General Information of Target

Target ID LDTP03290
Target Name Protein kinase C eta type (PRKCH)
Gene Name PRKCH
Gene ID 5583
Synonyms
PKCL; PRKCL; Protein kinase C eta type; EC 2.7.11.13; PKC-L; nPKC-eta
3D Structure
Download
2D Sequence (FASTA)
Download
3D Structure (PDB)
Download
Sequence
MSSGTMKFNGYLRVRIGEAVGLQPTRWSLRHSLFKKGHQLLDPYLTVSVDQVRVGQTSTK
QKTNKPTYNEEFCANVTDGGHLELAVFHETPLGYDHFVANCTLQFQELLRTTGASDTFEG
WVDLEPEGKVFVVITLTGSFTEATLQRDRIFKHFTRKRQRAMRRRVHQINGHKFMATYLR
QPTYCSHCREFIWGVFGKQGYQCQVCTCVVHKRCHHLIVTACTCQNNINKVDSKIAEQRF
GINIPHKFSIHNYKVPTFCDHCGSLLWGIMRQGLQCKICKMNVHIRCQANVAPNCGVNAV
ELAKTLAGMGLQPGNISPTSKLVSRSTLRRQGKESSKEGNGIGVNSSNRLGIDNFEFIRV
LGKGSFGKVMLARVKETGDLYAVKVLKKDVILQDDDVECTMTEKRILSLARNHPFLTQLF
CCFQTPDRLFFVMEFVNGGDLMFHIQKSRRFDEARARFYAAEIISALMFLHDKGIIYRDL
KLDNVLLDHEGHCKLADFGMCKEGICNGVTTATFCGTPDYIAPEILQEMLYGPAVDWWAM
GVLLYEMLCGHAPFEAENEDDLFEAILNDEVVYPTWLHEDATGILKSFMTKNPTMRLGSL
TQGGEHAILRHPFFKEIDWAQLNHRQIEPPFRPRIKSREDVSNFDPDFIKEEPVLTPIDE
GHLPMINQDEFRNFSYVSPELQP
Target Type
Literature-reported
Target Bioclass
Enzyme
Family
Protein kinase superfamily, AGC Ser/Thr protein kinase family, PKC subfamily
Subcellular location
Cytoplasm
Function
Calcium-independent, phospholipid- and diacylglycerol (DAG)-dependent serine/threonine-protein kinase that is involved in the regulation of cell differentiation in keratinocytes and pre-B cell receptor, mediates regulation of epithelial tight junction integrity and foam cell formation, and is required for glioblastoma proliferation and apoptosis prevention in MCF-7 cells. In keratinocytes, binds and activates the tyrosine kinase FYN, which in turn blocks epidermal growth factor receptor (EGFR) signaling and leads to keratinocyte growth arrest and differentiation. Associates with the cyclin CCNE1-CDK2-CDKN1B complex and inhibits CDK2 kinase activity, leading to RB1 dephosphorylation and thereby G1 arrest in keratinocytes. In association with RALA activates actin depolymerization, which is necessary for keratinocyte differentiation. In the pre-B cell receptor signaling, functions downstream of BLNK by up-regulating IRF4, which in turn activates L chain gene rearrangement. Regulates epithelial tight junctions (TJs) by phosphorylating occludin (OCLN) on threonine residues, which is necessary for the assembly and maintenance of TJs. In association with PLD2 and via TLR4 signaling, is involved in lipopolysaccharide (LPS)-induced RGS2 down-regulation and foam cell formation. Upon PMA stimulation, mediates glioblastoma cell proliferation by activating the mTOR pathway, the PI3K/AKT pathway and the ERK1-dependent phosphorylation of ELK1. Involved in the protection of glioblastoma cells from irradiation-induced apoptosis by preventing caspase-9 activation. In camptothecin-treated MCF-7 cells, regulates NF-kappa-B upstream signaling by activating IKBKB, and confers protection against DNA damage-induced apoptosis. Promotes oncogenic functions of ATF2 in the nucleus while blocking its apoptotic function at mitochondria. Phosphorylates ATF2 which promotes its nuclear retention and transcriptional activity and negatively regulates its mitochondrial localization.
TTD ID
T40149
Uniprot ID
P24723
DrugMap ID
TTONI0R
Ensemble ID
ENST00000332981.11
HGNC ID
HGNC:9403
ChEMBL ID
CHEMBL3616

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
IGROV1 SNV: p.M442V .
IPC298 SNV: p.P612L .
JURKAT SNV: p.A221T .
LNCaP clone FGC SNV: p.R271Ter .
MFE319 SNV: p.Q418R .
MOLT4 SNV: p.G37D IA-alkyne    Probe Info 
TOV21G SNV: p.W121C .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 4 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
AHL-Pu-1
 Probe Info 
C399(2.14)  LDD0170  [1]
DBIA
 Probe Info 
C399(1.08)  LDD1492  [2]
IA-alkyne
 Probe Info 
C493(0.00); C276(0.00)  LDD0166  [3]
Lodoacetamide azide
 Probe Info 
C399(0.00); C493(0.00)  LDD0037  [4]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0025  4SU-RNA DM93 C399(2.14)  LDD0170  [1]
 LDCM0214  AC1 HEK-293T C399(1.24)  LDD1507  [2]
 LDCM0215  AC10 HEK-293T C399(1.28)  LDD1508  [2]
 LDCM0226  AC11 HEK-293T C399(1.08)  LDD1509  [2]
 LDCM0237  AC12 HEK-293T C399(1.04)  LDD1510  [2]
 LDCM0259  AC14 HEK-293T C399(1.30)  LDD1512  [2]
 LDCM0270  AC15 HEK-293T C399(1.13)  LDD1513  [2]
 LDCM0276  AC17 HEK-293T C399(1.25)  LDD1515  [2]
 LDCM0277  AC18 HEK-293T C399(0.97)  LDD1516  [2]
 LDCM0278  AC19 HEK-293T C399(0.96)  LDD1517  [2]
 LDCM0279  AC2 HEK-293T C399(1.29)  LDD1518  [2]
 LDCM0280  AC20 HEK-293T C399(1.27)  LDD1519  [2]
 LDCM0281  AC21 HEK-293T C399(1.07)  LDD1520  [2]
 LDCM0282  AC22 HEK-293T C399(1.24)  LDD1521  [2]
 LDCM0283  AC23 HEK-293T C399(1.14)  LDD1522  [2]
 LDCM0284  AC24 HEK-293T C399(1.04)  LDD1523  [2]
 LDCM0285  AC25 HEK-293T C399(1.24)  LDD1524  [2]
 LDCM0286  AC26 HEK-293T C399(1.35)  LDD1525  [2]
 LDCM0287  AC27 HEK-293T C399(1.22)  LDD1526  [2]
 LDCM0288  AC28 HEK-293T C399(1.06)  LDD1527  [2]
 LDCM0289  AC29 HEK-293T C399(1.25)  LDD1528  [2]
 LDCM0290  AC3 HEK-293T C399(1.13)  LDD1529  [2]
 LDCM0291  AC30 HEK-293T C399(1.15)  LDD1530  [2]
 LDCM0292  AC31 HEK-293T C399(1.07)  LDD1531  [2]
 LDCM0293  AC32 HEK-293T C399(1.01)  LDD1532  [2]
 LDCM0294  AC33 HEK-293T C399(1.21)  LDD1533  [2]
 LDCM0295  AC34 HEK-293T C399(1.30)  LDD1534  [2]
 LDCM0296  AC35 HEK-293T C399(1.36)  LDD1535  [2]
 LDCM0297  AC36 HEK-293T C399(1.17)  LDD1536  [2]
 LDCM0298  AC37 HEK-293T C399(1.03)  LDD1537  [2]
 LDCM0299  AC38 HEK-293T C399(1.14)  LDD1538  [2]
 LDCM0300  AC39 HEK-293T C399(1.22)  LDD1539  [2]
 LDCM0301  AC4 HEK-293T C399(1.03)  LDD1540  [2]
 LDCM0302  AC40 HEK-293T C399(0.99)  LDD1541  [2]
 LDCM0303  AC41 HEK-293T C399(1.12)  LDD1542  [2]
 LDCM0304  AC42 HEK-293T C399(1.31)  LDD1543  [2]
 LDCM0305  AC43 HEK-293T C399(1.09)  LDD1544  [2]
 LDCM0306  AC44 HEK-293T C399(1.02)  LDD1545  [2]
 LDCM0307  AC45 HEK-293T C399(1.14)  LDD1546  [2]
 LDCM0308  AC46 HEK-293T C399(1.02)  LDD1547  [2]
 LDCM0309  AC47 HEK-293T C399(1.07)  LDD1548  [2]
 LDCM0310  AC48 HEK-293T C399(0.84)  LDD1549  [2]
 LDCM0311  AC49 HEK-293T C399(1.12)  LDD1550  [2]
 LDCM0312  AC5 HEK-293T C399(1.12)  LDD1551  [2]
 LDCM0313  AC50 HEK-293T C399(1.21)  LDD1552  [2]
 LDCM0314  AC51 HEK-293T C399(1.24)  LDD1553  [2]
 LDCM0315  AC52 HEK-293T C399(1.03)  LDD1554  [2]
 LDCM0316  AC53 HEK-293T C399(1.02)  LDD1555  [2]
 LDCM0317  AC54 HEK-293T C399(1.01)  LDD1556  [2]
 LDCM0318  AC55 HEK-293T C399(1.16)  LDD1557  [2]
 LDCM0319  AC56 HEK-293T C399(1.00)  LDD1558  [2]
 LDCM0320  AC57 HEK-293T C399(1.15)  LDD1559  [2]
 LDCM0321  AC58 HEK-293T C399(1.04)  LDD1560  [2]
 LDCM0322  AC59 HEK-293T C399(1.06)  LDD1561  [2]
 LDCM0323  AC6 HEK-293T C399(1.11)  LDD1562  [2]
 LDCM0324  AC60 HEK-293T C399(1.03)  LDD1563  [2]
 LDCM0325  AC61 HEK-293T C399(0.98)  LDD1564  [2]
 LDCM0326  AC62 HEK-293T C399(1.01)  LDD1565  [2]
 LDCM0327  AC63 HEK-293T C399(1.08)  LDD1566  [2]
 LDCM0328  AC64 HEK-293T C399(0.91)  LDD1567  [2]
 LDCM0334  AC7 HEK-293T C399(1.05)  LDD1568  [2]
 LDCM0345  AC8 HEK-293T C399(0.97)  LDD1569  [2]
 LDCM0248  AKOS034007472 HEK-293T C399(0.99)  LDD1511  [2]
 LDCM0356  AKOS034007680 HEK-293T C399(1.14)  LDD1570  [2]
 LDCM0275  AKOS034007705 HEK-293T C399(0.97)  LDD1514  [2]
 LDCM0367  CL1 HEK-293T C399(1.42)  LDD1571  [2]
 LDCM0368  CL10 HEK-293T C399(3.03)  LDD1572  [2]
 LDCM0369  CL100 HEK-293T C399(1.23)  LDD1573  [2]
 LDCM0370  CL101 HEK-293T C399(1.15)  LDD1574  [2]
 LDCM0371  CL102 HEK-293T C399(1.21)  LDD1575  [2]
 LDCM0372  CL103 HEK-293T C399(1.44)  LDD1576  [2]
 LDCM0373  CL104 HEK-293T C399(1.14)  LDD1577  [2]
 LDCM0374  CL105 HEK-293T C399(1.27)  LDD1578  [2]
 LDCM0375  CL106 HEK-293T C399(1.08)  LDD1579  [2]
 LDCM0376  CL107 HEK-293T C399(1.20)  LDD1580  [2]
 LDCM0377  CL108 HEK-293T C399(1.45)  LDD1581  [2]
 LDCM0378  CL109 HEK-293T C399(1.12)  LDD1582  [2]
 LDCM0379  CL11 HEK-293T C399(1.58)  LDD1583  [2]
 LDCM0380  CL110 HEK-293T C399(1.21)  LDD1584  [2]
 LDCM0381  CL111 HEK-293T C399(1.21)  LDD1585  [2]
 LDCM0382  CL112 HEK-293T C399(1.40)  LDD1586  [2]
 LDCM0383  CL113 HEK-293T C399(1.09)  LDD1587  [2]
 LDCM0384  CL114 HEK-293T C399(1.02)  LDD1588  [2]
 LDCM0385  CL115 HEK-293T C399(1.33)  LDD1589  [2]
 LDCM0386  CL116 HEK-293T C399(1.31)  LDD1590  [2]
 LDCM0387  CL117 HEK-293T C399(1.07)  LDD1591  [2]
 LDCM0388  CL118 HEK-293T C399(1.00)  LDD1592  [2]
 LDCM0389  CL119 HEK-293T C399(1.09)  LDD1593  [2]
 LDCM0390  CL12 HEK-293T C399(0.86)  LDD1594  [2]
 LDCM0391  CL120 HEK-293T C399(1.14)  LDD1595  [2]
 LDCM0392  CL121 HEK-293T C399(1.19)  LDD1596  [2]
 LDCM0393  CL122 HEK-293T C399(0.99)  LDD1597  [2]
 LDCM0394  CL123 HEK-293T C399(1.21)  LDD1598  [2]
 LDCM0395  CL124 HEK-293T C399(1.11)  LDD1599  [2]
 LDCM0396  CL125 HEK-293T C399(1.03)  LDD1600  [2]
 LDCM0397  CL126 HEK-293T C399(1.13)  LDD1601  [2]
 LDCM0398  CL127 HEK-293T C399(1.14)  LDD1602  [2]
 LDCM0399  CL128 HEK-293T C399(1.10)  LDD1603  [2]
 LDCM0400  CL13 HEK-293T C399(4.04)  LDD1604  [2]
 LDCM0401  CL14 HEK-293T C399(1.35)  LDD1605  [2]
 LDCM0402  CL15 HEK-293T C399(1.26)  LDD1606  [2]
 LDCM0403  CL16 HEK-293T C399(1.35)  LDD1607  [2]
 LDCM0404  CL17 HEK-293T C399(1.66)  LDD1608  [2]
 LDCM0405  CL18 HEK-293T C399(1.19)  LDD1609  [2]
 LDCM0406  CL19 HEK-293T C399(1.10)  LDD1610  [2]
 LDCM0407  CL2 HEK-293T C399(1.47)  LDD1611  [2]
 LDCM0408  CL20 HEK-293T C399(0.94)  LDD1612  [2]
 LDCM0409  CL21 HEK-293T C399(0.82)  LDD1613  [2]
 LDCM0410  CL22 HEK-293T C399(0.87)  LDD1614  [2]
 LDCM0411  CL23 HEK-293T C399(0.87)  LDD1615  [2]
 LDCM0412  CL24 HEK-293T C399(0.61)  LDD1616  [2]
 LDCM0413  CL25 HEK-293T C399(1.23)  LDD1617  [2]
 LDCM0414  CL26 HEK-293T C399(1.10)  LDD1618  [2]
 LDCM0415  CL27 HEK-293T C399(1.23)  LDD1619  [2]
 LDCM0416  CL28 HEK-293T C399(3.36)  LDD1620  [2]
 LDCM0417  CL29 HEK-293T C399(1.09)  LDD1621  [2]
 LDCM0418  CL3 HEK-293T C399(1.33)  LDD1622  [2]
 LDCM0419  CL30 HEK-293T C399(1.04)  LDD1623  [2]
 LDCM0420  CL31 HEK-293T C399(1.39)  LDD1624  [2]
 LDCM0421  CL32 HEK-293T C399(0.94)  LDD1625  [2]
 LDCM0422  CL33 HEK-293T C399(1.08)  LDD1626  [2]
 LDCM0423  CL34 HEK-293T C399(0.81)  LDD1627  [2]
 LDCM0424  CL35 HEK-293T C399(0.89)  LDD1628  [2]
 LDCM0425  CL36 HEK-293T C399(0.77)  LDD1629  [2]
 LDCM0426  CL37 HEK-293T C399(1.05)  LDD1630  [2]
 LDCM0428  CL39 HEK-293T C399(3.01)  LDD1632  [2]
 LDCM0429  CL4 HEK-293T C399(1.28)  LDD1633  [2]
 LDCM0430  CL40 HEK-293T C399(1.18)  LDD1634  [2]
 LDCM0431  CL41 HEK-293T C399(1.01)  LDD1635  [2]
 LDCM0432  CL42 HEK-293T C399(0.74)  LDD1636  [2]
 LDCM0433  CL43 HEK-293T C399(1.17)  LDD1637  [2]
 LDCM0434  CL44 HEK-293T C399(0.98)  LDD1638  [2]
 LDCM0435  CL45 HEK-293T C399(1.99)  LDD1639  [2]
 LDCM0436  CL46 HEK-293T C399(0.81)  LDD1640  [2]
 LDCM0437  CL47 HEK-293T C399(1.09)  LDD1641  [2]
 LDCM0438  CL48 HEK-293T C399(0.46)  LDD1642  [2]
 LDCM0439  CL49 HEK-293T C399(0.91)  LDD1643  [2]
 LDCM0440  CL5 HEK-293T C399(1.19)  LDD1644  [2]
 LDCM0441  CL50 HEK-293T C399(1.12)  LDD1645  [2]
 LDCM0443  CL52 HEK-293T C399(1.20)  LDD1646  [2]
 LDCM0444  CL53 HEK-293T C399(1.00)  LDD1647  [2]
 LDCM0445  CL54 HEK-293T C399(1.51)  LDD1648  [2]
 LDCM0446  CL55 HEK-293T C399(0.96)  LDD1649  [2]
 LDCM0447  CL56 HEK-293T C399(1.62)  LDD1650  [2]
 LDCM0448  CL57 HEK-293T C399(2.21)  LDD1651  [2]
 LDCM0449  CL58 HEK-293T C399(0.83)  LDD1652  [2]
 LDCM0450  CL59 HEK-293T C399(0.90)  LDD1653  [2]
 LDCM0451  CL6 HEK-293T C399(1.04)  LDD1654  [2]
 LDCM0452  CL60 HEK-293T C399(0.71)  LDD1655  [2]
 LDCM0453  CL61 HEK-293T C399(0.98)  LDD1656  [2]
 LDCM0454  CL62 HEK-293T C399(1.12)  LDD1657  [2]
 LDCM0455  CL63 HEK-293T C399(1.16)  LDD1658  [2]
 LDCM0456  CL64 HEK-293T C399(1.11)  LDD1659  [2]
 LDCM0457  CL65 HEK-293T C399(1.12)  LDD1660  [2]
 LDCM0458  CL66 HEK-293T C399(2.49)  LDD1661  [2]
 LDCM0459  CL67 HEK-293T C399(1.05)  LDD1662  [2]
 LDCM0460  CL68 HEK-293T C399(0.83)  LDD1663  [2]
 LDCM0461  CL69 HEK-293T C399(0.82)  LDD1664  [2]
 LDCM0462  CL7 HEK-293T C399(1.16)  LDD1665  [2]
 LDCM0463  CL70 HEK-293T C399(0.65)  LDD1666  [2]
 LDCM0464  CL71 HEK-293T C399(0.86)  LDD1667  [2]
 LDCM0465  CL72 HEK-293T C399(0.63)  LDD1668  [2]
 LDCM0466  CL73 HEK-293T C399(1.14)  LDD1669  [2]
 LDCM0467  CL74 HEK-293T C399(1.08)  LDD1670  [2]
 LDCM0469  CL76 HEK-293T C399(1.37)  LDD1672  [2]
 LDCM0470  CL77 HEK-293T C399(1.56)  LDD1673  [2]
 LDCM0471  CL78 HEK-293T C399(1.06)  LDD1674  [2]
 LDCM0472  CL79 HEK-293T C399(1.12)  LDD1675  [2]
 LDCM0473  CL8 HEK-293T C399(1.13)  LDD1676  [2]
 LDCM0474  CL80 HEK-293T C399(0.79)  LDD1677  [2]
 LDCM0475  CL81 HEK-293T C399(0.86)  LDD1678  [2]
 LDCM0476  CL82 HEK-293T C399(0.76)  LDD1679  [2]
 LDCM0477  CL83 HEK-293T C399(0.85)  LDD1680  [2]
 LDCM0478  CL84 HEK-293T C399(0.70)  LDD1681  [2]
 LDCM0479  CL85 HEK-293T C399(0.98)  LDD1682  [2]
 LDCM0480  CL86 HEK-293T C399(1.25)  LDD1683  [2]
 LDCM0481  CL87 HEK-293T C399(2.08)  LDD1684  [2]
 LDCM0482  CL88 HEK-293T C399(1.35)  LDD1685  [2]
 LDCM0483  CL89 HEK-293T C399(1.12)  LDD1686  [2]
 LDCM0484  CL9 HEK-293T C399(1.03)  LDD1687  [2]
 LDCM0485  CL90 HEK-293T C399(1.77)  LDD1688  [2]
 LDCM0486  CL91 HEK-293T C399(1.19)  LDD1689  [2]
 LDCM0487  CL92 HEK-293T C399(0.97)  LDD1690  [2]
 LDCM0488  CL93 HEK-293T C399(0.99)  LDD1691  [2]
 LDCM0489  CL94 HEK-293T C399(1.34)  LDD1692  [2]
 LDCM0490  CL95 HEK-293T C399(0.75)  LDD1693  [2]
 LDCM0491  CL96 HEK-293T C399(0.67)  LDD1694  [2]
 LDCM0492  CL97 HEK-293T C399(1.44)  LDD1695  [2]
 LDCM0493  CL98 HEK-293T C399(1.32)  LDD1696  [2]
 LDCM0494  CL99 HEK-293T C399(1.63)  LDD1697  [2]
 LDCM0495  E2913 HEK-293T C399(2.44)  LDD1698  [2]
 LDCM0468  Fragment33 HEK-293T C399(1.39)  LDD1671  [2]
 LDCM0427  Fragment51 HEK-293T C399(1.08)  LDD1631  [2]
 LDCM0022  KB02 HEK-293T C399(1.08)  LDD1492  [2]
 LDCM0023  KB03 HEK-293T C399(1.03)  LDD1497  [2]
 LDCM0024  KB05 HEK-293T C399(1.30)  LDD1502  [2]

The Interaction Atlas With This Target

The Drug(s) Related To This Target

Investigative
Click To Hide/Show 13 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Isis 6431 Antisense drug D0HU4L
Isis 6432 Antisense drug D02NUN
Isis 6434 Antisense drug D0DS2V
Isis 6435 Antisense drug D0Z3TU
Isis 6442 Antisense drug D07TMI
Isis 6443 Antisense drug D0UH5I
Isis 6445 Antisense drug D01YJD
Isis 6553 Antisense drug D04YKA
Isis 6581 Antisense drug D05ZZH
Isis 6603 Antisense drug D0LL1H
8-octyl-benzolactam-v9 Small molecular drug D04AXH
Ly-326449 Small molecular drug D06ZCX
Prostratin Small molecular drug D04JNZ
Discontinued
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Balanol Small molecular drug D0R2TM

References

1 Chemoproteomic capture of RNA binding activity in living cells. Nat Commun. 2023 Oct 7;14(1):6282. doi: 10.1038/s41467-023-41844-z.
Mass spectrometry data entry: PXD044625
2 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
3 SP3-FAIMS Chemoproteomics for High-Coverage Profiling of the Human Cysteinome*. Chembiochem. 2021 May 14;22(10):1841-1851. doi: 10.1002/cbic.202000870. Epub 2021 Feb 18.
Mass spectrometry data entry: PXD023056 , PXD023059 , PXD023058 , PXD023057 , PXD023060
4 Enhancing Cysteine Chemoproteomic Coverage through Systematic Assessment of Click Chemistry Product Fragmentation. Anal Chem. 2022 Mar 8;94(9):3800-3810. doi: 10.1021/acs.analchem.1c04402. Epub 2022 Feb 23.
Mass spectrometry data entry: PXD028853