Details of the Target

General Information of Target

Target ID LDTP09888
Target Name Proprotein convertase subtilisin/kexin type 5 (PCSK5)
Gene Name PCSK5
Gene ID 5125
Synonyms
PC5; PC6; Proprotein convertase subtilisin/kexin type 5; EC 3.4.21.-; Proprotein convertase 5; PC5; Proprotein convertase 6; PC6; hPC6; Subtilisin/kexin-like protease PC5
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MQLKIMPKKKRLSAGRVPLILFLCQMISALEVPLDPKLLEDLVQPPTITQQSPKDYIIDP
RENIVIQCEAKGKPPPSFSWTRNGTHFDIDKDPLVTMKPGTGTLIINIMSEGKAETYEGV
YQCTARNERGAAVSNNIVVRPSRSPLWTKEKLEPITLQSGQSLVLPCRPPIGLPPPIIFW
MDNSFQRLPQSERVSQGLNGDLYFSNVLPEDTREDYICYARFNHTQTIQQKQPISVKVIS
VDELNDTIAANLSDTEFYGAKSSRERPPTFLTPEGNASNKEELRGNVLSLECIAEGLPTP
IIYWAKEDGMLPKNRTVYKNFEKTLQIIHVSEADSGNYQCIAKNALGAIHHTISVRVKAA
PYWITAPQNLVLSPGEDGTLICRANGNPKPRISWLTNGVPIEIAPDDPSRKIDGDTIIFS
NVQERSSAVYQCNASNEYGYLLANAFVNVLAEPPRILTPANTLYQVIANRPALLDCAFFG
SPLPTIEWFKGAKGSALHEDIYVLHENGTLEIPVAQKDSTGTYTCVARNKLGMAKNEVHL
EIKDPTWIVKQPEYAVVQRGSMVSFECKVKHDHTLSLTVLWLKDNRELPSDERFTVDKDH
LVVADVSDDDSGTYTCVANTTLDSVSASAVLSVVAPTPTPAPVYDVPNPPFDLELTDQLD
KSVQLSWTPGDDNNSPITKFIIEYEDAMHKPGLWHHQTEVSGTQTTAQLKLSPYVNYSFR
VMAVNSIGKSLPSEASEQYLTKASEPDKNPTAVEGLGSEPDNLVITWKPLNGFESNGPGL
QYKVSWRQKDGDDEWTSVVVANVSKYIVSGTPTFVPYLIKVQALNDMGFAPEPAVVMGHS
GEDLPMVAPGNVRVNVVNSTLAEVHWDPVPLKSIRGHLQGYRIYYWKTQSSSKRNRRHIE
KKILTFQGSKTHGMLPGLEPFSHYTLNVRVVNGKGEGPASPDRVFNTPEGVPSAPSSLKI
VNPTLDSLTLEWDPPSHPNGILTEYTLKYQPINSTHELGPLVDLKIPANKTRWTLKNLNF
STRYKFYFYAQTSAGSGSQITEEAVTTVDEAGILPPDVGAGKVQAVNPRISNLTAAAAET
YANISWEYEGPEHVNFYVEYGVAGSKEEWRKEIVNGSRSFFGLKGLMPGTAYKVRVGAVG
DSGFVSSEDVFETGPAMASRQVDIATQGWFIGLMCAVALLILILLIVCFIRRNKGGKYPV
KEKEDAHADPEIQPMKEDDGTFGEYSDAEDHKPLKKGSRTPSDRTVKKEDSDDSLVDYGE
GVNGQFNEDGSFIGQYSGKKEKEPAEGNESSEAPSPVNAMNSFV
Target Type
Literature-reported
Target Bioclass
Enzyme
Family
Peptidase S8 family
Subcellular location
Secreted; Endomembrane system
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 and regulated secretory pathways. Plays an essential role in pregnancy establishment by proteolytic activation of a number of important factors such as BMP2, CALD1 and alpha-integrins.
TTD ID
T38581
Uniprot ID
Q92824
DrugMap ID
TTPFWHU
Ensemble ID
ENST00000376752.9
HGNC ID
HGNC:8747
ChEMBL ID
CHEMBL2826

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 2 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
IPM
 Probe Info  		N.A.  LDD0241  [1]
DBIA
 Probe Info  		C494(3.12)  LDD3385  [2]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0215  AC10 HEK-293T C468(1.01)  LDD1508  [3]
 LDCM0226  AC11 HEK-293T C494(0.97)  LDD1509  [3]
 LDCM0237  AC12 HEK-293T C494(1.20); C468(1.12)  LDD1510  [3]
 LDCM0270  AC15 HEK-293T C1082(0.37)  LDD1513  [3]
 LDCM0277  AC18 HEK-293T C468(1.01)  LDD1516  [3]
 LDCM0278  AC19 HEK-293T C494(1.25)  LDD1517  [3]
 LDCM0279  AC2 HEK-293T C468(0.93)  LDD1518  [3]
 LDCM0280  AC20 HEK-293T C494(0.94); C468(1.12)  LDD1519  [3]
 LDCM0283  AC23 HEK-293T C1082(1.01)  LDD1522  [3]
 LDCM0284  AC24 HEK-293T C494(0.73); C351(0.86)  LDD1523  [3]
 LDCM0286  AC26 HEK-293T C468(1.08)  LDD1525  [3]
 LDCM0287  AC27 HEK-293T C494(0.95)  LDD1526  [3]
 LDCM0288  AC28 HEK-293T C494(1.19); C468(1.13)  LDD1527  [3]
 LDCM0290  AC3 HEK-293T C494(1.03)  LDD1529  [3]
 LDCM0292  AC31 HEK-293T C1082(1.21)  LDD1531  [3]
 LDCM0293  AC32 HEK-293T C494(0.81); C351(0.80)  LDD1532  [3]
 LDCM0295  AC34 HEK-293T C468(1.15)  LDD1534  [3]
 LDCM0296  AC35 HEK-293T C494(1.16)  LDD1535  [3]
 LDCM0297  AC36 HEK-293T C494(1.04); C468(1.17)  LDD1536  [3]
 LDCM0300  AC39 HEK-293T C1082(0.92)  LDD1539  [3]
 LDCM0301  AC4 HEK-293T C494(1.25); C468(1.08)  LDD1540  [3]
 LDCM0302  AC40 HEK-293T C494(0.99); C351(0.86)  LDD1541  [3]
 LDCM0304  AC42 HEK-293T C468(1.02)  LDD1543  [3]
 LDCM0305  AC43 HEK-293T C494(1.12)  LDD1544  [3]
 LDCM0306  AC44 HEK-293T C494(1.11); C468(1.16)  LDD1545  [3]
 LDCM0309  AC47 HEK-293T C1082(0.92)  LDD1548  [3]
 LDCM0310  AC48 HEK-293T C494(1.13); C351(0.77)  LDD1549  [3]
 LDCM0313  AC50 HEK-293T C468(1.03)  LDD1552  [3]
 LDCM0314  AC51 HEK-293T C494(0.95)  LDD1553  [3]
 LDCM0315  AC52 HEK-293T C494(1.07); C468(1.15)  LDD1554  [3]
 LDCM0318  AC55 HEK-293T C1082(1.30)  LDD1557  [3]
 LDCM0319  AC56 HEK-293T C494(1.11); C351(0.81)  LDD1558  [3]
 LDCM0321  AC58 HEK-293T C468(1.05)  LDD1560  [3]
 LDCM0322  AC59 HEK-293T C494(1.02)  LDD1561  [3]
 LDCM0324  AC60 HEK-293T C494(0.96); C468(1.17)  LDD1563  [3]
 LDCM0327  AC63 HEK-293T C1082(0.99)  LDD1566  [3]
 LDCM0328  AC64 HEK-293T C494(1.03); C351(1.04)  LDD1567  [3]
 LDCM0334  AC7 HEK-293T C1082(0.55)  LDD1568  [3]
 LDCM0345  AC8 HEK-293T C494(0.89); C351(1.01)  LDD1569  [3]
 LDCM0275  AKOS034007705 HEK-293T C494(0.85); C351(0.73)  LDD1514  [3]
 LDCM0369  CL100 HEK-293T C494(0.92)  LDD1573  [3]
 LDCM0371  CL102 HEK-293T C494(0.95)  LDD1575  [3]
 LDCM0373  CL104 HEK-293T C494(0.78)  LDD1577  [3]
 LDCM0375  CL106 HEK-293T C494(1.02)  LDD1579  [3]
 LDCM0377  CL108 HEK-293T C494(0.95)  LDD1581  [3]
 LDCM0379  CL11 HEK-293T C1082(1.37)  LDD1583  [3]
 LDCM0380  CL110 HEK-293T C494(1.16)  LDD1584  [3]
 LDCM0382  CL112 HEK-293T C494(1.19)  LDD1586  [3]
 LDCM0384  CL114 HEK-293T C494(1.16)  LDD1588  [3]
 LDCM0386  CL116 HEK-293T C494(1.03)  LDD1590  [3]
 LDCM0388  CL118 HEK-293T C494(0.99)  LDD1592  [3]
 LDCM0390  CL12 HEK-293T C494(0.91); C351(1.10)  LDD1594  [3]
 LDCM0391  CL120 HEK-293T C494(0.84)  LDD1595  [3]
 LDCM0393  CL122 HEK-293T C494(1.06)  LDD1597  [3]
 LDCM0395  CL124 HEK-293T C494(0.88)  LDD1599  [3]
 LDCM0397  CL126 HEK-293T C494(1.13)  LDD1601  [3]
 LDCM0399  CL128 HEK-293T C494(1.07)  LDD1603  [3]
 LDCM0401  CL14 HEK-293T C494(0.95)  LDD1605  [3]
 LDCM0403  CL16 HEK-293T C494(1.06)  LDD1607  [3]
 LDCM0405  CL18 HEK-293T C468(1.05)  LDD1609  [3]
 LDCM0406  CL19 HEK-293T C494(1.08)  LDD1610  [3]
 LDCM0407  CL2 HEK-293T C494(1.03)  LDD1611  [3]
 LDCM0408  CL20 HEK-293T C494(1.37); C468(1.10)  LDD1612  [3]
 LDCM0411  CL23 HEK-293T C1082(1.48)  LDD1615  [3]
 LDCM0412  CL24 HEK-293T C494(1.27); C351(1.07)  LDD1616  [3]
 LDCM0414  CL26 HEK-293T C494(0.91)  LDD1618  [3]
 LDCM0416  CL28 HEK-293T C494(0.89)  LDD1620  [3]
 LDCM0419  CL30 HEK-293T C468(1.06)  LDD1623  [3]
 LDCM0420  CL31 HEK-293T C494(1.02)  LDD1624  [3]
 LDCM0421  CL32 HEK-293T C494(1.37); C468(1.09)  LDD1625  [3]
 LDCM0424  CL35 HEK-293T C1082(1.38)  LDD1628  [3]
 LDCM0425  CL36 HEK-293T C494(0.79); C351(1.05)  LDD1629  [3]
 LDCM0429  CL4 HEK-293T C494(0.87)  LDD1633  [3]
 LDCM0430  CL40 HEK-293T C494(0.93)  LDD1634  [3]
 LDCM0432  CL42 HEK-293T C468(1.10)  LDD1636  [3]
 LDCM0433  CL43 HEK-293T C494(1.11)  LDD1637  [3]
 LDCM0434  CL44 HEK-293T C494(1.06); C468(1.13)  LDD1638  [3]
 LDCM0437  CL47 HEK-293T C1082(1.50)  LDD1641  [3]
 LDCM0438  CL48 HEK-293T C494(0.76); C351(0.97)  LDD1642  [3]
 LDCM0441  CL50 HEK-293T C494(1.07)  LDD1645  [3]
 LDCM0443  CL52 HEK-293T C494(0.88)  LDD1646  [3]
 LDCM0445  CL54 HEK-293T C468(0.98)  LDD1648  [3]
 LDCM0446  CL55 HEK-293T C494(1.27)  LDD1649  [3]
 LDCM0447  CL56 HEK-293T C494(1.17); C468(1.21)  LDD1650  [3]
 LDCM0450  CL59 HEK-293T C1082(1.22)  LDD1653  [3]
 LDCM0451  CL6 HEK-293T C468(0.97)  LDD1654  [3]
 LDCM0452  CL60 HEK-293T C494(0.96); C351(1.18)  LDD1655  [3]
 LDCM0454  CL62 HEK-293T C494(0.99)  LDD1657  [3]
 LDCM0456  CL64 HEK-293T C494(0.89)  LDD1659  [3]
 LDCM0458  CL66 HEK-293T C468(1.11)  LDD1661  [3]
 LDCM0459  CL67 HEK-293T C494(1.05)  LDD1662  [3]
 LDCM0460  CL68 HEK-293T C494(1.12); C468(1.14)  LDD1663  [3]
 LDCM0462  CL7 HEK-293T C494(1.21)  LDD1665  [3]
 LDCM0464  CL71 HEK-293T C1082(2.22)  LDD1667  [3]
 LDCM0465  CL72 HEK-293T C494(1.00); C351(1.05)  LDD1668  [3]
 LDCM0467  CL74 HEK-293T C494(0.93)  LDD1670  [3]
 LDCM0469  CL76 HEK-293T C494(1.01)  LDD1672  [3]
 LDCM0471  CL78 HEK-293T C468(1.03)  LDD1674  [3]
 LDCM0472  CL79 HEK-293T C494(1.13)  LDD1675  [3]
 LDCM0473  CL8 HEK-293T C494(1.40); C468(1.14)  LDD1676  [3]
 LDCM0474  CL80 HEK-293T C494(1.09); C468(1.12)  LDD1677  [3]
 LDCM0477  CL83 HEK-293T C1082(0.85)  LDD1680  [3]
 LDCM0478  CL84 HEK-293T C494(0.89); C351(0.97)  LDD1681  [3]
 LDCM0480  CL86 HEK-293T C494(1.02)  LDD1683  [3]
 LDCM0482  CL88 HEK-293T C494(0.93)  LDD1685  [3]
 LDCM0485  CL90 HEK-293T C468(1.17)  LDD1688  [3]
 LDCM0486  CL91 HEK-293T C494(1.15)  LDD1689  [3]
 LDCM0487  CL92 HEK-293T C494(1.22); C468(1.27)  LDD1690  [3]
 LDCM0490  CL95 HEK-293T C1082(0.01)  LDD1693  [3]
 LDCM0491  CL96 HEK-293T C494(1.00); C351(1.08)  LDD1694  [3]
 LDCM0493  CL98 HEK-293T C494(1.05)  LDD1696  [3]
 LDCM0427  Fragment51 HEK-293T C494(1.02)  LDD1631  [3]
 LDCM0022  KB02 HEK-293T C494(1.13)  LDD1492  [3]
 LDCM0023  KB03 HEK-293T C494(1.09)  LDD1497  [3]
 LDCM0024  KB05 OVISE C494(3.12)  LDD3385  [2]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 8 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Pachytene checkpoint protein 2 homolog (TRIP13) AAA ATPase family Q15645
Phenylalanine--tRNA ligase, mitochondrial (FARS2) Class-II aminoacyl-tRNA synthetase family O95363
Proprotein convertase subtilisin/kexin type 6 (PCSK6) Peptidase S8 family P29122
Tribbles homolog 3 (TRIB3) CAMK Ser/Thr protein kinase family Q96RU7
Serine/threonine-protein kinase 16 (STK16) Ser/Thr protein kinase family O75716
TNF receptor-associated factor 4 (TRAF4) TNF receptor-associated factor family Q9BUZ4
Tripartite motif-containing protein 42 (TRIM42) TRIM/RBCC family Q8IWZ5
Glutaredoxin-3 (GLRX3) . O76003
Transporter and channel
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
MyoD family inhibitor (MDFI) MDFI family Q99750
Phospholipid scramblase 4 (PLSCR4) Phospholipid scramblase family Q9NRQ2
Transcription factor
Click To Hide/Show 9 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Homeobox protein Hox-B9 (HOXB9) Abd-B homeobox family P17482
Homeobox protein Hox-A1 (HOXA1) Antp homeobox family P49639
Zinc finger protein 547 (ZNF547) Krueppel C2H2-type zinc-finger protein family Q8IVP9
Zinc finger protein 655 (ZNF655) Krueppel C2H2-type zinc-finger protein family Q8N720
Zinc finger protein 837 (ZNF837) Krueppel C2H2-type zinc-finger protein family Q96EG3
Nuclear receptor subfamily 4 group A member 3 (NR4A3) Nuclear hormone receptor family Q92570
Homeobox protein OTX1 (OTX1) Paired homeobox family P32242
POU domain, class 4, transcription factor 2 (POU4F2) POU transcription factor family Q12837
Homeobox protein MOX-2 (MEOX2) . P50222
Other
Click To Hide/Show 29 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Cysteine-rich tail protein 1 (CYSRT1) CYSRT1 family A8MQ03
Dedicator of cytokinesis protein 2 (DOCK2) DOCK family Q92608
Protein INCA1 (INCA1) INCA family Q0VD86
Keratin-associated protein 1-1 (KRTAP1-1) KRTAP type 1 family Q07627
Keratin-associated protein 10-7 (KRTAP10-7) KRTAP type 10 family P60409
Keratin-associated protein 10-8 (KRTAP10-8) KRTAP type 10 family P60410
Keratin-associated protein 10-9 (KRTAP10-9) KRTAP type 10 family P60411
Keratin-associated protein 12-2 (KRTAP12-2) KRTAP type 12 family P59991
Keratin-associated protein 19-2 (KRTAP19-2) KRTAP type 19 family Q3LHN2
Keratin-associated protein 3-1 (KRTAP3-1) KRTAP type 3 family Q9BYR8
Keratin-associated protein 3-2 (KRTAP3-2) KRTAP type 3 family Q9BYR7
Keratin-associated protein 4-12 (KRTAP4-12) KRTAP type 4 family Q9BQ66
Keratin-associated protein 5-9 (KRTAP5-9) KRTAP type 5 family P26371
Late cornified envelope protein 1D (LCE1D) LCE family Q5T752
Late cornified envelope protein 1F (LCE1F) LCE family Q5T754
Late cornified envelope protein 2C (LCE2C) LCE family Q5TA81
Late cornified envelope protein 3C (LCE3C) LCE family Q5T5A8
Late cornified envelope protein 3D (LCE3D) LCE family Q9BYE3
Notch homolog 2 N-terminal-like protein A (NOTCH2NLA) NOTCH family Q7Z3S9
Notch homolog 2 N-terminal-like protein C (NOTCH2NLC) NOTCH family P0DPK4
Keratin-associated protein 11-1 (KRTAP11-1) PMG family Q8IUC1
Keratin-associated protein 13-3 (KRTAP13-3) PMG family Q3SY46
Protein sprouty homolog 1 (SPRY1) Sprouty family O43609
Tektin-4 (TEKT4) Tektin family Q8WW24
Synaptic plasticity regulator PANTS (C22orf39) UPF0545 family Q6P5X5
Fibroblast growth factor receptor substrate 3 (FRS3) . O43559
FMR1-interacting protein NUFIP2 (NUFIP2) . Q7Z417
Sperm mitochondrial-associated cysteine-rich protein (SMCP) . P49901
Uncharacterized protein C17orf50 (C17orf50) . Q8WW18

The Drug(s) Related To This Target

Investigative
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Furin Inhibitor Peptide Small molecular drug D05JJL

References

1 Oxidant-Induced Bioconjugation for Protein Labeling in Live Cells. ACS Chem Biol. 2023 Jan 20;18(1):112-122. doi: 10.1021/acschembio.2c00740. Epub 2022 Dec 21.
2 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
3 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