter .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 14 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
TH211
 Probe Info  		Y323(20.00)  LDD0257  [1]
STPyne
 Probe Info  		K161(1.89)  LDD2217  [2]
IPM
 Probe Info  		N.A.  LDD0241  [3]
m-APA
 Probe Info  		11.80  LDD0403  [4]
AHL-Pu-1
 Probe Info  		C307(2.20)  LDD0168  [5]
IA-alkyne
 Probe Info  		C119(2.16)  LDD0372  [5]
EA-probe
 Probe Info  		N.A.  LDD0440  [6]
HHS-482
 Probe Info  		Y261(0.96); Y323(0.90)  LDD0285  [7]
HHS-475
 Probe Info  		Y323(0.83); Y261(0.96)  LDD0264  [8]
HHS-465
 Probe Info  		Y261(10.00); Y323(10.00)  LDD2237  [9]
DBIA
 Probe Info  		C459(1.06)  LDD1175  [10]
NAIA_4
 Probe Info  		C76(0.00); C293(0.00); C307(0.00)  LDD2226  [11]
Acrolein
 Probe Info  		C307(0.00); C293(0.00)  LDD0217  [12]
AOyne
 Probe Info  		15.00  LDD0443  [13]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0025  4SU-RNA HEK-293T C307(2.20)  LDD0168  [5]
 LDCM0026  4SU-RNA+native RNA HEK-293T C307(2.35); C119(3.23)  LDD0169  [5]
 LDCM0215  AC10 HEK-293T C119(1.05)  LDD1508  [14]
 LDCM0226  AC11 HEK-293T C119(0.87)  LDD1509  [14]
 LDCM0237  AC12 HEK-293T C119(1.06)  LDD1510  [14]
 LDCM0259  AC14 HEK-293T C119(1.11)  LDD1512  [14]
 LDCM0270  AC15 HEK-293T C119(0.89)  LDD1513  [14]
 LDCM0277  AC18 HEK-293T C119(1.03)  LDD1516  [14]
 LDCM0278  AC19 HEK-293T C119(1.03)  LDD1517  [14]
 LDCM0279  AC2 HEK-293T C119(1.08)  LDD1518  [14]
 LDCM0280  AC20 HEK-293T C119(0.96)  LDD1519  [14]
 LDCM0282  AC22 HEK-293T C119(1.00)  LDD1521  [14]
 LDCM0283  AC23 HEK-293T C119(0.88)  LDD1522  [14]
 LDCM0284  AC24 HEK-293T C119(1.08)  LDD1523  [14]
 LDCM0286  AC26 HEK-293T C119(1.05)  LDD1525  [14]
 LDCM0287  AC27 HEK-293T C119(0.92)  LDD1526  [14]
 LDCM0288  AC28 HEK-293T C119(0.92)  LDD1527  [14]
 LDCM0290  AC3 HEK-293T C119(1.01)  LDD1529  [14]
 LDCM0291  AC30 HEK-293T C119(0.98)  LDD1530  [14]
 LDCM0292  AC31 HEK-293T C119(0.86)  LDD1531  [14]
 LDCM0293  AC32 HEK-293T C119(1.07)  LDD1532  [14]
 LDCM0295  AC34 HEK-293T C119(1.10)  LDD1534  [14]
 LDCM0296  AC35 PaTu 8988t C459(1.06)  LDD1175  [10]
 LDCM0297  AC36 PaTu 8988t C459(1.28)  LDD1176  [10]
 LDCM0298  AC37 PaTu 8988t C459(1.35)  LDD1177  [10]
 LDCM0299  AC38 PaTu 8988t C459(1.36)  LDD1178  [10]
 LDCM0300  AC39 PaTu 8988t C459(1.46)  LDD1179  [10]
 LDCM0301  AC4 HEK-293T C119(1.08)  LDD1540  [14]
 LDCM0302  AC40 PaTu 8988t C459(1.65)  LDD1181  [10]
 LDCM0303  AC41 PaTu 8988t C459(1.27)  LDD1182  [10]
 LDCM0304  AC42 PaTu 8988t C459(1.54)  LDD1183  [10]
 LDCM0305  AC43 PaTu 8988t C459(1.39)  LDD1184  [10]
 LDCM0306  AC44 PaTu 8988t C459(2.05)  LDD1185  [10]
 LDCM0307  AC45 PaTu 8988t C459(1.50)  LDD1186  [10]
 LDCM0308  AC46 HEK-293T C119(1.05)  LDD1547  [14]
 LDCM0309  AC47 HEK-293T C119(0.95)  LDD1548  [14]
 LDCM0310  AC48 HEK-293T C119(1.02)  LDD1549  [14]
 LDCM0313  AC50 HEK-293T C119(1.04)  LDD1552  [14]
 LDCM0314  AC51 HEK-293T C119(0.88)  LDD1553  [14]
 LDCM0315  AC52 HEK-293T C119(1.04)  LDD1554  [14]
 LDCM0317  AC54 HEK-293T C119(0.91)  LDD1556  [14]
 LDCM0318  AC55 HEK-293T C119(0.86)  LDD1557  [14]
 LDCM0319  AC56 HEK-293T C119(0.92)  LDD1558  [14]
 LDCM0321  AC58 HEK-293T C119(0.94)  LDD1560  [14]
 LDCM0322  AC59 HEK-293T C119(0.84)  LDD1561  [14]
 LDCM0323  AC6 HEK-293T C119(1.03)  LDD1562  [14]
 LDCM0324  AC60 HEK-293T C119(1.07)  LDD1563  [14]
 LDCM0326  AC62 HEK-293T C119(0.83)  LDD1565  [14]
 LDCM0327  AC63 HEK-293T C119(0.88)  LDD1566  [14]
 LDCM0328  AC64 HEK-293T C119(0.88)  LDD1567  [14]
 LDCM0334  AC7 HEK-293T C119(0.98)  LDD1568  [14]
 LDCM0345  AC8 HEK-293T C119(1.00)  LDD1569  [14]
 LDCM0275  AKOS034007705 HEK-293T C119(0.95)  LDD1514  [14]
 LDCM0156  Aniline NCI-H1299 11.80  LDD0403  [4]
 LDCM0108  Chloroacetamide HeLa C307(0.00); C293(0.00)  LDD0222  [12]
 LDCM0367  CL1 HEK-293T C119(0.98)  LDD1571  [14]
 LDCM0368  CL10 HEK-293T C119(1.06)  LDD1572  [14]
 LDCM0369  CL100 HEK-293T C119(0.98)  LDD1573  [14]
 LDCM0370  CL101 HEK-293T C119(1.07)  LDD1574  [14]
 LDCM0371  CL102 HEK-293T C119(0.94)  LDD1575  [14]
 LDCM0372  CL103 HEK-293T C119(0.93)  LDD1576  [14]
 LDCM0373  CL104 HEK-293T C119(1.01)  LDD1577  [14]
 LDCM0374  CL105 HEK-293T C119(0.93)  LDD1578  [14]
 LDCM0375  CL106 HEK-293T C119(0.92)  LDD1579  [14]
 LDCM0376  CL107 HEK-293T C119(0.96)  LDD1580  [14]
 LDCM0377  CL108 HEK-293T C119(0.92)  LDD1581  [14]
 LDCM0378  CL109 HEK-293T C119(1.06)  LDD1582  [14]
 LDCM0379  CL11 HEK-293T C119(0.90)  LDD1583  [14]
 LDCM0380  CL110 HEK-293T C119(0.85)  LDD1584  [14]
 LDCM0381  CL111 HEK-293T C119(0.99)  LDD1585  [14]
 LDCM0382  CL112 HEK-293T C119(1.11)  LDD1586  [14]
 LDCM0383  CL113 HEK-293T C119(1.08)  LDD1587  [14]
 LDCM0384  CL114 HEK-293T C119(0.95)  LDD1588  [14]
 LDCM0385  CL115 HEK-293T C119(1.00)  LDD1589  [14]
 LDCM0386  CL116 HEK-293T C119(0.95)  LDD1590  [14]
 LDCM0387  CL117 PaTu 8988t C459(1.25)  LDD1266  [10]
 LDCM0388  CL118 PaTu 8988t C459(1.69)  LDD1267  [10]
 LDCM0389  CL119 PaTu 8988t C459(1.34)  LDD1268  [10]
 LDCM0390  CL12 HEK-293T C119(1.10)  LDD1594  [14]
 LDCM0391  CL120 PaTu 8988t C459(1.26)  LDD1270  [10]
 LDCM0392  CL121 HEK-293T C119(0.91)  LDD1596  [14]
 LDCM0393  CL122 HEK-293T C119(0.84)  LDD1597  [14]
 LDCM0394  CL123 HEK-293T C119(0.85)  LDD1598  [14]
 LDCM0395  CL124 HEK-293T C119(0.82)  LDD1599  [14]
 LDCM0396  CL125 HEK-293T C119(0.84)  LDD1600  [14]
 LDCM0397  CL126 HEK-293T C119(0.77)  LDD1601  [14]
 LDCM0398  CL127 HEK-293T C119(0.95)  LDD1602  [14]
 LDCM0399  CL128 HEK-293T C119(1.09)  LDD1603  [14]
 LDCM0400  CL13 HEK-293T C119(0.98)  LDD1604  [14]
 LDCM0401  CL14 HEK-293T C119(0.93)  LDD1605  [14]
 LDCM0402  CL15 HEK-293T C119(0.90)  LDD1606  [14]
 LDCM0403  CL16 PaTu 8988t C459(1.12)  LDD1282  [10]
 LDCM0404  CL17 PaTu 8988t C459(1.14)  LDD1283  [10]
 LDCM0405  CL18 PaTu 8988t C459(1.29)  LDD1284  [10]
 LDCM0406  CL19 PaTu 8988t C459(1.17)  LDD1285  [10]
 LDCM0407  CL2 HEK-293T C119(0.97)  LDD1611  [14]
 LDCM0408  CL20 PaTu 8988t C459(0.98)  LDD1287  [10]
 LDCM0409  CL21 PaTu 8988t C459(1.21)  LDD1288  [10]
 LDCM0410  CL22 PaTu 8988t C459(1.47)  LDD1289  [10]
 LDCM0411  CL23 PaTu 8988t C459(1.23)  LDD1290  [10]
 LDCM0412  CL24 PaTu 8988t C459(1.21)  LDD1291  [10]
 LDCM0413  CL25 PaTu 8988t C459(1.19)  LDD1292  [10]
 LDCM0414  CL26 PaTu 8988t C459(1.25)  LDD1293  [10]
 LDCM0415  CL27 PaTu 8988t C459(2.26)  LDD1294  [10]
 LDCM0416  CL28 PaTu 8988t C459(1.53)  LDD1295  [10]
 LDCM0417  CL29 PaTu 8988t C459(1.11)  LDD1296  [10]
 LDCM0418  CL3 HEK-293T C119(0.94)  LDD1622  [14]
 LDCM0419  CL30 PaTu 8988t C459(1.42)  LDD1298  [10]
 LDCM0420  CL31 PaTu 8988t C459(1.15)  LDD1299  [10]
 LDCM0421  CL32 PaTu 8988t C459(1.27)  LDD1300  [10]
 LDCM0422  CL33 PaTu 8988t C459(1.18)  LDD1301  [10]
 LDCM0423  CL34 PaTu 8988t C459(1.38)  LDD1302  [10]
 LDCM0424  CL35 PaTu 8988t C459(1.57)  LDD1303  [10]
 LDCM0425  CL36 PaTu 8988t C459(1.12)  LDD1304  [10]
 LDCM0426  CL37 PaTu 8988t C459(1.54)  LDD1305  [10]
 LDCM0428  CL39 PaTu 8988t C459(1.39)  LDD1307  [10]
 LDCM0429  CL4 HEK-293T C119(0.94)  LDD1633  [14]
 LDCM0430  CL40 PaTu 8988t C459(1.15)  LDD1309  [10]
 LDCM0431  CL41 PaTu 8988t C459(1.36)  LDD1310  [10]
 LDCM0432  CL42 PaTu 8988t C459(1.54)  LDD1311  [10]
 LDCM0433  CL43 PaTu 8988t C459(2.21)  LDD1312  [10]
 LDCM0434  CL44 PaTu 8988t C459(1.69)  LDD1313  [10]
 LDCM0435  CL45 PaTu 8988t C459(1.54)  LDD1314  [10]
 LDCM0436  CL46 PaTu 8988t C459(0.91)  LDD1315  [10]
 LDCM0437  CL47 PaTu 8988t C459(0.84)  LDD1316  [10]
 LDCM0438  CL48 PaTu 8988t C459(0.76)  LDD1317  [10]
 LDCM0439  CL49 PaTu 8988t C459(1.07)  LDD1318  [10]
 LDCM0441  CL50 PaTu 8988t C459(1.24)  LDD1320  [10]
 LDCM0442  CL51 PaTu 8988t C459(0.80)  LDD1321  [10]
 LDCM0443  CL52 PaTu 8988t C459(0.91)  LDD1322  [10]
 LDCM0444  CL53 PaTu 8988t C459(0.94)  LDD1323  [10]
 LDCM0445  CL54 PaTu 8988t C459(0.95)  LDD1324  [10]
 LDCM0446  CL55 PaTu 8988t C459(0.95)  LDD1325  [10]
 LDCM0447  CL56 PaTu 8988t C459(0.94)  LDD1326  [10]
 LDCM0448  CL57 PaTu 8988t C459(0.98)  LDD1327  [10]
 LDCM0449  CL58 PaTu 8988t C459(0.70)  LDD1328  [10]
 LDCM0450  CL59 PaTu 8988t C459(0.79)  LDD1329  [10]
 LDCM0451  CL6 HEK-293T C119(0.98)  LDD1654  [14]
 LDCM0452  CL60 PaTu 8988t C459(1.18)  LDD1331  [10]
 LDCM0453  CL61 HEK-293T C119(0.87)  LDD1656  [14]
 LDCM0454  CL62 HEK-293T C119(0.92)  LDD1657  [14]
 LDCM0455  CL63 HEK-293T C119(0.83)  LDD1658  [14]
 LDCM0456  CL64 HEK-293T C119(1.01)  LDD1659  [14]
 LDCM0458  CL66 HEK-293T C119(1.04)  LDD1661  [14]
 LDCM0459  CL67 HEK-293T C119(1.05)  LDD1662  [14]
 LDCM0460  CL68 HEK-293T C119(1.02)  LDD1663  [14]
 LDCM0462  CL7 HEK-293T C119(1.07)  LDD1665  [14]
 LDCM0463  CL70 HEK-293T C119(1.11)  LDD1666  [14]
 LDCM0464  CL71 HEK-293T C119(0.90)  LDD1667  [14]
 LDCM0465  CL72 HEK-293T C119(1.10)  LDD1668  [14]
 LDCM0466  CL73 HEK-293T C119(0.92)  LDD1669  [14]
 LDCM0467  CL74 HEK-293T C119(0.93)  LDD1670  [14]
 LDCM0469  CL76 PaTu 8988t C459(1.16)  LDD1348  [10]
 LDCM0470  CL77 PaTu 8988t C459(1.13)  LDD1349  [10]
 LDCM0471  CL78 PaTu 8988t C459(1.29)  LDD1350  [10]
 LDCM0472  CL79 PaTu 8988t C459(1.39)  LDD1351  [10]
 LDCM0473  CL8 HEK-293T C119(0.79)  LDD1676  [14]
 LDCM0474  CL80 PaTu 8988t C459(1.33)  LDD1353  [10]
 LDCM0475  CL81 PaTu 8988t C459(1.29)  LDD1354  [10]
 LDCM0476  CL82 PaTu 8988t C459(1.18)  LDD1355  [10]
 LDCM0477  CL83 PaTu 8988t C459(1.10)  LDD1356  [10]
 LDCM0478  CL84 PaTu 8988t C459(1.55)  LDD1357  [10]
 LDCM0479  CL85 PaTu 8988t C459(1.09)  LDD1358  [10]
 LDCM0480  CL86 PaTu 8988t C459(1.43)  LDD1359  [10]
 LDCM0481  CL87 PaTu 8988t C459(1.66)  LDD1360  [10]
 LDCM0482  CL88 PaTu 8988t C459(1.31)  LDD1361  [10]
 LDCM0483  CL89 PaTu 8988t C459(1.89)  LDD1362  [10]
 LDCM0485  CL90 PaTu 8988t C459(1.24)  LDD1364  [10]
 LDCM0486  CL91 HEK-293T C119(1.07)  LDD1689  [14]
 LDCM0487  CL92 HEK-293T C119(0.86)  LDD1690  [14]
 LDCM0489  CL94 HEK-293T C119(1.03)  LDD1692  [14]
 LDCM0490  CL95 HEK-293T C119(0.99)  LDD1693  [14]
 LDCM0491  CL96 HEK-293T C119(0.85)  LDD1694  [14]
 LDCM0492  CL97 HEK-293T C119(0.92)  LDD1695  [14]
 LDCM0493  CL98 HEK-293T C119(0.88)  LDD1696  [14]
 LDCM0494  CL99 HEK-293T C119(0.91)  LDD1697  [14]
 LDCM0495  E2913 HEK-293T C119(1.07)  LDD1698  [14]
 LDCM0175  Ethacrynic acid HeLa N.A.  LDD0440  [6]
 LDCM0468  Fragment33 HEK-293T C119(0.82)  LDD1671  [14]
 LDCM0427  Fragment51 PaTu 8988t C459(1.55)  LDD1306  [10]
 LDCM0116  HHS-0101 DM93 Y323(0.83); Y261(0.96)  LDD0264  [8]
 LDCM0117  HHS-0201 DM93 Y323(0.84); Y261(1.06)  LDD0265  [8]
 LDCM0118  HHS-0301 DM93 Y323(0.60); Y261(0.98)  LDD0266  [8]
 LDCM0119  HHS-0401 DM93 Y323(0.85); Y261(0.97)  LDD0267  [8]
 LDCM0120  HHS-0701 DM93 Y323(0.99); Y261(1.28)  LDD0268  [8]
 LDCM0123  JWB131 DM93 Y261(0.96); Y323(0.90)  LDD0285  [7]
 LDCM0124  JWB142 DM93 Y261(0.77); Y323(0.51)  LDD0286  [7]
 LDCM0125  JWB146 DM93 Y261(1.79); Y323(0.85)  LDD0287  [7]
 LDCM0126  JWB150 DM93 Y261(2.99); Y323(4.76)  LDD0288  [7]
 LDCM0127  JWB152 DM93 Y261(1.95); Y323(1.31)  LDD0289  [7]
 LDCM0128  JWB198 DM93 Y261(1.08); Y323(0.70)  LDD0290  [7]
 LDCM0129  JWB202 DM93 Y261(0.30); Y323(0.32)  LDD0291  [7]
 LDCM0130  JWB211 DM93 Y261(0.92); Y323(0.75)  LDD0292  [7]
 LDCM0022  KB02 HEK-293T C459(1.05); C119(0.95)  LDD1492  [14]
 LDCM0023  KB03 HEK-293T C459(1.14); C119(0.84)  LDD1497  [14]
 LDCM0024  KB05 HEK-293T C459(1.05); C119(1.01)  LDD1502  [14]
 LDCM0627  NUDT7-COV-1 HEK-293T C293(1.39); C76(1.33); C307(0.46)  LDD2206  [15]
 LDCM0628  OTUB2-COV-1 HEK-293T C307(1.02); C293(0.33)  LDD2207  [15]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Caspase-3 (CASP3) Peptidase C14A family P42574
E3 ubiquitin-protein ligase TTC3 (TTC3) . P53804
Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Hsp90 co-chaperone Cdc37 (CDC37) CDC37 family Q16543

The Drug(s) Related To This Target

Investigative
Click To Hide/Show 19 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Isis 29112 Antisense drug D03EYM
Isis 29135 Antisense drug D04YQN
Isis 29136 Antisense drug D02UHI
Isis 29137 Antisense drug D0M2JX
Isis 29138 Antisense drug D0O7OI
Isis 29139 Antisense drug D0Q0FZ
Isis 29154 Antisense drug D0W4XP
Isis 29155 Antisense drug D0N7AF
Isis 29156 Antisense drug D0U1QU
Isis 29159 Antisense drug D07CCC
Isis 29160 Antisense drug D06AOQ
Isis 29161 Antisense drug D04IBO
Isis 29176 Antisense drug D06AZX
Isis 29177 Antisense drug D05BFX
Isis 29178 Antisense drug D0N9AT
Isis 29200 Antisense drug D04QYU
Isis 29201 Antisense drug D0AH5P
Isis 29202 Antisense drug D00NPN
Sb-747651a Small molecular drug D0I1FJ

References

1 Chemoproteomic profiling of kinases in live cells using electrophilic sulfonyl triazole probes. Chem Sci. 2021 Jan 21;12(9):3295-3307. doi: 10.1039/d0sc06623k.
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Mass spectrometry data entry: PXD044625
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Mass spectrometry data entry: PXD041264
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Mass spectrometry data entry: PXD044402
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