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

PCSK4 (Q6UW60) - Overview - Molecular Target Synopsis

Protein


PCSK4, Proprotein convertase subtilisin/kexin type 4
Enzyme Classification 3.4.21.-
UniProt Q6UW60

Also Known as PCSK4_HUMAN, PCSK4, PC4

Proprotein convertase involved in the processing of hormone and other protein precursors at sites comprised of pairs of basic amino acid residues (By similarity). In males, important for ADAM2 processing as well as other acrosomal proteins with roles in fertilization and critical for normal fertilization events such as sperm capacitation, acrosome reaction and binding of sperm to zona pellucida (By similarity). Plays also a role in female fertility, involved in the regulation of trophoblast migration and placental development, may be through the proteolytical processing and activation of proteins such as IGF2 (PubMed:16040806). May also participate in folliculogenesis in the ovaries. The proPCSK4 form interacts with HSPA5; the interaction takes place at the endoplasmic reticulum.

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: PCSK4 is active in the following subcellular-locations: acrosome membrane, cytoplasmic vesicle, membrane, secretory vesicle.
GO terms: PCSK4 is active in the following subcellular-locations: acrosomal membrane, acrosomal vesicle, integral component of Golgi membrane, membrane, trans-Golgi network.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project PCSK4 has gain in 0 cell-lines, loss in 4 cell-lines and no signal in 1001 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: TK_10, HL_60, ACHN

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: NCI-H345, HCC364, SUM 1315M02

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: SK-N-SH, K562, NHLF

(see details)

RNA Interference


PCSK4 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 PCSK4 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


PCSK4 has been screened with 6 compounds (6 bioactivities), 1 compounds have bioactivities that show binding affinity of <= 500nM (1 bioactivities). (see details)