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

SERPINC1 (P01008) - Overview - Molecular Target Synopsis

Protein


SERPINC1, Antithrombin-III
UniProt P01008

Also Known as ANT3_HUMAN, SERPINC1, AT3

Most important serine protease inhibitor in plasma that regulates the blood coagulation cascade. AT-III inhibits thrombin, matriptase-3/TMPRSS7, as well as factors IXa, Xa and XIa. Its inhibitory activity is greatly enhanced in the presence of heparin. Forms protease inhibiting heterodimer with TMPRSS7.

4EB1 deposition date (2012-03-23)
HYPERSTABLE IN-FRAME INSERTION VARIANT OF ANTITHROMBIN
RCSB/PDB
Inspect Structure
See all 3D Structures for SERPINC1

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
464ENSG00000117601ENST00000367698ENSP00000356671P01008-1

Drugs


SERPINC1 is targeted by Approved Drugs Enoxaparin Sodium, Ardeparin Sodium, Tinzaparin Sodium, Heparin Calcium, Heparin Sodium, Dalteparin Sodium. (see details)
Enoxaparin Sodium
Ardeparin Sodium
Tinzaparin Sodium
Heparin Calcium
Heparin Sodium
Dalteparin Sodium

Sub-cellular localization


UniProt: SERPINC1 is active in the following subcellular-locations: extracellular space, secreted.
GO terms: SERPINC1 is active in the following subcellular-locations: blood microparticle, endoplasmic reticulum lumen, extracellular exosome, extracellular region, extracellular space, plasma membrane.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project SERPINC1 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: LOXIMVI, NCI_H522, OVCAR_4

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: C3A, NCI-H1781, Hep G2

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, NHLF, HSMM

(see details)

RNA Interference


SERPINC1 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


For SERPINC1 there are:
27 structures (51 chains) solved
24 are solved in complex with at least one small molecule ligand
2 are solved with an approved drug

SERPINC1 is solved in complex with the approved drug(s):

NTO/FONDAPARINUX (2GD4_C, 2GD4_I, 3EVJ_I, 3EVJ_L).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


SERPINC1 has been screened with 33 compounds (58 bioactivities), 5 compounds have bioactivities that show binding affinity of <= 500nM (5 bioactivities). (see details)