Summary for peptidase S01.216: coagulation factor Xa

Summary Gene structure Alignment Tree Sequences Sequence features Distribution Structure Literature Human EST Mouse EST Substrates Inhibitors Pharma

 

Names
MEROPS Namecoagulation factor Xa
Other namesF10 g.p. (Homo sapiens) (activated), Stuart factor (activated), prothrombase, prothrombinase, thrombokinase
Domain architecture
MEROPS Classification
Classification Clan PA >> Subclan PA(S) >> Family S1 >> Subfamily A >> S01.216
Holotypecoagulation factor Xa (Homo sapiens), Uniprot accession P00742 (peptidase unit: 235-469), MERNUM MER0000212
History Identifier created: Handbook of Proteolytic Enzymes (1998) Academic Press, London.
Activity
Catalytic typeSerine
PeplistIncluded in the Peplist with identifier PL00310
NC-IUBMBSubclass 3.4 (Peptidases) >> Sub-subclass 3.4.21 (Serine endopeptidases) >> Peptidase 3.4.21.6
EnzymologyBRENDA database
Proteolytic eventsCutDB database (14 cleavages)
Activity statushuman: active (Brown et al., 2004)
mouse: active (Heidtmann et al., 1998)
BiotechnologyReagent for cleavage of recombinant fusion proteins (Jenny et al., 2003).
PhysiologyConverts prothrombin to thrombin in blood coagulation, and can also activate factors V, VII and VIII.
KnockoutKnockout mice have been described by Dewerchin et al. (2000), and suggested to form an effective model for the bleeding disorders observed in severe factor X deficiency in humans.
Pharmaceutical relevanceBecause of its role in converting prothrombin to thrombin in blood coagulation, activated factor X is a drug target for control of coagulation (Choi-Sledeski et al., 2003). It has been reported that synthetic inhibitors are effective antithrombotic agents in animal models, with a low risk of bleeding (Ieko et al., 2004).
Pathways KEGGComplement and coagulation cascades
Other databases WIKIPEDIAhttp://en.wikipedia.org/wiki/Coagulation_factor_Xa
Cleavage site specificity Explanations of how to interpret the following cleavage site sequence logo and specificity matrix can be found here.
Cleavage patternai/-/Gpf/RScissile bondtsi/vf/-/g (based on 59 cleavages)
weblogo
Specificity matrix
 
Amino acid P4 P3 P2 P1 P1' P2' P3' P4'
Gly 1 3 30 0 1 0 7 13
Pro 4 0 10 0 0 0 1 1
Ala 14 4 1 0 0 3 2 1
Val 0 2 0 0 2 12 0 0
Leu 6 4 2 0 3 1 1 3
Ile 12 0 2 0 8 1 0 5
Met 1 0 0 0 1 2 2 0
Phe 6 8 8 0 0 9 4 1
Tyr 1 1 0 0 0 1 1 0
Trp 1 0 2 0 0 0 0 0
Ser 2 4 0 0 9 6 5 4
Thr 1 1 0 0 12 2 5 2
Cys 0 0 0 0 2 0 1 0
Asn 0 2 0 0 1 1 2 3
Gln 1 5 0 0 2 1 1 2
Asp 0 6 1 0 0 2 0 3
Glu 3 11 3 0 0 1 5 0
Lys 1 3 0 8 1 1 2 3
Arg 2 1 0 51 0 0 1 2
His 0 0 0 0 1 0 3 0
Specificity from combinatorial peptides
 
Organism comment P4 P3 P2 P1 P1' P2' P3' P4' optimal substrate fluorophore or acceptor-donor pair Reference
Homo sapiens recombinant n/broad R/broad R R - - - - nRRR ACC Harris et al., 2000
Homo sapiens recombinant I/R/P F/R F/G/W R - - - - IFFR AMC Furlong et al., 2002
Bos taurus recombinant - - - - F/A/M G/A/F G/N/P - xxxx+FGGx Abz-Dnp Ludeman et al., 2003
Homo sapiens recombinant - Q/G/H F - S L S/H - xQFx+SLSx Abz-EDDnp Bianchini et al., 2002
Human genetics
Gene symbol Locus Megabases Ensembl Entrez gene Gene Cards OMIM
F10 13q34 ENSG00000126218 2159 F10 227600
Mouse genetics
Gene symbol Position Megabases Ensembl Entrez gene MGI
F10 8:A1.1 ENSMUSG00000031444 14058 MGI:103107