Details of the Target

General Information of Target

Target ID LDTP13281
Target Name ProSAAS (PCSK1N)
Gene Name PCSK1N
Gene ID 27344
Synonyms
ProSAAS; Proprotein convertase subtilisin/kexin type 1 inhibitor; Proprotein convertase 1 inhibitor; pro-SAAS) [Cleaved into: KEP; Big SAAS; b-SAAS; Little SAAS; l-SAAS; N-proSAAS; Big PEN-LEN; b-PEN-LEN; SAAS CT(1-49); PEN; Little LEN; l-LEN; Big LEN; b-LEN; SAAS CT(25-40))]
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MSGSSARSSHLSQPVVKSVLVYRNGDPFYAGRRVVIHEKKVSSFEVFLKEVTGGVQAPFG
AVRNIYTPRTGHRIRKLDQIQSGGNYVAGGQEAFKKLNYLDIGEIKKRPMEVVNTEVKPV
IHSRINVSARFRKPLQEPCTIFLIANGDLINPASRLLIPRKTLNQWDHVLQMVTEKITLR
SGAVHRLYTLEGKLVESGAELENGQFYVAVGRDKFKKLPYSELLFDKSTMRRPFGQKASS
LPPIVGSRKSKGSGNDRHSKSTVGSSDNSSPQPLKRKGKKEDVNSEKLTKLKQNVKLKNS
QETIPNSDEGIFKAGAERSETRGAAEVQEDEDTQVEVPVDQRPAEIVDEEEDGEKANKDA
EQKEDFSGMNGDLEEEGGREATDAPEQVEEILDHSEQQARPARVNGGTDEENGEELQQVN
NELQLVLDKERKSQGAGSGQDEADVDPQRPPRPEVKITSPEENENNQQNKDYAAVA
Target Bioclass
Other
Subcellular location
Secreted
Function
May function in the control of the neuroendocrine secretory pathway. Proposed be a specific endogenous inhibitor of PCSK1. ProSAAS and Big PEN-LEN, both containing the C-terminal inhibitory domain, but not the further processed peptides reduce PCSK1 activity in the endoplasmic reticulum and Golgi. It reduces the activity of the 84 kDa form but not the autocatalytically derived 66 kDa form of PCSK1. Subsequent processing of proSAAS may eliminate the inhibition. Slows down convertase-mediated processing of proopiomelanocortin and proenkephalin. May control the intracellular timing of PCSK1 rather than its total level of activity.; [Big LEN]: Endogenous ligand for GPR171. Neuropeptide involved in the regulation of feeding.; [PEN]: Endogenous ligand for GPR171. Neuropeptide involved in the regulation of feeding.
Uniprot ID
Q9UHG2
Ensemble ID
ENST00000218230.6
HGNC ID
HGNC:17301

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
FBPP2
 Probe Info  		2.88  LDD0054  [1]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0008  Tranylcypromine SH-SY5Y 2.88  LDD0054  [1]

References

1 Tranylcypromine specificity for monoamine oxidase is limited by promiscuous protein labelling and lysosomal trapping. RSC Chem Biol. 2020 Aug 12;1(4):209-213. doi: 10.1039/d0cb00048e. eCollection 2020 Oct 1.
Mass spectrometry data entry: PXD018580