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

F12 (P00748) - Overview - Molecular Target Synopsis

Protein


F12, Coagulation factor XII
Enzyme Classification 3.4.21.38
UniProt P00748

Also Known as FA12_HUMAN, F12

Factor XII is a serum glycoprotein that participates in the initiation of blood coagulation, fibrinolysis, and the generation of bradykinin and angiotensin. Prekallikrein is cleaved by factor XII to form kallikrein, which then cleaves factor XII first to alpha-factor XIIa and then trypsin cleaves it to beta-factor XIIa. Alpha-factor XIIa activates factor XI to factor XIa. Interacts with HRG; the interaction, which is enhanced in the presence of zinc ions and inhibited by heparin-binding, inhibits factor XII autoactivation and contact-initiated coagulation.

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
615ENSG00000131187ENST00000253496ENSP00000253496P00748-1

Sub-cellular localization


UniProt: F12 is active in the following subcellular-locations: secreted.
GO terms: F12 is active in the following subcellular-locations: collagen-containing extracellular matrix, extracellular exosome, extracellular region, extracellular space, plasma membrane, rough endoplasmic reticulum.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project F12 has gain in 2 cell-lines, loss in 2 cell-lines and no signal in 1001 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: MCF7, SR, HCC_2998

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: DV-90, HuH-7, SR-786

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: A549, NHLF, HSMM

(see details)

3D Structures


For F12 there are:
6 structures (8 chains) solved
3 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


F12 has been screened with 208 compounds (228 bioactivities), 5 compounds have bioactivities that show binding affinity of <= 500nM (5 bioactivities). (see details)