Molecular Target Synopsis
Overview
Domains and Structures
Drugs and Clinical Candidates
Druggability
Chemistry
Ligand Efficiency Plot
Pathways
Family Cladogram
Interaction Network
Gene Expression
Gene Copy Number Variation
RNAi
Mutations
Germline Genetics

PCSK6 (P29122) - Overview - Molecular Target Synopsis

Protein


PCSK6, Proprotein convertase subtilisin/kexin type 6
Enzyme Classification 3.4.21.-
UniProt P29122

Also Known as PCSK6_HUMAN, PCSK6, PACE4

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. The PACE4A-I precursor protein seems to exist in the reticulum endoplasmic as both a monomer and a dimer-sized complex whereas mature PACE4A-I exists only as a monomer, suggesting that propeptide cleavage affects its tertiary or quaternary structure. Interacts (immature form including the propeptide) with RCN3; probably involved in the maturation and the secretion of PCSK6 (PubMed:16433634).

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: PCSK6 is active in the following subcellular-locations: endomembrane system, endoplasmic reticulum, secreted.
GO terms: PCSK6 is active in the following subcellular-locations: cell surface, collagen-containing extracellular matrix, endoplasmic reticulum, extracellular region, extracellular space, Golgi lumen, membrane, plasma membrane.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project PCSK6 has gain in 2 cell-lines, loss in 1 cell-lines and no signal in 1001 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: M14, HT29, NCI_H322M

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: Hs 255.T, Hs 675.T, SK-MEL-1

In Array Express (RNA-seq of long poly adenylated RNA and long non poly adenylated RNA from ENCODE cell lines), the highest expressing cell lines are: K562, SK-N-SH, NHLF

(see details)

RNA Interference


PCSK6 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: . (see details)

3D Structures


At greater than 50% identity similarity to PCSK6 there are:
21 structures (44 chains) solved
3 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


PCSK6 has been screened with 42 compounds (43 bioactivities), 33 compounds have bioactivities that show binding affinity of <= 500nM (34 bioactivities). (see details)