Tchem FURIN Furin

Protein Summary

Description

Ubiquitous endoprotease within constitutive secretory pathways capable of cleavage at the RX(K/R)R consensus motif (PubMed:11799113, PubMed:1629222, PubMed:1713771, PubMed:2251280, PubMed:24666235, PubMed:25974265, PubMed:7592877, PubMed:7690548, PubMed:9130696). Mediates processing of TGFB1, an essential step in TGF-beta-1 activation (PubMed:7737999). (Microbial infection) Probably cleaves and activates anthrax and diphtheria toxins. (Microbial infection) Required for H7N1 and H5N1 influenza virus infection probably by cleaving hemagglutinin. This gene encodes a member of the subtilisin-like proprotein convertase family, which includes proteases that process protein and peptide precursors trafficking through regulated or constitutive branches of the secretory pathway. It encodes a type 1 membrane bound protease that is expressed in many tissues, including neuroendocrine, liver, gut, and brain. The encoded protein undergoes an initial autocatalytic processing event in the ER and then sorts to the trans-Golgi network through endosomes where a second autocatalytic event takes place and the catalytic activity is acquired. The product of this gene is one of the seven basic amino acid-specific members which cleave their substrates at single or paired basic residues. Some of its substrates include proparathyroid hormone, transforming growth factor beta 1 precursor, proalbumin, pro-beta-secretase, membrane type-1 matrix metalloproteinase, beta subunit of pro-nerve growth factor and von Willebrand factor. It is also thought to be one of the proteases responsible for the activation of HIV envelope glycoproteins gp160 and gp140 and may play a role in tumor progression. This gene is located in close proximity to family member proprotein convertase subtilisin/kexin type 6 and upstream of the FES oncogene. Alternative splicing results in multiple transcript variants. [provided by RefSeq, Jan 2014]

Uniprot Accession IDs

• P09958
• Q14336
• Q6LBS3
• Q9UCZ5

Gene Name

• FURIN

Ensembl ID

• ENST00000268171
• ENSP00000268171
• ENSG00000140564
• ENST00000610579
• ENSP00000484952
• ENST00000618099
• ENSP00000483552

Symbol

• FUR
• PACE
• PCSK3
• FUR
• PACE
• SPC1
• PCSK3

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
protein domain	1
biological process	0.93
molecular function	0.91
cellular component	0.88
hub protein	0.75

Protein Classes

PANTHER Classes

Protein / ... / Serine Protease / Furin

DTO Classes

Protein / Enzyme / Protease / Serine Protease / Furin

IDG Development Level Summary

Tdark

These are targets about which virtually nothing is known. They do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 2335.33   (req: < 5)

Gene RIFs: 122   (req: <= 3)

Antibodies: 394   (req: <= 50)

Tbio

These targets do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 2335.33   (req: >= 5)

Gene RIFs: 122   (req: > 3)

Antibodies: 394   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 35

Tchem

Target has at least one ChEMBL compound with an activity cutoff of < 30 nM - AND - satisfies the preceding conditions

Active Ligands: 289

Tclin

Target has at least one approved drug - AND - satisfies the preceding conditions

Active Drug: 0

Expression Data (0 Tissues)

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No expression data found

Protein Sequence and Structure

Residue Counts

Protein Sequence

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Related Tools (4)

Target Illumination GWAS Analytics (TIGA)

TIGA scores and ranks GWAS discovered associations according to the quantity and quality of the evidence supporting the association.

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GENEVA

GENEVA (GENe Expression Variance Analysis) allows you to identify RNA-sequencing datasets from the Gene Expression Omnibus (GEO) that contain conditions modulating a gene or a gene signature.

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GlyGen

GlyGen is a data integration and dissemination project for carbohydrate and glycoconjugate related data.

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ARCHS4

ARCHS4 provides access to gene-function predictions based on RNA-seq co-expression, and gene expression levels across cell and tissues.

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Approved Drugs (0)

No approved drugs found

Active Ligands (289)

Explore Active Ligands

1 – 10 of 289

CHEMBL3126388

FURINTchem Enzyme

pKi : 9.92

CHEMBL568525

FURINTchem Enzyme

pKi : 8.2

phenylacetyl-Arg-Val-Arg-4-amidinobenzylamide

FURINTchem Enzyme

pKi : 8.8

CHEMBL3115771

FURINTchem Enzyme

pKi : 8.51

CHEMBL3115770

FURINTchem Enzyme

pKi : 8.28

CHEMBL569918

FURINTchem Enzyme

pKi : 8.44

CHEMBL569280

FURINTchem Enzyme

pKi : 7.07

CHEMBL568067

FURINTchem Enzyme

pKi : 6.76

CHEMBL1645024

FURINTchem Enzyme

pKi : 6.24

CHEMBL4065072

FURINTchem Enzyme

pKi : 9.52

Protein-Protein Interactions (264)

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1 – 10 of 264

• See Interactions on String-DB

MPRIP

Tbio

Family:  Enzyme

Novelty:  0.03253403

p_int:  0.999969667

p_ni:  0.000030333

p_wrong:  1e-9

Data Source:  BioPlex

SCPEP1

Tbio

Family:  Enzyme

Novelty:  0.08603794

p_int:  0.999949502

p_ni:  0.000050493

p_wrong:  5e-9

Score:  0.179

Data Source:  BioPlex,STRINGDB

PPP1R10

Tbio

Family:  Enzyme

Novelty:  0.01119155

p_int:  0.999839567

p_ni:  0.000160433

Data Source:  BioPlex

ZC3H4

Tbio

Novelty:  0.14897433

p_int:  0.999726741

p_ni:  0.000272185

p_wrong:  0.000001074

Data Source:  BioPlex

LEMD3

Tbio

Novelty:  0.00579701

p_int:  0.999418037

p_ni:  0.000581961

p_wrong:  2e-9

Data Source:  BioPlex

SERPINA5

Tbio

Family:  Enzyme

Novelty:  0.00152504

p_int:  0.999268525

p_ni:  0.000731409

p_wrong:  6.6e-8

Score:  0.446

Data Source:  BioPlex,STRINGDB

ATE1

Tbio

Family:  Enzyme

Novelty:  0.01672896

p_int:  0.999010489

p_ni:  0.000989512

Data Source:  BioPlex

SAFB

Tbio

Novelty:  0.01750671

p_int:  0.995516788

p_ni:  0.004483207

p_wrong:  5e-9

Data Source:  BioPlex

RHOBTB3

Tbio

Novelty:  0.09149494

p_int:  0.99495582

p_ni:  0.005044

p_wrong:  1.8e-7

Data Source:  BioPlex

SERPINE2

Tbio

Novelty:  0.00246375

p_int:  0.994270975

p_ni:  0.005729009

p_wrong:  1.6e-8

Score:  0.256

Data Source:  BioPlex,STRINGDB

Nearest Tclin Targets

Nearest Tclin calculations are only available for targets with KEGG Pathway annotations.

Pathways (54)

Reactome (40)

PathwayCommons (14)

Activation of Matrix Metalloproteinases (R-HSA-1592389)

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Data Source	Name	Explore in Pharos	Explore in Source
Reactome	Activation of Matrix Metalloproteinases	33 targets	R-HSA-1592389
Reactome	Amyloid fiber formation	79 targets	R-HSA-977225
Reactome	Assembly Of The HIV Virion	16 targets	R-HSA-175474
Reactome	Assembly of active LPL and LIPC lipase complexes	19 targets	R-HSA-8963889
Reactome	Collagen degradation	40 targets	R-HSA-1442490

Name	Explore in Pharos	Explore in Source
Activation of Matrix Metalloproteinases	33 targets	R-HSA-1592389
Amyloid fiber formation	79 targets	R-HSA-977225
Assembly Of The HIV Virion	16 targets	R-HSA-175474
Assembly of active LPL and LIPC lipase complexes	19 targets	R-HSA-8963889
Collagen degradation	40 targets	R-HSA-1442490

Viral Interactions (0)

No viral interactions found

Gene Ontology Terms (48)

Functions (8)

Components (13)

Processes (27)

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1 – 8 of 8

GO Term	Evidence	Assigned by
endopeptidase activity	Inferred from Direct Assay (IDA)	BHF-UCL
nerve growth factor binding	Inferred from Direct Assay (IDA)	BHF-UCL
peptidase activity	Inferred from Direct Assay (IDA)	UniProtKB
peptide binding	Inferred from Direct Assay (IDA)	BHF-UCL
serine-type endopeptidase activity	Inferred from Direct Assay (IDA)	UniProtKB
serine-type endopeptidase inhibitor activity	Inferred from Direct Assay (IDA)	BHF-UCL
protease binding	Inferred from Physical Interaction (IPI)	BHF-UCL
metal ion binding	Inferred from Electronic Annotation (IEA)	UniProtKB-KW

Disease Associations (null)

No disease associations found

GWAS Traits (57)

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GWAS Trait	EFO ID	Study Count	SNP Count	Beta Count	Odds Ratio	Evidence (Mean Rank Score)	Provenance
coronary artery disease	EFO_0001645	8	7	5	1.1	98.6
type 2 diabetes mellitus	MONDO_0005148	9	4	5	1.1	98.3
red blood cell distribution width	EFO_0005192	4	5	6		96.1
diastolic blood pressure	EFO_0006336	4	2	4		95.2
birth weight	EFO_0004344	4	4	4		94.9

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GWAS Trait	EFO ID	Beta Count	Odds Ratio	Evidence (Mean Rank Score)	Provenance
coronary artery disease	EFO_0001645	5	1.1	98.6
type 2 diabetes mellitus	MONDO_0005148	5	1.1	98.3
red blood cell distribution width	EFO_0005192	6		96.1
diastolic blood pressure	EFO_0006336	4		95.2
birth weight	EFO_0004344	4		94.9

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UniProt Keyword Find Similar Targets

No Header	No Header
3D-structure
Autocatalytic cleavage
Calcium
Cell membrane
Cleavage on pair of basic residues
Complete proteome
Disulfide bond
Endosome
Glycoprotein
Golgi apparatus

GWAS Trait Find Similar Targets

No Header	No Header
age at first sexual intercourse measurement
Agents acting on the renin-angiotensin system use measurement
angina pectoris
antisocial behaviour measurement
Antithrombotic agent use measurement
apolipoprotein A 1 measurement
appendicular lean mass
attention deficit hyperactivity disorder
autism spectrum disorder
balding measurement

MGI Phenotype Find Similar Targets

No Header	No Header
cardiovascular system phenotype
digestive/alimentary phenotype
embryo phenotype
growth/size/body region phenotype
hematopoietic system phenotype
immune system phenotype
integument phenotype
limbs/digits/tail phenotype
mortality/aging
nervous system phenotype

IDG Resources

No IDG generated resources found

Orthologs (11)

1 – 5 of 11

Species	Name	Source ID	Gene ID	OMA	EggNOG	Inparanoid
Chimp	furin, paired basic amino acid cleaving enzyme	VGNC:7766	453652
Macaque	furin, paired basic amino acid cleaving enzyme		715813
Mouse	furin (paired basic amino acid cleaving enzyme)	MGI:97513	18550
Rat	furin (paired basic amino acid cleaving enzyme)	RGD:3274	54281
Dog	furin, paired basic amino acid cleaving enzyme	VGNC:41010	488746

Species	Name	OMA	EggNOG	Inparanoid
Chimp	furin, paired basic amino acid cleaving enzyme
Macaque	furin, paired basic amino acid cleaving enzyme
Mouse	furin (paired basic amino acid cleaving enzyme)
Rat	furin (paired basic amino acid cleaving enzyme)
Dog	furin, paired basic amino acid cleaving enzyme

Publication Statistics

PubMed Score 2335.33

PubMed score by year

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PubTator Score 1027.35

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Related Publications

Text Mined References (204)

GeneRif Annotations (122)

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PMID	Year	Title