Details of the Target

General Information of Target

Target ID LDTP02856
Target Name Neuroendocrine convertase 2 (PCSK2)
Gene Name PCSK2
Gene ID 5126
Synonyms
NEC2; Neuroendocrine convertase 2; NEC 2; EC 3.4.21.94; KEX2-like endoprotease 2; Prohormone convertase 2; Proprotein convertase 2; PC2
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MKGGCVSQWKAAAGFLFCVMVFASAERPVFTNHFLVELHKGGEDKARQVAAEHGFGVRKL
PFAEGLYHFYHNGLAKAKRRRSLHHKQQLERDPRVKMALQQEGFDRKKRGYRDINEIDIN
MNDPLFTKQWYLINTGQADGTPGLDLNVAEAWELGYTGKGVTIGIMDDGIDYLHPDLASN
YNAEASYDFSSNDPYPYPRYTDDWFNSHGTRCAGEVSAAANNNICGVGVAYNSKVAGIRM
LDQPFMTDIIEASSISHMPQLIDIYSASWGPTDNGKTVDGPRELTLQAMADGVNKGRGGK
GSIYVWASGDGGSYDDCNCDGYASSMWTISINSAINDGRTALYDESCSSTLASTFSNGRK
RNPEAGVATTDLYGNCTLRHSGTSAAAPEAAGVFALALEANLGLTWRDMQHLTVLTSKRN
QLHDEVHQWRRNGVGLEFNHLFGYGVLDAGAMVKMAKDWKTVPERFHCVGGSVQDPEKIP
STGKLVLTLTTDACEGKENFVRYLEHVQAVITVNATRRGDLNINMTSPMGTKSILLSRRP
RDDDSKVGFDKWPFMTTHTWGEDARGTWTLELGFVGSAPQKGVLKEWTLMLHGTQSAPYI
DQVVRDYQSKLAMSKKEELEEELDEAVERSLKSILNKN
Target Type
Literature-reported
Target Bioclass
Enzyme
Family
Peptidase S8 family, Furin subfamily
Subcellular location
Cytoplasmic vesicle, secretory vesicle
Function
Serine endopeptidase which is involved in the processing of hormone and other protein precursors at sites comprised of pairs of basic amino acid residues. Responsible for the release of glucagon from proglucagon in pancreatic A cells.
TTD ID
T97749
Uniprot ID
P16519
DrugMap ID
TT46F0P
Ensemble ID
ENST00000262545.7
HGNC ID
HGNC:8744
ChEMBL ID
CHEMBL2433

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
A549 SNV: p.R539C .
EOL1 SNV: p.G312S .
HCT15 SNV: p.R239W; p.E437K .
HEC1B SNV: p.R106Ter .
HEL SNV: p.R605W .
HEL9217 SNV: p.R605W .
KMS11 SNV: p.Ter639QextTer27 .
PANC0403 SNV: p.R419Q .
SW1990 SNV: p.P93S .
U937 SNV: p.Ter639YextTer27 .

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
DBIA
 Probe Info  		C225(4.68)  LDD3342  [1]
NAIA_5
 Probe Info  		N.A.  LDD2225  [2]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 HCC15 C225(1.43)  LDD2340  [1]
 LDCM0023  KB03 HCC15 C225(1.28)  LDD2757  [1]
 LDCM0024  KB05 NCI-H1155 C225(4.68)  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 N-Acryloylindole-alkyne (NAIA) enables imaging and profiling new ligandable cysteines and oxidized thiols by chemoproteomics. Nat Commun. 2023 Jun 15;14(1):3564. doi: 10.1038/s41467-023-39268-w.
Mass spectrometry data entry: PXD041264