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

F2 (P00734) - Overview - Molecular Target Synopsis

Protein


F2, Prothrombin
Enzyme Classification 3.4.21.5
UniProt P00734

Also Known as THRB_HUMAN, F2

Thrombin, which cleaves bonds after Arg and Lys, converts fibrinogen to fibrin and activates factors V, VII, VIII, XIII, and, in complex with thrombomodulin, protein C. Functions in blood homeostasis, inflammation and wound healing. Heterodimer (named alpha-thrombin) of a light and a heavy chain; disulfide-linked. Forms a heterodimer with SERPINA5.

6P9U
CRYSTAL STRUCTURE OF HUMAN THROMBIN MUTANT W215A
RCSB/PDB
Inspect Structure
See all 3D Structures for F2

Isoforms / Transcripts (Protein Coding)


Drugs


F2 is targeted by Approved Drugs Dabigatran Etexilate Mesylate, Lepirudin, Bivalirudin, Argatroban, Desirudin, Antithrombin Alfa. (see details)
Dabigatran Etexilate Mesylate
Lepirudin
Bivalirudin
Argatroban
Desirudin
Antithrombin Alfa

Sub-cellular localization


UniProt: F2 is active in the following subcellular-locations: extracellular space, secreted.
GO terms: F2 is active in the following subcellular-locations: blood microparticle, endoplasmic reticulum lumen, extracellular exosome, extracellular region, extracellular space, Golgi lumen, plasma membrane.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project F2 has gain in 2 cell-lines, loss in 0 cell-lines and no signal in 1003 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: NCI_H460, SK_OV_3, LOXIMVI

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: Hep G2, C3A, JHH-7

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: HepG2, SK-N-SH, NHLF

(see details)

3D Structures


For F2 there are:
400 structures (884 chains) solved
343 are solved in complex with at least one small molecule ligand
2 are solved with an approved drug

F2 is solved in complex with the approved drug(s):

PRL/PROFLAVINE (1BCU_H),
BGC/DEXTROSE (3P70_B, 3P70_F, 3P70_H).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


F2 has been screened with 9030 compounds (11635 bioactivities), 3002 compounds have bioactivities that show binding affinity of <= 500nM (3675 bioactivities). (see details)