Details of the Target

General Information of Target

Target ID LDTP03468
Target Name Proprotein convertase subtilisin/kexin type 6 (PCSK6)
Gene Name PCSK6
Gene ID 5046
Synonyms
PACE4; Proprotein convertase subtilisin/kexin type 6; EC 3.4.21.-; Paired basic amino acid cleaving enzyme 4; Subtilisin-like proprotein convertase 4; SPC4; Subtilisin/kexin-like protease PACE4
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MPPRAPPAPGPRPPPRAAAATDTAAGAGGAGGAGGAGGPGFRPLAPRPWRWLLLLALPAA
CSAPPPRPVYTNHWAVQVLGGPAEADRVAAAHGYLNLGQIGNLEDYYHFYHSKTFKRSTL
SSRGPHTFLRMDPQVKWLQQQEVKRRVKRQVRSDPQALYFNDPIWSNMWYLHCGDKNSRC
RSEMNVQAAWKRGYTGKNVVVTILDDGIERNHPDLAPNYDSYASYDVNGNDYDPSPRYDA
SNENKHGTRCAGEVAASANNSYCIVGIAYNAKIGGIRMLDGDVTDVVEAKSLGIRPNYID
IYSASWGPDDDGKTVDGPGRLAKQAFEYGIKKGRQGLGSIFVWASGNGGREGDYCSCDGY
TNSIYTISVSSATENGYKPWYLEECASTLATTYSSGAFYERKIVTTDLRQRCTDGHTGTS
VSAPMVAGIIALALEANSQLTWRDVQHLLVKTSRPAHLKASDWKVNGAGHKVSHFYGFGL
VDAEALVVEAKKWTAVPSQHMCVAASDKRPRSIPLVQVLRTTALTSACAEHSDQRVVYLE
HVVVRTSISHPRRGDLQIYLVSPSGTKSQLLAKRLLDLSNEGFTNWEFMTVHCWGEKAEG
QWTLEIQDLPSQVRNPEKQGKLKEWSLILYGTAEHPYHTFSAHQSRSRMLELSAPELEPP
KAALSPSQVEVPEDEEDYTAQSTPGSANILQTSVCHPECGDKGCDGPNADQCLNCVHFSL
GSVKTSRKCVSVCPLGYFGDTAARRCRRCHKGCETCSSRAATQCLSCRRGFYHHQEMNTC
VTLCPAGFYADESQKNCLKCHPSCKKCVDEPEKCTVCKEGFSLARGSCIPDCEPGTYFDS
ELIRCGECHHTCGTCVGPGREECIHCAKNFHFHDWKCVPACGEGFYPEEMPGLPHKVCRR
CDENCLSCAGSSRNCSRCKTGFTQLGTSCITNHTCSNADETFCEMVKSNRLCERKLFIQF
CCRTCLLAG
Target Type
Literature-reported
Target Bioclass
Enzyme
Family
Peptidase S8 family
Subcellular location
Secreted; Endoplasmic reticulum; Endomembrane system; Peripheral membrane protein
Function
Serine endoprotease that processes various proproteins by cleavage at paired basic amino acids, recognizing the RXXX[KR]R consensus motif. Likely functions in the constitutive secretory pathway, with unique restricted distribution in both neuroendocrine and non-neuroendocrine tissues.
TTD ID
T86503
Uniprot ID
P29122
DrugMap ID
TT75LN9
Ensemble ID
ENST00000611716.5
HGNC ID
HGNC:8569
ChEMBL ID
CHEMBL2951

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
A172 SNV: p.L97M .
EFO27 SNV: p.E587K .
HT115 SNV: p.D214A .
IGR1 SNV: p.V147L .
LS180 SNV: p.V200A .
MEWO SNV: p.T127I .
NCIH358 SNV: p.G685C .
NCIH446 SNV: p.G685V .
SNU478 SNV: p.R249C .
TC71 SNV: p.L524M .
TE1 SNV: p.I330M .
TOV21G SNV: p.P616Q .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 3 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info  		C528(2.34)  LDD3380  [1]
PF-06672131
 Probe Info  		N.A.  LDD0152  [2]
AOyne
 Probe Info  		14.40  LDD0443  [3]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0215  AC10 HEK-293T C528(1.01)  LDD1508  [4]
 LDCM0226  AC11 HEK-293T C528(1.21)  LDD1509  [4]
 LDCM0237  AC12 HEK-293T C528(0.97)  LDD1510  [4]
 LDCM0259  AC14 HEK-293T C528(1.15)  LDD1512  [4]
 LDCM0270  AC15 HEK-293T C528(0.86)  LDD1513  [4]
 LDCM0277  AC18 HEK-293T C528(1.07)  LDD1516  [4]
 LDCM0278  AC19 HEK-293T C528(1.53)  LDD1517  [4]
 LDCM0279  AC2 HEK-293T C528(1.15)  LDD1518  [4]
 LDCM0280  AC20 HEK-293T C528(0.94)  LDD1519  [4]
 LDCM0281  AC21 HEK-293T C528(1.07)  LDD1520  [4]
 LDCM0282  AC22 HEK-293T C528(1.35)  LDD1521  [4]
 LDCM0283  AC23 HEK-293T C528(0.82)  LDD1522  [4]
 LDCM0284  AC24 HEK-293T C528(0.98)  LDD1523  [4]
 LDCM0286  AC26 HEK-293T C528(1.05)  LDD1525  [4]
 LDCM0287  AC27 HEK-293T C528(1.01)  LDD1526  [4]
 LDCM0288  AC28 HEK-293T C528(1.13)  LDD1527  [4]
 LDCM0289  AC29 HEK-293T C528(1.10)  LDD1528  [4]
 LDCM0290  AC3 HEK-293T C528(1.07)  LDD1529  [4]
 LDCM0291  AC30 HEK-293T C528(1.17)  LDD1530  [4]
 LDCM0292  AC31 HEK-293T C528(0.86)  LDD1531  [4]
 LDCM0293  AC32 HEK-293T C528(1.06)  LDD1532  [4]
 LDCM0295  AC34 HEK-293T C528(1.16)  LDD1534  [4]
 LDCM0296  AC35 HEK-293T C528(1.11)  LDD1535  [4]
 LDCM0297  AC36 HEK-293T C528(0.91)  LDD1536  [4]
 LDCM0298  AC37 HEK-293T C528(1.08)  LDD1537  [4]
 LDCM0299  AC38 HEK-293T C528(0.94)  LDD1538  [4]
 LDCM0300  AC39 HEK-293T C528(0.85)  LDD1539  [4]
 LDCM0301  AC4 HEK-293T C528(1.03)  LDD1540  [4]
 LDCM0302  AC40 HEK-293T C528(0.76)  LDD1541  [4]
 LDCM0304  AC42 HEK-293T C528(1.10)  LDD1543  [4]
 LDCM0305  AC43 HEK-293T C528(1.09)  LDD1544  [4]
 LDCM0306  AC44 HEK-293T C528(1.13)  LDD1545  [4]
 LDCM0307  AC45 HEK-293T C528(0.89)  LDD1546  [4]
 LDCM0308  AC46 HEK-293T C528(1.16)  LDD1547  [4]
 LDCM0309  AC47 HEK-293T C528(0.95)  LDD1548  [4]
 LDCM0310  AC48 HEK-293T C528(0.94)  LDD1549  [4]
 LDCM0312  AC5 HEK-293T C528(0.99)  LDD1551  [4]
 LDCM0313  AC50 HEK-293T C528(1.00)  LDD1552  [4]
 LDCM0314  AC51 HEK-293T C528(1.10)  LDD1553  [4]
 LDCM0315  AC52 HEK-293T C528(1.00)  LDD1554  [4]
 LDCM0316  AC53 HEK-293T C528(0.94)  LDD1555  [4]
 LDCM0317  AC54 HEK-293T C528(1.09)  LDD1556  [4]
 LDCM0318  AC55 HEK-293T C528(0.88)  LDD1557  [4]
 LDCM0319  AC56 HEK-293T C528(0.95)  LDD1558  [4]
 LDCM0321  AC58 HEK-293T C528(1.12)  LDD1560  [4]
 LDCM0322  AC59 HEK-293T C528(1.12)  LDD1561  [4]
 LDCM0323  AC6 HEK-293T C528(1.05)  LDD1562  [4]
 LDCM0324  AC60 HEK-293T C528(1.10)  LDD1563  [4]
 LDCM0325  AC61 HEK-293T C528(1.13)  LDD1564  [4]
 LDCM0326  AC62 HEK-293T C528(1.22)  LDD1565  [4]
 LDCM0327  AC63 HEK-293T C528(0.86)  LDD1566  [4]
 LDCM0328  AC64 HEK-293T C528(1.30)  LDD1567  [4]
 LDCM0334  AC7 HEK-293T C528(0.83)  LDD1568  [4]
 LDCM0345  AC8 HEK-293T C528(0.87)  LDD1569  [4]
 LDCM0248  AKOS034007472 HEK-293T C528(0.93)  LDD1511  [4]
 LDCM0275  AKOS034007705 HEK-293T C528(1.17)  LDD1514  [4]
 LDCM0367  CL1 HEK-293T C528(1.02)  LDD1571  [4]
 LDCM0368  CL10 HEK-293T C528(1.42)  LDD1572  [4]
 LDCM0369  CL100 HEK-293T C593(1.02)  LDD1573  [4]
 LDCM0370  CL101 HEK-293T C528(1.07)  LDD1574  [4]
 LDCM0371  CL102 HEK-293T C528(1.05)  LDD1575  [4]
 LDCM0372  CL103 HEK-293T C528(1.20)  LDD1576  [4]
 LDCM0373  CL104 HEK-293T C593(1.07)  LDD1577  [4]
 LDCM0374  CL105 HEK-293T C528(1.20)  LDD1578  [4]
 LDCM0375  CL106 HEK-293T C528(0.97)  LDD1579  [4]
 LDCM0376  CL107 HEK-293T C528(1.02)  LDD1580  [4]
 LDCM0377  CL108 HEK-293T C593(1.20)  LDD1581  [4]
 LDCM0378  CL109 HEK-293T C528(1.13)  LDD1582  [4]
 LDCM0379  CL11 HEK-293T C528(0.97)  LDD1583  [4]
 LDCM0380  CL110 HEK-293T C528(1.18)  LDD1584  [4]
 LDCM0381  CL111 HEK-293T C528(0.95)  LDD1585  [4]
 LDCM0382  CL112 HEK-293T C593(0.67)  LDD1586  [4]
 LDCM0383  CL113 HEK-293T C528(0.87)  LDD1587  [4]
 LDCM0384  CL114 HEK-293T C528(1.11)  LDD1588  [4]
 LDCM0385  CL115 HEK-293T C528(1.09)  LDD1589  [4]
 LDCM0386  CL116 HEK-293T C593(0.96)  LDD1590  [4]
 LDCM0387  CL117 HEK-293T C528(1.13)  LDD1591  [4]
 LDCM0388  CL118 HEK-293T C528(1.21)  LDD1592  [4]
 LDCM0389  CL119 HEK-293T C528(1.10)  LDD1593  [4]
 LDCM0390  CL12 HEK-293T C528(1.17)  LDD1594  [4]
 LDCM0391  CL120 HEK-293T C593(1.24)  LDD1595  [4]
 LDCM0392  CL121 HEK-293T C528(1.25)  LDD1596  [4]
 LDCM0393  CL122 HEK-293T C528(1.09)  LDD1597  [4]
 LDCM0394  CL123 HEK-293T C528(1.18)  LDD1598  [4]
 LDCM0395  CL124 HEK-293T C593(1.17)  LDD1599  [4]
 LDCM0396  CL125 HEK-293T C528(0.86)  LDD1600  [4]
 LDCM0397  CL126 HEK-293T C528(1.19)  LDD1601  [4]
 LDCM0398  CL127 HEK-293T C528(1.10)  LDD1602  [4]
 LDCM0399  CL128 HEK-293T C593(0.99)  LDD1603  [4]
 LDCM0400  CL13 HEK-293T C528(1.01)  LDD1604  [4]
 LDCM0401  CL14 HEK-293T C528(1.17)  LDD1605  [4]
 LDCM0402  CL15 HEK-293T C528(1.28)  LDD1606  [4]
 LDCM0403  CL16 HEK-293T C593(0.79)  LDD1607  [4]
 LDCM0405  CL18 HEK-293T C528(1.28)  LDD1609  [4]
 LDCM0406  CL19 HEK-293T C528(1.03)  LDD1610  [4]
 LDCM0407  CL2 HEK-293T C528(1.08)  LDD1611  [4]
 LDCM0408  CL20 HEK-293T C528(0.97)  LDD1612  [4]
 LDCM0409  CL21 HEK-293T C528(1.00)  LDD1613  [4]
 LDCM0410  CL22 HEK-293T C528(1.16)  LDD1614  [4]
 LDCM0411  CL23 HEK-293T C528(0.85)  LDD1615  [4]
 LDCM0412  CL24 HEK-293T C528(0.97)  LDD1616  [4]
 LDCM0413  CL25 HEK-293T C528(0.91)  LDD1617  [4]
 LDCM0414  CL26 HEK-293T C528(1.06)  LDD1618  [4]
 LDCM0415  CL27 HEK-293T C528(1.05)  LDD1619  [4]
 LDCM0416  CL28 HEK-293T C593(1.06)  LDD1620  [4]
 LDCM0418  CL3 HEK-293T C528(1.10)  LDD1622  [4]
 LDCM0419  CL30 HEK-293T C528(1.05)  LDD1623  [4]
 LDCM0420  CL31 HEK-293T C528(1.23)  LDD1624  [4]
 LDCM0421  CL32 HEK-293T C528(1.06)  LDD1625  [4]
 LDCM0422  CL33 HEK-293T C528(1.16)  LDD1626  [4]
 LDCM0423  CL34 HEK-293T C528(1.07)  LDD1627  [4]
 LDCM0424  CL35 HEK-293T C528(0.87)  LDD1628  [4]
 LDCM0425  CL36 HEK-293T C528(1.10)  LDD1629  [4]
 LDCM0426  CL37 HEK-293T C528(0.88)  LDD1630  [4]
 LDCM0428  CL39 HEK-293T C528(1.21)  LDD1632  [4]
 LDCM0429  CL4 HEK-293T C593(0.98)  LDD1633  [4]
 LDCM0430  CL40 HEK-293T C593(0.89)  LDD1634  [4]
 LDCM0432  CL42 HEK-293T C528(0.99)  LDD1636  [4]
 LDCM0433  CL43 HEK-293T C528(1.05)  LDD1637  [4]
 LDCM0434  CL44 HEK-293T C528(1.17)  LDD1638  [4]
 LDCM0435  CL45 HEK-293T C528(0.97)  LDD1639  [4]
 LDCM0436  CL46 HEK-293T C528(1.08)  LDD1640  [4]
 LDCM0437  CL47 HEK-293T C528(0.94)  LDD1641  [4]
 LDCM0438  CL48 HEK-293T C528(0.86)  LDD1642  [4]
 LDCM0439  CL49 HEK-293T C528(0.97)  LDD1643  [4]
 LDCM0441  CL50 HEK-293T C528(1.16)  LDD1645  [4]
 LDCM0443  CL52 HEK-293T C593(0.81)  LDD1646  [4]
 LDCM0445  CL54 HEK-293T C528(0.98)  LDD1648  [4]
 LDCM0446  CL55 HEK-293T C528(1.10)  LDD1649  [4]
 LDCM0447  CL56 HEK-293T C528(1.09)  LDD1650  [4]
 LDCM0448  CL57 HEK-293T C528(0.99)  LDD1651  [4]
 LDCM0449  CL58 HEK-293T C528(0.96)  LDD1652  [4]
 LDCM0450  CL59 HEK-293T C528(0.97)  LDD1653  [4]
 LDCM0451  CL6 HEK-293T C528(1.18)  LDD1654  [4]
 LDCM0452  CL60 HEK-293T C528(1.13)  LDD1655  [4]
 LDCM0453  CL61 HEK-293T C528(0.73)  LDD1656  [4]
 LDCM0454  CL62 HEK-293T C528(1.09)  LDD1657  [4]
 LDCM0455  CL63 HEK-293T C528(1.02)  LDD1658  [4]
 LDCM0456  CL64 HEK-293T C593(1.00)  LDD1659  [4]
 LDCM0458  CL66 HEK-293T C528(1.11)  LDD1661  [4]
 LDCM0459  CL67 HEK-293T C528(1.09)  LDD1662  [4]
 LDCM0460  CL68 HEK-293T C528(0.97)  LDD1663  [4]
 LDCM0461  CL69 HEK-293T C528(0.94)  LDD1664  [4]
 LDCM0462  CL7 HEK-293T C528(1.12)  LDD1665  [4]
 LDCM0463  CL70 HEK-293T C528(0.97)  LDD1666  [4]
 LDCM0464  CL71 HEK-293T C528(0.85)  LDD1667  [4]
 LDCM0465  CL72 HEK-293T C528(1.35)  LDD1668  [4]
 LDCM0466  CL73 HEK-293T C528(1.00)  LDD1669  [4]
 LDCM0467  CL74 HEK-293T C528(1.07)  LDD1670  [4]
 LDCM0469  CL76 HEK-293T C593(1.01)  LDD1672  [4]
 LDCM0471  CL78 HEK-293T C528(1.03)  LDD1674  [4]
 LDCM0472  CL79 HEK-293T C528(1.18)  LDD1675  [4]
 LDCM0473  CL8 HEK-293T C528(1.31)  LDD1676  [4]
 LDCM0474  CL80 HEK-293T C528(1.09)  LDD1677  [4]
 LDCM0475  CL81 HEK-293T C528(0.95)  LDD1678  [4]
 LDCM0476  CL82 HEK-293T C528(0.92)  LDD1679  [4]
 LDCM0477  CL83 HEK-293T C528(0.98)  LDD1680  [4]
 LDCM0478  CL84 HEK-293T C528(1.09)  LDD1681  [4]
 LDCM0479  CL85 HEK-293T C528(1.17)  LDD1682  [4]
 LDCM0480  CL86 HEK-293T C528(1.07)  LDD1683  [4]
 LDCM0481  CL87 HEK-293T C528(1.07)  LDD1684  [4]
 LDCM0482  CL88 HEK-293T C593(0.87)  LDD1685  [4]
 LDCM0484  CL9 HEK-293T C528(1.18)  LDD1687  [4]
 LDCM0485  CL90 HEK-293T C528(1.23)  LDD1688  [4]
 LDCM0486  CL91 HEK-293T C528(1.08)  LDD1689  [4]
 LDCM0487  CL92 HEK-293T C528(0.86)  LDD1690  [4]
 LDCM0488  CL93 HEK-293T C528(0.96)  LDD1691  [4]
 LDCM0489  CL94 HEK-293T C528(0.96)  LDD1692  [4]
 LDCM0490  CL95 HEK-293T C528(0.91)  LDD1693  [4]
 LDCM0491  CL96 HEK-293T C528(0.85)  LDD1694  [4]
 LDCM0492  CL97 HEK-293T C528(1.07)  LDD1695  [4]
 LDCM0493  CL98 HEK-293T C528(1.21)  LDD1696  [4]
 LDCM0494  CL99 HEK-293T C528(1.09)  LDD1697  [4]
 LDCM0495  E2913 HEK-293T C528(1.20)  LDD1698  [4]
 LDCM0468  Fragment33 HEK-293T C528(1.04)  LDD1671  [4]
 LDCM0427  Fragment51 HEK-293T C528(1.02)  LDD1631  [4]
 LDCM0022  KB02 HEK-293T C528(1.05)  LDD1492  [4]
 LDCM0023  KB03 HEK-293T C528(1.05)  LDD1497  [4]
 LDCM0024  KB05 OV-90 C528(2.34)  LDD3380  [1]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Transcription factor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Zinc finger protein 441 (ZNF441) Krueppel C2H2-type zinc-finger protein family Q8N8Z8

The Drug(s) Related To This Target

Investigative
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Furin Inhibitor Peptide Small molecular drug D05JJL
Peptide 18 Small molecular drug D0A6FZ

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 Site-Specific Activity-Based Protein Profiling Using Phosphonate Handles. Mol Cell Proteomics. 2023 Jan;22(1):100455. doi: 10.1016/j.mcpro.2022.100455. Epub 2022 Nov 24.
Mass spectrometry data entry: PXD036569
3 Chemoproteomic profiling of targets of lipid-derived electrophiles by bioorthogonal aminooxy probe. Redox Biol. 2017 Aug;12:712-718. doi: 10.1016/j.redox.2017.04.001. Epub 2017 Apr 5.
4 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