Details of the Target

General Information of Target

Target ID LDTP03467
Target Name Neuroendocrine convertase 1 (PCSK1)
Gene Name PCSK1
Gene ID 5122
Synonyms
NEC1; Neuroendocrine convertase 1; NEC 1; EC 3.4.21.93; Prohormone convertase 1; Proprotein convertase 1; PC1
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MERRAWSLQCTAFVLFCAWCALNSAKAKRQFVNEWAAEIPGGPEAASAIAEELGYDLLGQ
IGSLENHYLFKHKNHPRRSRRSAFHITKRLSDDDRVIWAEQQYEKERSKRSALRDSALNL
FNDPMWNQQWYLQDTRMTAALPKLDLHVIPVWQKGITGKGVVITVLDDGLEWNHTDIYAN
YDPEASYDFNDNDHDPFPRYDPTNENKHGTRCAGEIAMQANNHKCGVGVAYNSKVGGIRM
LDGIVTDAIEASSIGFNPGHVDIYSASWGPNDDGKTVEGPGRLAQKAFEYGVKQGRQGKG
SIFVWASGNGGRQGDNCDCDGYTDSIYTISISSASQQGLSPWYAEKCSSTLATSYSSGDY
TDQRITSADLHNDCTETHTGTSASAPLAAGIFALALEANPNLTWRDMQHLVVWTSEYDPL
ANNPGWKKNGAGLMVNSRFGFGLLNAKALVDLADPRTWRSVPEKKECVVKDNDFEPRALK
ANGEVIIEIPTRACEGQENAIKSLEHVQFEATIEYSRRGDLHVTLTSAAGTSTVLLAERE
RDTSPNGFKNWDFMSVHTWGENPIGTWTLRITDMSGRIQNEGRIVNWKLILHGTSSQPEH
MKQPRVYTSYNTVQNDRRGVEKMVDPGEEQPTQENPKENTLVSKSPSSSSVGGRRDELEE
GAPSQAMLRLLQSAFSKNSPPKQSPKKSPSAKLNIPYENFYEALEKLNKPSQLKDSEDSL
YNDYVDVFYNTKPYKHRDDRLLQALVDILNEEN
Target Type
Literature-reported
Target Bioclass
Enzyme
Family
Peptidase S8 family, Furin subfamily
Subcellular location
Cytoplasmic vesicle, secretory vesicle
Function
Involved in the processing of hormone and other protein precursors at sites comprised of pairs of basic amino acid residues. Substrates include POMC, renin, enkephalin, dynorphin, somatostatin, insulin and AGRP.
TTD ID
T36445
Uniprot ID
P29120
DrugMap ID
TTED9LZ
Ensemble ID
ENST00000311106.8
HGNC ID
HGNC:8743
ChEMBL ID
CHEMBL3182

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
EFO27 SNV: p.A421T .
HCT15 SNV: p.N401K; p.P631H .
HSC3 SNV: p.S382Ter .
IGR1 SNV: p.I61F .
IPC298 SNV: p.E629K .
MFE319 Deletion: p.G42AfsTer55 .
NCIH2286 SNV: p.D272Y; p.P455L .
PANC0403 SNV: p.S647R .
SBC5 SNV: p.A45E .
SW1116 SNV: p.K637T .
SW1271 SNV: p.L22M .
SW480 SNV: p.W172C .
SW756 SNV: p.E104Q .
TF1 SNV: p.Y697H .

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  		C494(4.32); C212(4.83); C347(4.49)  LDD3342  [1]
CY-1
 Probe Info  		N.A.  LDD0246  [2]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 HCC15 C494(1.58); C212(1.50)  LDD2340  [1]
 LDCM0023  KB03 HCC15 C494(1.74); C212(2.00)  LDD2757  [1]
 LDCM0024  KB05 NCI-H1155 C494(4.32); C212(4.83); C347(4.49)  LDD3342  [1]

The Interaction Atlas With This Target

The Drug(s) Related To This Target

Approved
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Insulin Human BiotechDrug DB00030
Investigative
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Phenylacetyl-arg-val-arg-4-amidinobenzylamide Small molecular drug D0Y9PH

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 Cyclopropenone, Cyclopropeniminium Ion, and Cyclopropenethione as Novel Electrophilic Warheads for Potential Target Discovery of Triple-Negative Breast Cancer. J Med Chem. 2023 Feb 23;66(4):2851-2864. doi: 10.1021/acs.jmedchem.2c01889. Epub 2023 Feb 10.