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

FURIN (P09958) - Overview - Molecular Target Synopsis

Protein


FURIN, Furin
Enzyme Classification 3.4.21.75
UniProt P09958

Also Known as FURIN_HUMAN, FURIN, FUR, PACE, PCSK3

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. Interacts with FLNA (By similarity). Binds to PACS1 which mediates TGN localization and connection to clathrin adapters (PubMed:11331585).

6HLD
X-RAY STRUCTURE OF FURIN IN COMPLEX WITH THE CYCLIC PEPTIDE C[SUCCINYL-PHE-2-NAL-(ARG)3-LYS]-LYS-4-AMBA
RCSB/PDB
Inspect Structure
See all 3D Structures for FURIN

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: FURIN is active in the following subcellular-locations: cell membrane, endosome membrane, golgi apparatus, secreted, trans-golgi network membrane.
GO terms: FURIN is active in the following subcellular-locations: cell surface, endoplasmic reticulum, endosome membrane, extracellular exosome, extracellular region, Golgi lumen, Golgi membrane, integral component of Golgi membrane, membrane, membrane raft, plasma membrane, trans-Golgi network, trans-Golgi network transport vesicle.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project FURIN has gain in 2 cell-lines, loss in 0 cell-lines and no signal in 1002 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: SR, SK_OV_3, EKVX

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: HuH-7, MKN-74, HCC2302

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, HUVEC, IMR-90

(see details)

3D Structures


For FURIN there are:
20 structures (36 chains) solved
2 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


FURIN has been screened with 455 compounds (506 bioactivities), 130 compounds have bioactivities that show binding affinity of <= 500nM (132 bioactivities). (see details)